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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 8776. Отображено 100.
02-02-2012 дата публикации

Novel lipids and compositions for the delivery of therapeutics

Номер: US20120027796A1
Автор: David Butler, Jayaprakash K. Narayanannair, Kallanthottathil G. Rajeev, Laxmab Eltepu, Muthiah Manoharan, Muthusamy Jayaraman
Принадлежит: Alnylam Pharmaceuticals Inc

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures: (Formula (I) or (XXXV)).

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Номер записи: 1
19-04-2012 дата публикации

Novel lipids and compositions for the delivery of therapeutics

Номер: US20120095075A1
Автор: David Butler, Kallanthottathil G. Rajeev, Laxman Eltepu, Muthiah Manoharan, Muthusamy Jayaraman, Narayanannair K. Jayaprakash
Принадлежит: Alnylam Pharmaceuticals Inc

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure:

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Номер записи: 2
07-06-2012 дата публикации

Novel formulation of meloxicam

Номер: US20120141548A1
Автор: Aaron Dodd, Adrian Russell, Felix Meiser, H William Bosvch, Marck Norret
Принадлежит: Fundacion Universidad del Norte Co

The present invention relates to methods for producing particles of meloxicam using dry milling processes as well as compositions comprising meloxicam, medicaments produced using meloxicam in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of meloxicam administered by way of said medicaments.

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Номер записи: 3
27-12-2012 дата публикации

Microparticle dispersion liquid manufacturing method and microparticle dispersion liquid manufacturing apparatus

Номер: US20120328480A1
Автор: Gen Takebe, Mitsuo Hiramatsu, Tokio Takagi
Принадлежит: Hamamatsu Photonics KK

In a dissolving step, a poorly soluble drug and a dispersion stabilizer are dissolved in a volatile organic solvent. In a fixing step, the organic solvent, contained in a solution obtained in the dissolving step, is removed by evaporation, pellet-form residues are obtained by the organic solvent removal, and the residues are fixed on respective bottom surfaces of a plurality of locations of a container. In a water injecting step, water is injected into each of a plurality of recesses of the container. In an irradiating step, laser light L, emitted from a light irradiating unit, is irradiated simultaneously or successively on the residues fixed on the respective bottom surfaces of the recesses of the container, and the residues are thereby pulverized and made into microparticles and a microparticle dispersion liquid, constituted of the microparticles being dispersed in the water, is manufactured.

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Номер записи: 4
07-02-2013 дата публикации

Synthetic nanostructures including nucleic acids and/or other entities

Номер: US20130034599A1
Автор: Andrea Luthi, C. Shad Thaxton, Chad A. Mirkin, David M. Leander, Kaylin M. MCMAHON, Raja Kannan Mutharasan, Sushant Tripathy
Принадлежит: Northwestern University

Articles, compositions, kits, and methods relating to nanostructures, including synthetic nanostructures, are provided. Certain embodiments described herein include structures having a core-shell type arrangement; for instance, a nanostructure core may be surrounded by a shell including a material, such as a lipid bilayer, and may include other components such as oligonucleotides. In some embodiments, the structures, when introduced into a subject, can be used to deliver nucleic acids and/or can regulate gene expression. Accordingly, the structures described herein may be used to diagnose, prevent, treat or manage certain diseases or bodily conditions. In some cases, the structures are both a therapeutic agent and a diagnostic agent.

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Номер записи: 5
07-02-2013 дата публикации

Method and a system for producing thermolabile nanoparticles with controlled properties and nanoparticles matrices made thereby

Номер: US20130035279A1
Автор: Amol Ashok Pawar, Chandra Venkataraman
Принадлежит: INDIAN INSTITUTE OF TECHNOLOGY BOMBAY

This disclosure relates to a method and a system of producing nanoparticles and nanoparticle matrices of thermolabile, biocompatible matrix materials, like lipids and biopolymers with controlled properties. A prototype pulse-heat aerosol system is described for single-step production of free, thermolabile nanoparticles with sufficient control over size, morphology and crystallinity with controlled-release properties, for possible therapeutic, cosmetic or diagnostic use. Nanoparticles of the range 50 to 500 nm are obtained and are found suitable for controlled drugs delivery.

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Номер записи: 6
28-02-2013 дата публикации

Use of Gold Nanoclusters in Ameliorating Oxidate Stress and/or Aging

Номер: US20130052270A1
Автор: Cheng-An Lin, Hsueh-Hsiao Wang, Hung-I Yeh, Walter H. Chang
Принадлежит: CHUNG YUAN CHRISTIAN UNIVERSITY, MACKAY MEMORIAL HOSPITAL

Disclosed herein is the novel use of a gold nanocluser for ameliorating oxidative stress and/or aging of a cultured cell or a subject having an oxidative stress and/or aging condition mediated by a vascular factor. The gold nanocluster has a particle size ranging from about 0.1 to 20 nm, and preferably is dihydrolipoic acid (DHLA) coated gold nanocluster.

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Номер записи: 7
14-03-2013 дата публикации

Novel cationic lipids and methods of use thereof

Номер: US20130064894A1
Автор: Alan Martin, James Heyes, Mark Wood
Принадлежит: PROTIVA BIOTHERAPEUTICS INC

The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of a specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.

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Номер записи: 8
27-06-2013 дата публикации

Methods and compositions for cellular drug release

Номер: US20130164335A1
Автор: CHENG Chen, Feng-Huei Lin
Принадлежит: National Health Research Institutes

Methods and compositions for producing a cellular drug release are disclosed. The method comprises: a) providing a composition comprising a therapeutically effective amount of a pharmacological agent adsorbed onto mesoporous hydroxyapatite (HAP) with hydrophobic surfaces; b) exposing the composition to a cell; c) causing entry of the mesoporous HAP into the cell and degradation of the HAP in the lysosomes of the cell and desorption of the agent from the mesoporous HAP; d) causing release of the desorbed agent from the lysosomes into the cytoplasm of the cell; and e) causing release of the desorbed agent to outside the cell. The composition comprises a) mesoporous HAP with hydrophobic surfaces; and b) a therapeutically effective amount of a pharmacological agent, adsorbed onto the hydrophobic surfaces of the mesoporous. HAP. The composition is characterized in that it constantly releases the agent in vivo for a period of at least 4 weeks.

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Номер записи: 9
29-08-2013 дата публикации

Sustained-Release Pharmaceutical Composition

Номер: US20130225492A1
Автор: Hiroaki Matsubara, Masanori Fukushima, Satoaki Matoba, Shigeki Hijikata, Tsutomu Sato, Yu Aso
Принадлежит: Kaken Pharmaceutical Co Ltd, Koken Co Ltd, Kyoto Prefectural Public Univ Corp, KYOTO UNIVERSITY

Provided is a pharmaceutical composition, including a drug and a collagen, in which the composition is satisfactory in handleability and has sustained-release property. The sustained-release pharmaceutical composition includes: a drug; a collagen; and at least one kind of sugar selected from monosaccharides, disaccharides, trisaccharides, and tetrasaccharides. The inventors of the present invention have found that the in vivo administration of a collagen solution containing a sugar results in the gelation of a collagen. Based on this finding, the inventors have found that a composition containing a drug, a collagen, and a sugar can control the release rate of the drug, and such composition can be used as a sustained-release pharmaceutical composition.

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Номер записи: 10
03-10-2013 дата публикации

Modified polynucleotides for the production of secreted proteins

Номер: US20130259923A1
Автор: Antonin De Fougerolles, Atanu Roy, Jason P. SCHRUM, Jeff Lynn Ellsworth, Justin Guild, Kenechi Ejebe, Kristy M. WOOD, Matthias John, Paul Hatala, Sayda M. ELBASHIR, Stephane Bancel, Susan Whoriskey, Tirtha Chakraborty
Принадлежит: Moderna Therapeutics Inc

The invention relates to compositions and methods for the preparation, manufacture and therapeutic use of polynucleotides, primary transcripts and mmRNA molecules.

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Номер записи: 11
17-10-2013 дата публикации

Novel Low Molecular Weight Cationic Lipids For Oligonucleotide Delivery

Номер: US20130274504A1
Автор: Matthew G. Stanton, Steven L. Colletti
Принадлежит: Individual

The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.

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Номер записи: 12
17-10-2013 дата публикации

Low molecular weight cationic lipids for oligonucleotide delivery

Номер: US20130274523A1
Автор: John A. Bawiec, Iii, Zhengwu J. Deng
Принадлежит: Individual

The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.

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Номер записи: 13
07-11-2013 дата публикации

Stable Formulations for Lyophilizing Therapeutic Particles

Номер: US20130295183A1
Автор: Christina Van Geen Hoven, Greg Troiano, James Wright, Stephen E. Zale, Young-Ho Song
Принадлежит: Bind Therapeutics Inc

The present disclosure generally relates to lyophilized pharmaceutical compositions comprising polymeric nanoparticles which, upon reconstitution, have low levels of greater than 10 micron size particles. Other aspects of the invention include methods of making such nanoparticles.

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Номер записи: 14
13-02-2014 дата публикации

Nanocapsulation of essential oils for preventing or curing infectious diseases alone or with an antibiotic

Номер: US20140045692A1
Автор: Elisabeth Rossines, Jean Pierre Benoit, Marie Laure JOLY-GUILLOU, Patrick Saulnier
Принадлежит: Eydo Pharma, Institut National de la Sante et de la Recherche Medicale INSERM, Universite dAngers

A composition, an encapsulated composition and/or nanoparticles comprising at least one essential oil having a large spectrum antibacterial, antiparasitic, antifungal activity and/or a plant antipathogen, optionally at least one antibiotic and optionally a pharmaceutically acceptable carrier is disclosed. Methods for treating infectious diseases and especially bacterial, parasitic, fungal and/or plant infectious by using this composition, encapsulated composition and/or nanoparticles are also disclosed.

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Номер записи: 15
20-03-2014 дата публикации

Composition comprising lipid nanoparticles and a corticosteroid or vitamin d derivative

Номер: US20140079785A1
Автор: Karsten Petersson, Louise Bastholm Jensen
Принадлежит: Leo Pharma AS

A pharmaceutical composition comprises, as a therapeutically active ingredient, a corticosteroid and/or vitamin D derivative incorporated as a solid solution or dispersion in lipid nanoparticles, said lipid nanoparticles being solid at ambient temperature and comprising a first lipid with a melting point above body temperature, the first lipid being a wax selected from the group consisting of esters of C 12-24 alcohols and C 12-24 fatty acids, glyceryl mono-, di- or triesters of C 12-24 fatty acids, C 12-24 fatty alcohols, and cholesterol, optionally a second lipid which is an oil at ambient temperature and miscible with the first lipid, and a pharmaceutically acceptable surfactant.

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Номер записи: 16
07-01-2016 дата публикации

CONTROLLED RELEASE NANOPARTICLES AND METHODS OF USE

Номер: US20160000724A1
Автор: HALDAR MANAS K., Kulkarni Prajakta S., Mallik Sanku, Srivastava D. K.
Принадлежит:

Provided herein are nanoparticles that include a lipid layer and a compartment surrounded by the lipid layer. The lipid layer may include a lipid and a lipoprotein. The lipid may include a POPE lipid covalently attached to a hydrophilic polymer by a disulfide bond. The lipoprotein may include a trigger protein. The concentration of the first lipid may be between 1 mol % and 30 mol %. The disulfide bond of the first lipid is stable under conditions that include 10% human serum and is broken under conditions that include 50 micromolar glutathione. The hydrophilic polymer may include a PEG molecule. The trigger protein may include an amino acid repeat region, such as (GPX)n. The trigger protein may include a peptide bond that is cleaved by a gelatinase (e.g., gelatinase-B protease), or a member of the ADAM family of proteases (e.g., ADAM10 protease). Also provided are methods of using the nanoparticles. 1. A nanoparticle comprising a lipid layer and a compartment surrounded by the lipid layer ,wherein the lipid layer comprises (i) a first lipid, the first lipid comprising a POPE lipid covalently attached to a hydrophilic polymer by a disulfide bond, and (ii) a lipoprotein, the lipoprotein comprising a trigger protein,wherein the concentration of the first lipid is between 1 mole percent (mol %) and 30 mol %, andwherein the disulfide bond of the first lipid is stable under conditions comprising 10% human serum and is broken under conditions comprising 50 micromolar glutathione.28-. (canceled)9. The nanoparticle of wherein the trigger protein comprises an amino acid repeat region.10. The nanoparticle of wherein the amino acid repeat region comprises (GPX)n claim 9 , wherein X is 4-hydroxyproline or proline claim 9 , and n is at least 3.11. The nanoparticle of wherein the trigger protein comprises a peptide bond that is cleaved by a gelatinase or a member of the ADAM family of proteases.12. The nanoparticle of wherein the gelatinase is gelatinase-B protease.13. The ...

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Номер записи: 17
07-01-2021 дата публикации

NANOPARTICLE CANCER THERAPY

Номер: US20210000751A1
Автор: KEMPSON Ivan Mark, TURNBULL Tyron James
Принадлежит:

Methods of potentiating chemotherapy or radiotherapy are disclosed. The methods comprise administering to a subject in need of chemotherapeutic or radiotherapeutic treatment an effective amount of a composition comprising biocompatible nanoparticles, particularly gold nanoparticles, under conditions in which the nanoparticles alter one or more cell regulatory mechanisms in cells in which the nanoparticles are localised or other cells. Then one or more doses of a chemotherapeutic or radiotherapeutic treatment are administered to the subject either concurrently with or after the nanoparticles have altered the one or more cell regulatory mechanisms in the cells in which the nanoparticles are localised or other cells. Also disclosed are methods of enhancing the effects of chemotherapy or radiotherapy on a cell population, methods of increasing the amount of strand breaks in DNA in a cell, and methods of inducing cancer cell death. 1. A method of potentiating chemotherapy or radiotherapy , the method comprising:administering to a subject in need of chemotherapeutic or radiotherapeutic treatment an effective amount of a composition comprising biocompatible nanoparticles under conditions in which the nanoparticles alter one or more cell regulatory mechanisms and perpetuate DNA double strand breaks in cells in which the nanoparticles are localised or other cells; andadministering one or more doses of a chemotherapeutic or radiotherapeutic treatment to the subject either concurrently with or after the nanoparticles have altered the one or more cell regulatory mechanisms in the cells in which the nanoparticles are localised or other cells, wherein said one or more dose of chemotherapeutic or radiotherapeutic treatment acts on the cells in which the nanoparticles are localised or other cells and the potentiation of the chemotherapy or radiotherapy and said method does not involve interaction of the chemotherapeutic or radiotherapeutic treatment with the biocompatible ...

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Номер записи: 18
02-01-2020 дата публикации

Solid Oral Pharmaceutical Compositions for Isoxazoline Compounds

Номер: US20200000718A1
Автор: Freehauf Keith, Guerino Frank, Lutz Jürgen, Waldron Niki
Принадлежит: Intervet Inc.

A solid oral pharmaceutical composition for delivery of a pharmaceutically acceptable active ingredient to an animal where the composition comprises an isoxazoline compound, a solvent and an excipient, a process for the manufacture of such solid oral pharmaceutical composition and a method of controlling a parasite infection administering such solid oral pharmaceutical composition. 2. The solid oral pharmaceutical composition of wherein the composition is prepared by a method comprisinga. dissolving the isoxazoline compound of formula (I) in a solvent to form an isooxazoline solution;b. adding the isoxazoline solution to a solid carrier and mix to form a first mixture;c. adding all other dry excipients to the first mixture and mix to form a second mixture;d. adding liquid ingredients, qlycerol and soybean oil, to the second dry mixture;e. mixing to form wet mass;f. melting a polyethylene glycol forming agent and adding to the wet mass;g. mixing to form the final bulk mass; andh. forming soft chewable tablets in a forming machine.3. The solid oral pharmaceutical composition of wherein the solid carrier is microcrystalline cellulose.4. The solid oral pharmaceutical composition of wherein the solvent is selected from 2-pyrrolidone claim 1 , dimethyl acetamide or mixtures thereof.5. The solid oral pharmaceutical composition of wherein the solvent is dimethyl acetamide.6. (canceled)7. The solid oral pharmaceutical composition of wherein the isoxazoline compound is fluralaner.8. The solid oral pharmaceutical composition of wherein the isoxazoline compound is 4-[5-(3 claim 1 ,5-dichlorophenyl)-4 claim 1 ,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-N—[(Z)-(methoxyimino)methyl]-2-methyl-benzamide.9. The solid oral pharmaceutical composition of wherein the isoxazoline compound is afoxolaner.10. The solid oral pharmaceutical composition of wherein the isoxazoline compound is 5-[5-(3 claim 1 ,5-Dichlorophenyl)-4 claim 1 ,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-3-methyl-N-[2 ...

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Номер записи: 19
05-01-2017 дата публикации

LIPID NANOPARTICLE COMPOSITIONS AND METHODS AS CARRIERS OF CANNABINOIDS IN STANDARDIZED PRECISION-METERED DOSAGE FORMS

Номер: US20170000744A1
Автор: Kaufman Richard Clark
Принадлежит: NANOSPHERE HEALTH SCIENCES, LLC

This disclosure teaches phospholipid nanoparticle compositions of cannabinoids formed from phospholipids and simpler lipids in an unfired sequential process that encapsulate a high concentration of cannabinoids, and create standardized precision-metered dosage forms of cannabinoids; yielding an increase cannabinoid transport across hydrophobic mucosa; increase the bioavailability of the cannabinoid 2-fold to 8-fold, decrease the dose of cannabinoids 2-fold to 8-fold less than an amount of cannabinoids needed to illicit the same therapeutic effect compared to raw and non-encapsulated cannabinoids; where the nanoparticle dynamic structure reduces the adverse effects of cannabinoids; and enable safe more efficacious cannabinoid therapy. 1. A nanosphere compositional structure comprising encapsulated cannabinoids dispersed into a stable adjustable fluid viscoelastic nanoparticle structure comprised of an outer single layer of essential phospholipids , liquid lipids and excipients; andwherein the nanoparticle structure has a particle size distribution from 50 to 150 nm.23.- (canceled)4. The nanosphere compositional structure of claim 1 , wherein the structure can be administered across the sublingual mucous mucosa and/or the buccal mucosa of a mammal and wherein the structure can enter the systemic circulation.5. The nanopshere compositional structure of claim 1 , wherein the structure is administered across dermal and/or the epidermal barriers and wherein the structure can enter the systemic circulation.6. The nanopshere compositional structure of claim 1 , wherein the structure can be administered across nasal mucous mucosal barriers and wherein the structure can enter the systemic circulation.7. The nanopshere compositional structure of claim 1 , wherein the structure can be administered across the intestinal mucosal barriers and wherein the structure can enter the systemic circulation.8. The nanosphere compositional structure of claim 1 , wherein the nanoparticle is ...

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Номер записи: 20
07-01-2021 дата публикации

INTRADUCTAL METHODS OF TREATMENT OF BREAST DISORDERS

Номер: US20210000920A1
Автор: Quay Steven C.
Принадлежит: Atossa Therapeutics, Inc.

The present invention relates to intraductal methods and compositions for treating subjects having breast disorders. Compositions comprise repolarizing agents and polarization blockading agents capable of repolarizing M2-macrophages to M1-macrophages in the tumor microenvironment, decreasing M2-macrophages, increasing M1-macrophages and/or increasing sensitivity to chemotherapy in the subject. 1. A method of treating a subject having a breast disorder , the method comprising delivering intraductally to the subject a composition comprising a repolarizing agent capable of repolarizing a M2-polarized macrophage , or a blockading agent capable of blocking M2 polarization of macrophages , or both.2. A method of promoting increased sensitivity to chemotherapy in a subject having a breast disorder , comprising: administering intraductally to the subject a composition comprising a repolarizing agent or a blockading agent or both , wherein administration of the composition promotes increased sensitivity to chemotherapy.3. A method for selective reduction of M2 macrophages in a subject having a breast disorder comprising intraductally administering to the subject a composition comprising a repolarizing agent or a blockading agent or both.4. The method of any of the preceding claims , wherein the M2 macrophage phenotype is any one or more of M2a phenotype , M2b phenotype , and M2c phenotype , or a combination thereof.5. The method of any of the preceding claims , wherein the intraductal administration of the composition comprising a repolarizing agent or a blockading agent or both results in one or more of:a. decreased M2 macrophages;b. increased M1-macrophages;c. M1/M2-macrophage homeostasis;d. decreased release of anti-inflammatory cytokines, chemokines or growth factors;e. increased release of pro-inflammatory cytokines, chemokines, or growth factors;f. increased tumoricidal activity of macrophages;g. increased cytotoxic T-lymphocyte infiltration in to TME; andh. increased ...

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Номер записи: 21
07-01-2021 дата публикации

Photodynamically active organosilica nanoparticles and medical uses thereof

Номер: US20210000955A1
Автор: Chenjie Xu, Hongzhong Chen, Huijun Phoebe THAM, Keming Xu, Subramanian Venkatraman, Wei Qi LIM, Yanli Zhao
Принадлежит: NANYANG TECHNOLOGICAL UNIVERSITY

The present application provides an organosilica nanoparticle comprising: (a) a photosensitizer for photodynamic therapy covalently incorporated therein; and (b) optionally, at least one agent encapsulated therein, as well as a pharmaceutical composition comprising said organosilica nanoparticle. Also provided herein are said organosilica nanoparticle or pharmaceutical composition for use as a medicament or in the treatment of a disease, disorder, or condition. More specifically, provided is a method for treating a disease, disorder, or condition in a subject using said aid organosilica nanoparticle or pharmaceutical composition.

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Номер записи: 22
07-01-2016 дата публикации

SUPRAMOLECULAR MAGNETIC NANOPARTICLES

Номер: US20160000918A1
Автор: CHEN Kuan-Ju, Cheon Jinwoo, Noh Seung-hyun, Tseng Hsian-Rong
Принадлежит:

A supramolecular magnetic nanoparticle (SMNP) can be formed by self-assembly of structural components, binding components, terminating components and at least one magnetic nanoparticle. The SMNP can provide on-demand release of a cargo and act as part of an on-demand drug release system. 1. A supramolecular magnetic nanoparticle (SMNP) comprising:a plurality of structural components each including a plurality of binding elements;at least one magnetic nanoparticle each including a plurality of binding elements;a plurality of binding components each including a plurality of binding regions, wherein each of the binding regions is adapted to bind to a binding element;a plurality of terminating components each including a terminating element , wherein the terminating element is adapted to occupy a binding region; anda cargo;wherein the plurality of terminating components are present in a sufficient quantity relative to the plurality of binding regions of the plurality of binding components to terminate further binding.2. The supramolecular magnetic nanoparticle (SMNP) of claim 1 , wherein said plurality of structural components comprises at least one of a dendrimer claim 1 , branched polyethyleneimide claim 1 , linear polyethyleneimide claim 1 , polylysine claim 1 , polylactide claim 1 , polylactide-co-glycolide claim 1 , polyanhydrides claim 1 , poly-ε-caprolactones claim 1 , polymethyl methacrylate claim 1 , poly(N-isopropyl acrylamide) or polypeptides.3. The supramolecular magnetic nanoparticle (SMNP) of claim 2 , wherein said plurality of structural components comprises a dendrimer.4. The supramolecular magnetic nanoparticle (SMNP) of claim 1 , wherein said plurality of terminating components comprises at least one of polyethylene glycol claim 1 , an adamantane derivative claim 1 , target ligands claim 1 , peptides claim 1 , antibodies or proteins.530500. The supramolecular magnetic nanoparticle (SMNP) of claim 1 , wherein the supramolecular magnetic nanoparticle ( ...

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Номер записи: 23
04-01-2018 дата публикации

LIPID NANOPARTICLE COMPOSITIONS

Номер: US20180000953A1
Автор: Almarsson Örn, LAWLOR Ciaran Patrick
Принадлежит:

Disclosed herein are nanoparticle compositions including an mRNA and a lipid component and methods of using the same. The present invention provides compositions and methods involving lipid-containing nanoparticle compositions to deliver mRNA to cells. In one aspect, the invention provides a nanoparticle composition including (i) a lipid component including a phospholipid (which may or may not be unsaturated), a PEG lipid, a structural lipid, and a compound of formula (I) and (ii) an mRNA encoding a polypeptide of interest. 2. A method of delivering an mRNA to a mammalian cell , said method comprising administering to a subject a nanoparticle composition , said composition comprising (i) a lipid component comprising a compound of formula (I) , a phospholipid , a structural lipid , and a PEG lipid; and (ii) an mRNA , said administering comprising contacting said mammalian cell with said nanoparticle composition , whereby said mRNA is delivered to said cell.3. The method of or , wherein said PEG lipid is selected from the group consisting of a PEG-modified phosphatidylethanolamine , a PEG-modified phosphatidic acid , a PEG-modified ceramide , a PEG-modified dialkylamine , a PEG-modified diacylglyceril , and a PEG-modified dialkylglycerol.4. The method of any one of to , wherein said structural lipid is selected from the group consisting of cholesterol , fecosterol , sitosterol , ergosterol , campesterol , stigmasterol , brassicasterol , tomatidine , ursolic acid , and alpha-tocopherol.5. The method of claim 4 , wherein said structural lipid is cholesterol.6. The method of any one of to claim 4 , wherein said phospholipid includes a moiety selected from the group consisting of phosphatidyl choline claim 4 , phosphatidyl ethanolamine claim 4 , phosphatidyl glycerol claim 4 , phosphatidyl serine claim 4 , phosphatidic acid claim 4 , 2-lysophosphatidyl choline claim 4 , and a sphingomyelin.7. The method of any one of to claim 4 , wherein said phospholipid includes one or ...

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Номер записи: 24
04-01-2018 дата публикации

COMPOSITIONS OF JASMONATE COMPOUNDS AND METHODS OF USE

Номер: US20180000958A1
Автор: Fehr Pereira Lopes Jose E.
Принадлежит:

The disclosure describes nanocarried and/or microcarried jasmonate compounds and their pharmaceutical compositions, as well as use thereof for treating or preventing angiogenesis-related or NF-κB-related disorders. Also disclosed are methods of making the nanocarried and/or microcarried compounds and their compositions. 1. A pharmaceutical composition comprising a pharmaceutically acceptable solvent and a plurality of nanocarriers or microcarriers that contain a jasmonate compound , whereinthe nanocarriers or microcarriers are formed of a cyclodextrin or a dendrimer, or are synthetic nanoemulsion particles (LDEs) comprising a cholesteryl ester core surrounded by a phospholipid layer;the nanocarriers have a size ranging from 1 nanometer (nm) to 900 nm; orthe microcarriers have a size ranging from 1 micron to 50 micron; andthe pharmaceutical composition has a concentration of the jasmonate compound ranging from 1 nM to 1 M.2. The pharmaceutical composition of claim 1 , wherein the jasmonate compound is selected from the group consisting of jasmonic acid claim 1 , 7-iso -jasmonic acid claim 1 , 9 claim 1 ,10-dihydrojasmonic acid claim 1 , 9 claim 1 ,10-dihydro-isojasmonic acid claim 1 , 2 claim 1 ,3-didehydrojasmonic acid claim 1 , 3 claim 1 ,4-didehydrojasmonic acid claim 1 , 3 claim 1 ,7-didehydrojasmonic acid claim 1 , 4 claim 1 ,5-didehydrojasmonic acid claim 1 , 4 claim 1 ,5-didehydro-7-isojasmonic acid claim 1 , cucurbic acid claim 1 , 6-epi-cucurbic acid claim 1 , 6-epi-cucurbic acid-lactone claim 1 , 12-hydroxy-jasmonic acid claim 1 , 12-hydroxy-jasmonic acid-lactone claim 1 , 11-hydroxy-jasmonic acid claim 1 , 8-hydroxy-jasmonic acid claim 1 , homo-jasmonic acid claim 1 , dihomo-jasmonic acid claim 1 , 11-hydroxy-dihomo-jasmonic acid claim 1 , 8-hydroxy-dihomo-jasmonic acid claim 1 , tuberonic acid claim 1 , tuberonic acid-O-β-glucopyranoside claim 1 , cucurbic acid-O-β-glucopyranoside claim 1 , 5 claim 1 ,6-didehydro-jasmonic acid claim 1 , 6 claim 1 ,7- ...

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Номер записи: 25
04-01-2018 дата публикации

Poly(Beta-Amino Ester)s With Additives for Drug Delivery

Номер: US20180000968A1
Автор: Borros Gomez Salvador, Oh Sejin
Принадлежит:

Disclosed are nanoparticles comprising an end-modified poly(β-amino ester) and an additive that is a sugar or sugar derivative, such as a sugar, a sugar alcohol or chitosan. The nanoparticles may be used in any field where polymers have been found useful, including in medical fields, particularly in drug delivery. The polymers are useful in delivering a polynucleotide such as DNA, RNA or siRNA, a small molecule or a protein. Also disclosed are compositions comprising said nanoparticles and an active agent, methods for preparing said nanoparticles, said nanoparticles and compositions for use in medicine, and in vitro methods using said nanoparticles and compositions. 1. A nanoparticle comprising an end-modified poly(β-amino ester) and 1 to 35 weight percent , relative to the end-modified poly(β-amino ester) , of a sugar or sugar alcohol.2. A nanoparticle according to claim 1 , comprising 2 to 15 weight percent claim 1 , relative to the end-modified poly(β-amino ester) claim 1 , of the sugar or sugar alcohol.3. A nanoparticle according to wherein the nanoparticle has a coating comprising a sugar or sugar alcohol.4. A nanoparticle according to claim 3 , comprising 1 to 18 weight percent claim 3 , relative to the end-modified poly(β-amino ester) claim 3 , of the sugar or sugar alcohol.5. A nanoparticle according to any one of to claim 3 , wherein the sugar or sugar alcohol is a sugar alcohol having the general formula HOCH(CHOH)CHOH wherein n is from 3 to 46. A nanoparticle according to claim 5 , wherein the sugar alcohol is mannitol.7. A nanoparticle comprising an end-modified poly(β-amino ester) and chitosan claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , at 0.15 to 3.0 weight percent relative to the end-modified poly(β-amino ester).8. A nanoparticle according to any preceding claim claim 5 , wherein each end modification of the end-modified poly(β-amino ester) is independently selected from an oligopeptide and R; wherein Ris selected from the group ...

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Номер записи: 26
02-01-2020 дата публикации

SYNTHETIC NANOPARTICLES FOR DELIVERY OF IMMUNOMODULATORY COMPOUNDS

Номер: US20200000931A1
Автор: DANE Eric, Irvine Darrell J.
Принадлежит:

The present disclosure provides a synthetic nanoparticle comprising a peptide nucleic acid (PNA) oligomer conjugated to a lipid, wherein the PNA oligomer noncovalently complexes with an immunomodulatory compound, thereby forming a nanoparticle. The nanoparticles are useful to elicit immune responses and can be used to treat a broad range of cancers and infectious diseases. 152-. (canceled)54. The composition of claim 53 , wherein the positively charged amino acid is lysine or arginine.55. The composition of claim 53 , wherein Xaaand Xaaare lysine and n is 3 to 6.56. The composition of claim 53 , wherein the PNA oligomer is lysine-(G)-lysine claim 53 , wherein G is guanine.57. The composition of claim 53 , wherein the one or more lipids is a diacyl lipid tail.58. The composition of claim 53 , wherein the CDN is cyclic di-guanine mono phosphate (cdGMP) claim 53 , an agonist of STING (STimulator of Interferon Genes) claim 53 , cyclic di-inosine monophosphate or cyclic d-AMP.59. The composition of claim 53 , further comprising a polymer claim 53 , wherein the polymer is polyethylene glycol claim 53 , or another hydrophilic polymer.60. The composition of claim 53 , wherein the PNA oligomer is noncovalently complexed to the CDN through pi-pi base stacking and hydrogen-bonding interactions.61. The composition of claim 53 , wherein the nanoparticle has a diameter in the range of approximately 10 nm to approximately 100 nm.62. The composition of claim 53 , wherein the nanoparticle comprises a structure selected from the group consisting of a worm-like micelle claim 53 , a disc-like micelle claim 53 , a nanofiber and a spherical micelle.63. A method of modulating an immune response in a subject claim 53 , inducing or enhancing an immune response in a subject with cancer claim 53 , or treating cancer claim 53 , comprising administering to a subject in need thereof the composition of .64. The method of claim 63 , wherein the immune response is an antigen specific immune ...

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Номер записи: 27
03-01-2019 дата публикации

Polynucleotides encoding alpha-galactosidase a for the treatment of fabry disease

Номер: US20190000932A1
Автор: Ellalahewage Sathyajith Kumarasinghe, Iain Mcfadyen, Kerry BENENATO, Lin Tung GUEY, Paolo Martini, Staci SABNIS, Stephen G. Hoge, Vladimir PRESNYAK, Xuling ZHU
Принадлежит: ModernaTx Inc

The invention relates to mRNA therapy for the treatment of Fabry disease. mRNAs for use in the invention, when administered in vivo, encode human the α-galactosidase A (GLA), isoforms thereof, functional fragments thereof, and fusion proteins comprising GLA. mRNAs of the invention are preferably encapsulated in lipid nanoparticles (LNPs) to effect efficient delivery to cells and/or tissues in subjects, when administered thereto. mRNA therapies of the invention increase and/or restore deficient levels of GLA expression and/or activity in subjects. mRNA therapies of the invention further decrease levels of toxic metabolites associated with deficient GLA activity in subjects, namely Gb3 and lyso-Gb3.

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Номер записи: 28
03-01-2019 дата публикации

POLYNUCLEOTIDES ENCODING ALPHA-GALACTOSIDASE A FOR THE TREATMENT OF FABRY DISEASE

Номер: US20190000933A1
Автор: Benenato Kerry, GUEY Lin Tung, HOGE Stephen G., KUMARASINGHE Ellalahewage Sathyajith, Martini Paolo, Mcfadyen Iain, Presnyak Vladimir, SABNIS Staci, ZHU Xuling
Принадлежит:

The invention relates to mRNA therapy for the treatment of Fabry disease. mRNAs for use in the invention, when administered in vivo, encode human the α-galactosidase A (GLA), isoforms thereof, functional fragments thereof, and fusion proteins comprising GLA. mRNAs of the invention are preferably encapsulated in lipid nanoparticles (LNPs) to effect efficient delivery to cells and/or tissues in subjects, when administered thereto. mRNA therapies of the invention increase and/or restore deficient levels of GLA expression and/or activity in subjects. mRNA therapies of the invention further decrease levels of toxic metabolites associated with deficient GLA activity in subjects, namely Gb3 and lyso-Gb3. 1161.-. (canceled)163. The lipid nanoparticle of claim 162 , wherein the ORF is at least 80% identical to the nucleotide sequence of SEQ ID NO: 79.164. The lipid nanoparticle of claim 162 , wherein the ORF is at least 85% identical to the nucleotide sequence of SEQ ID NO: 79.165. The lipid nanoparticle of claim 162 , wherein the ORF is at least 90% identical to the nucleotide sequence of SEQ ID NO: 79.166. The lipid nanoparticle of claim 162 , wherein the ORF is at least 95% identical to the nucleotide sequence of SEQ ID NO: 79.167. The lipid nanoparticle of claim 162 , wherein the ORF is at least 98% identical to the nucleotide sequence of SEQ ID NO: 79.168. The lipid nanoparticle of claim 162 , wherein the ORF is at least 99% identical to the nucleotide sequence of SEQ ID NO: 79.169. The lipid nanoparticle of claim 162 , wherein the ORF is 100% identical to the nucleotide sequence of SEQ ID NO: 79.170. The lipid nanoparticle of claim 163 , wherein the 5′ UTR is at least 80% identical to the nucleotide sequence of SEQ ID NO: 33.171. The lipid nanoparticle of claim 163 , wherein the 3′ UTR comprises the nucleotide sequence of SEQ ID NO: 162.172. The lipid nanoparticle of claim 163 , wherein the 5′ terminal cap is Cap1.173. The lipid nanoparticle of claim 163 , wherein the ...

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Номер записи: 29
03-01-2019 дата публикации

NUCLEIC ACID VACCINES

Номер: US20190000959A1
Автор: BOUCHON Axel, Ciaramella Giuseppe, Huang Eric Yi-Chun
Принадлежит: ModernaTX, Inc.

The invention relates to compositions and methods for the preparation, manufacture and therapeutic use ribonucleic acid vaccines (NAVs) comprising polynucleotide molecules encoding one or more antigens. 1. A method of vaccinating a subject comprising administering to the subject a nucleic acid vaccine comprising one or more RNA polynucleotides comprising an open reading frame encoding an antigenic polypeptide that is derived from an infectious agent , wherein the RNA polynucleotide is formulated within a cationic lipid nanoparticle having a molar ratio of about 20-60% ionizable cationic lipid: about 5-25% non-cationic lipid: about 25-55% sterol; and about 0.5-15% PEG-modified lipid , wherein the nucleic acid vaccine elicits an immune response having a longer lasting antibody titer than an antibody titer elicited by a reference nucleic acid vaccine comprising the one or more RNA polynucleotides not formulated within a cationic lipid nanoparticle having a molar ratio of about 20-60% ionizable cationic lipid: about 5-25% non-cationic lipid: about 25-55% sterol; and about 0.5-15% PEG-modified lipid.2. The method of claim 1 , wherein the method comprises administering to the subject a single dosage of between 0.001 mg/kg and 0.005 mg/kg of the nucleic acid vaccine in an effective amount to vaccinate the subject.3. The method of claim 1 , wherein the open reading frame is codon-optimized.4. The method of claim 1 , wherein the ionizable cationic lipid nanoparticle has a polydispersity value of less than 0.4.5. The method of claim 1 , wherein the polynucleotide has a poly-A tail of 80-250 nucleotides in length.6. The method of claim 1 , wherein a second dose of the nucleic acid vaccine is administered to the subject.7. The method of claim 1 , wherein the RNA polynucleotide includes a chemical modification selected from the group consisting of pseudouridine claim 1 , N1-methylpseudouridine claim 1 , 2-thiouridine claim 1 , 4′-thiouridine claim 1 , 5-methylcytosine claim 1 , ...

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Номер записи: 30
03-01-2019 дата публикации

METHOD FOR TREATING CANCER BY PHOTODYNAMIC THERAPY

Номер: US20190000974A1
Автор: KIM Sehoon, KWON Ick Chan, LEE Sangyoup
Принадлежит:

The present invention discloses a method for treating cancer disease by photodynamic therapy. The photodynamic therapy in the present invention uses a methylene blue nanoparticle as a therapeutic agent. The methylene blue nanoparticle of the present invention for use as a topical cancer targeting phototherapeutic agent is composed of only a material of which the composition is clinically used or derived from human bodies, and thus a nanopreparation in which a barrier to clinical entry is low and the possibility of commercialization is very high, exhibits near-infrared fluorescence along with cancer targeting property, capacity of generating a singlet oxygen and the like. Therefore, the methylene blue nanoparticle in the present invention is able to cure cancer cells by cell apoptosis in irradiation conditions. 1. A method for treating of cancer using methylene blue nanoparticles , the method comprising steps of:a) administrating a therapeutic agent containing the methylene blue nanoparticles into a tissue;b) applying light irradiation to the tissue;c) generating a singlet oxygen from the methylene blue nanoparticles; andd) inducing cell apoptosis and reducing cancer area.2. The method of claim 1 , wherein each of the methylene blue nanoparticles comprises a methylene blue-fatty acid complex and an amphiphilic copolymer of pluronic F-68 claim 1 ,wherein the amphiphilic copolymer comprises a polyoxyethylenepolyoxypropylene-polyoxyethylene block copolymer;the methylene blue-fatty acid complex is enclosed in a micelle formed by the amphiphilic copolymer; andeach of the methylene blue nanoparticles has a diameter of 80 to 100 nm and is self-assembled in an aqueous environment.3. The method of claim 2 , wherein fatty acid of the methylene blue-fatty acid complex is oleic acid or salt thereof.4. The method of claim 2 , wherein the amphiphilic copolymer is directly bonded to the methylene blue-fatty acid complex.5. The method of claim 1 , wherein each of the methylene blue ...

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Номер записи: 31
03-01-2019 дата публикации

Lipids and Lipid Compositions for the Delivery of Active Agents

Номер: US20190002393A1
Автор: BECKWITH Rohan Eric John, Brito Luis, DECHRISTOPHER Brian Addison, Gamber Gabriel Grant, Geall Andrew, ZABAWA Thomas
Принадлежит:

This invention provides for a compound of formula (I): 7. The compound claim 1 , or salt thereof claim 1 , according to claim 1 , wherein the compound is selected from the group consisting of:2,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy)benzyl 4-(dimethylamino)butanoate;((2-(((4-(dimethylamino)butanoyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-(((3-(dimethylamino)propanoyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-(((1-methylpiperidine-4-carbonyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-((((3-(dimethylamino)propoxy)carbonyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-((((3-(diethylamino)propoxy)carbonyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);3-(dimethylamino) propyl 4-methyl-2,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy)benzyl carbonate;4-methyl-2,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy)benzyl 4-(dimethylamino)butanoate;(9Z,9′Z,12Z,12′Z)-((2-(((4-(dimethylamino)butanoyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(butane-4,1-diyl) bis(octadeca-9,12-dienoate);4-(dimethylamino) butyl 4-methyl-2,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy)benzyl carbonate;((2-(((1-ethylpiperidine-4-carbonyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-(((1-isopropylpiperidine-4-carbonyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-((2-(1-methylpiperidin-4-yl)acetoxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-(((4-(pyrrolidin-1-yl)butanoyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);2,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy)benzyl (3-(dimethylamino)propyl) carbonate;(9Z,9′Z,12Z,12′Z)-((2-(((4-(dimethylamino)butanoyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(ethane-2,1-diyl) bis(octadeca-9,12-dienoate);2,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy)benzyl 3-(dimethylamino)propanoate;2,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy) ...

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Номер записи: 32
07-01-2021 дата публикации

NOVEL FORMULATION OF MELOXICAM

Номер: US20210002267A1
Автор: Bosch H. William, Dodd Aaron, Meiser Felix, Norret Marck, Russell Adrian
Принадлежит:

The present invention relates to methods for producing particles of meloxicam using dry milling processes as well as compositions comprising meloxicam, medicaments produced using meloxicam in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of meloxicam administered by way of said medicaments. 1. A method for producing a composition , comprising the steps of:dry milling a solid biologically active material and a millable grinding matrix in a mill comprising a plurality of milling bodies, for a time period sufficient to produce particles of the biologically active material dispersed in an at least partially milled grinding material,wherein the biologically active material is meloxicam.241.-. (canceled) The present invention relates to methods for producing particles of meloxicam using dry milling processes as well as compositions comprising meloxicam, medicaments produced using meloxicam in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of meloxicam administered by way of said medicaments.Poor bioavailability is a significant problem encountered in the development of compositions in the therapeutic, cosmetic, agricultural and food industries, particularly those materials containing a biologically active material that is poorly soluble in water at physiological pH. An active material's bioavailability is the degree to which the active material becomes available to the target tissue in the body or other medium after systemic administration through, for example, oral or intravenous means. Many factors affect bioavailability, including the form of dosage and the solubility and dissolution rate of the active material.In therapeutic applications, poorly and slowly water-soluble materials tend to be eliminated from the gastrointestinal tract before being absorbed into the circulation. In addition, ...

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Номер записи: 33
03-01-2019 дата публикации

POLYNUCLEOTIDES ENCODING ALPHA-GALACTOSIDASE A FOR THE TREATMENT OF FABRY DISEASE

Номер: US20190002890A1
Автор: Benenato Kerry, GUEY Lin Tung, HOGE Stephen G., KUMARASINGHE Ellalahewage Sathyajith, Martini Paolo, Mcfadyen Iain, Presnyak Vladimir, SABNIS Staci, ZHU Xuling
Принадлежит:

The invention relates to mRNA therapy for the treatment of Fabry disease. mRNAs for use in the invention, when administered in vivo, encode human the α-galactosidase A (GLA), isoforms thereof, functional fragments thereof, and fusion proteins comprising GLA. mRNAs of the invention are preferably encapsulated in lipid nanoparticles (LNPs) to effect efficient delivery to cells and/or tissues in subjects, when administered thereto. mRNA therapies of the invention increase and/or restore deficient levels of GLA expression and/or activity in subjects. mRNA therapies of the invention further decrease levels of toxic metabolites associated with deficient GLA activity in subjects, namely Gb3 and lyso-Gb3. 1161. -. (canceled)162. A messenger RNA (mRNA) comprising:(i) a 5′-terminal cap;(ii) a 5′ untranslated region (UTR);(iii) an open reading frame (ORF) encoding a human α-galactosidase A (GLA) polypeptide, wherein the ORF comprises a nucleotide sequence at least 95% identical to the nucleotide sequence of SEQ ID NO: 79;(iv) a 3′ UTR; and(v) a poly-A tail.163. The mRNA of claim 162 , wherein the ORF is at least 98% identical to the nucleotide sequence of SEQ ID NO: 79.164. The mRNA of claim 162 , wherein the ORF is at least 99% identical to the nucleotide sequence of SEQ ID NO: 79.165. The mRNA of claim 162 , wherein the ORF is 100% identical to the nucleotide sequence of SEQ ID NO: 79.166. The mRNA of claim 162 , wherein the 5′ UTR is at least 80% identical to the nucleotide sequence of SEQ ID NO: 33.167. The mRNA of claim 162 , wherein the 3′ UTR comprises the nucleotide sequence of SEQ ID NO: 162.168. The mRNA of claim 162 , wherein the 5′ terminal cap is Cap1.169. The mRNA of claim 162 , wherein the poly-A tail is about 100 residues in length.170. The mRNA of claim 162 , wherein at least 95% of uridines in the ORF are 5-methoxyuridines.171. The mRNA of claim 162 , wherein at least 99% of uridines in the ORF are 5-methoxyuridines.172. The mRNA of claim 162 , wherein 100% ...

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Номер записи: 34
01-01-2015 дата публикации

Thermal treatment of a pilosebaceous unit with metal nanoparticles in surfactant containing solutions

Номер: US20150005691A1
Автор: Alice Ann Chen Kim, Todd James Harris
Принадлежит: Sienna Labs Inc

Treatment of skin tissue with photoactive materials and light, such as nanoparticles and formulations which are useful for cosmetic, diagnostic and therapeutic applications to mammals such as humans. In particular, embodiments of thermal treatment of a pilosebaceous unit with metal nanoparticles in surfactant containing solutions are disclosed.

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Номер записи: 35
20-01-2022 дата публикации

PROCESS FOR PREPARING PHARMACEUTICAL COMPOSITIONS

Номер: US20220016031A1
Автор: Cote Aaron, GUZMAN FRANCISCO J., II Joseph L., Koynov Athanas, Kukura, Lamberto David J., Schenck Luke R.
Принадлежит: Merck Sharp & Dohme Corp.

A process for preparing and isolating pharmaceutical active ingredient particles having a particle size of between about 0.1 and 30 microns, wherein a slurry comprising the active ingredient and one or more pharmaceutically acceptable excipients is fed into a thin film evaporator under suitable conditions for less than 10 minutes sufficient to generate solid matrix particles comprising active ingredient and one or more excipients, wherein the particles have less than 5% residual solvent. 1. A process for preparing and isolating pharmaceutical active ingredient particles having a particle size of between about 0.1 and 30 microns , wherein a dried solids-containing slurry comprising: (a) a pharmaceutical active ingredient , and one or more of: (b) a steric stability polymer , (c) an electrostatic stability surfactant , and (d) a redispersibility excipient is fed into a thin film evaporator comprising shear rates exceeding 4 ,000 s , temperature between about 50° C. and 100° C. , vacuum from 10 mbar to 75 mbar pressure , and Reynolds Numbers above 200 ,000 , to provide turbulent mixing for less than 10 minutes and sufficient to generate solid matrix particles comprising the pharmaceutical active ingredient and the one or more excipients , wherein the particles have less than 5% residual solvent.2. (canceled)3. The process of wherein the dried solids-containing slurry is fed into the thin film evaporator under shear claim 1 , temperature and pressure conditions to provide turbulent mixing for less than 5 minutes.4. The process of wherein the particles have a particle size of between 0.1 and 5 microns.5. The process of wherein the particles have a particle size of between 0.1 and 0.25 microns.6. The process of wherein the particles are crystalline.7. The process of wherein the particles are amorphous.8. The process of wherein the steric stability polymer is a cellulosic polymer claim 2 , a methacrylate claim 2 , a vinyl polymer claim 2 , a copolymer claim 2 , or ...

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Номер записи: 36
14-01-2016 дата публикации

PEPTIDE-BASED HYDROGEL PARTICLES AND USES THEREOF

Номер: US20160008291A1
Автор: ADLER-ABRAMOVICH Lihi, Buzhansky Ludmila, Gazit Ehud, ISCHAKOV Rafael
Принадлежит:

Compositions comprising self-assembled hydrogel particles formed of short peptides which comprise one or more aromatic amino acid residue(s) in an inverted emulsion are disclosed. Such hydrogel particles which encapsulate an active agent and uses thereof in therapeutic and diagnostic applications are also disclosed. 1. A composition comprising a plurality of physically discrete hydrogel particles , each hydrogel particle comprising a three-dimensional network made of a plurality of self-assembled peptides and an aqueous medium , wherein each peptide in the plurality of peptides comprises 2-6 amino acid residues , at least one of the amino acids being an aromatic amino acid.2. (canceled)3. The composition of claim 1 , wherein an average diameter of each of the hydrogel particles ranges from 10 nm to 1000 nm claim 1 , or from 10 nm to 500 nm.4. The composition of claim 1 , wherein the plurality of peptides comprises a plurality of dipeptides.5. (canceled)6. The composition of claim 4 , wherein each peptide in the plurality of dipeptides is an aromatic-homodipeptide.7. (canceled)8. The composition of claim 6 , wherein the plurality of aromatic dipeptides comprises a plurality of diphenylalanine peptides.9. The composition of claim 1 , wherein at least one of the peptides comprises a RGD sequence.10. The composition of claim 1 , wherein each peptide in the plurality of peptides comprises an RGD sequence.11. The composition of claim 1 , wherein at least one of the peptides comprises an end-capped moiety.12. The composition of claim 11 , wherein each of the peptides comprises an end-capped moiety.13. The composition of claim 12 , wherein the end-capping moiety is an aromatic end-capping moiety.1415-. (canceled)16. The composition of claim 1 , wherein the plurality of peptides comprises a plurality of diphenylalanine peptides having an end-capping moiety substituting the N-terminus thereof.17. The composition of claim 16 , wherein each of the diphenylalanine peptide is an ...

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Номер записи: 37
14-01-2016 дата публикации

Method for the production of sub-micrometric particles and their theranostic use in oncology with a specific apparatus

Номер: US20160008467A1
Автор: Filippo GHERLINZONI, Michele GOTTARDI, Paolo Matteazzi
Принадлежит: MBN Nanomaterialia SpA

The invention relates to a method for producing sub-micrometric particles, which comprises: mechanochemical treatment of homogeneous or heterogeneous magnetic materials until a mass which consists mostly of magnetic nanocrystal aggregates is obtained; selection of aggregates so that the nanocrystals have a Curie temperature within a predefined variation range; functionalization of the aggregates in order to obtain coating thereof with molecules of one or more of the following types of substances: substances for which the tumour cells have a particular metabolic avidity; substances having a biochemical affinity with the tumour cells; substances having an affinity with the acid microenvironment which surrounds the neoplastic cells. In addition to the method the following are claimed: the particles thus produced; their theranostic use which allows the in vivo execution, without interruption, of the diagnosis or monitoring step and the therapy step by means of magnetic hyperthermia of malignant neoplasms, including those localized in the so-called “sanctuary sites” such as the central nervous system and the testicle; an apparatus designed for this use.

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Номер записи: 38
11-01-2018 дата публикации

Cleavable Lipids

Номер: US20180008543A1
Автор: DeRosa Frank, GUILD Braydon Charles, Heartlein Michael, Zhang Jerry Chi
Принадлежит:

Disclosed herein are novel compounds, pharmaceutical compositions comprising such compounds and related methods of their use. The compounds described herein are useful, e.g., as liposomal delivery vehicles to facilitate the delivery of encapsulated polynucleotides to target cells and subsequent iransfection of said target cells, and in certain embodiments are characterized as having one or more properties that afford such compounds advantages relative to other similarly classified lipids. 2. (canceled)3. The nanoparticle of claim 1 , wherein Ris imidazole.4. The nanoparticle of claim 1 , wherein{'sub': '1', 'Ris imidazole;'}andn is 1.5. The nanoparticle of claim 1 , wherein Ris guanidinium.6. The nanoparticle-of claim 1 , wherein{'sub': '1', 'Ris guanidinium;'}andn is 1.723.-. (canceled)2629.-. (canceled)30. The nanoparticle of claim 1 , further comprising one or more compounds selected from the group consisting of a cationic lipid claim 1 , a PEG-modified lipid claim 1 , a non-cationic lipid and a helper lipid.31. (canceled)32. The nanoparticle of claim 1 , wherein one or more of the polynucleotides comprises a chemical modification.33. The nanoparticle of claim 1 , wherein the one or more polynucleotides is selected from the group consisting of an antisense oligonucleotide claim 1 , siRNA claim 1 , miRNA claim 1 , snRNA claim 1 , snoRNA and combinations thereof.34. (canceled)35. The nanoparticle of claim 1 , wherein the one or more polynucleotides comprise DNA.36. The nanoparticle of claim 1 , wherein the one or more polynucleotides comprise RNA.37. (canceled)38. The nanoparticle of claim 36 , wherein the RNA encodes an enzyme.39. The nanoparticle of claim 38 , wherein the enzyme is selected from the group consisting of agalsidase alfa claim 38 , alpha-L-iduronidase claim 38 , iduronate-2-sulfatase claim 38 , N-acetylglucosamine-1-phosphate transferase claim 38 , N-acetylglucosaminidase claim 38 , alpha-glucosaminide acetyltransferase claim 38 , N- ...

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Номер записи: 39
11-01-2018 дата публикации

SUBSTANCE-CONTAINING VESICLE, AND PRODUCTION METHOD THEREFOR

Номер: US20180008549A1
Автор: Anraku Yasutaka, Goto Akinori, Kataoka Kazunori, Kishimura Akihiro
Принадлежит:

Provided is a monodisperse agglomerate of a substance-containing vesicle filled with a substance at a concentration higher than conventionally possible. A mixed solution, in which a target substance is included in an aqueous medium, is mixed with a monodisperse agglomerate of a crosslinked vesicle comprising a prescribed polymer which includes a first polymer, i.e. a block copolymer having uncharged hydrophilic segments and first charged segments, and a second polymer having second charged segments carrying a charge opposite to that of the first charged segments, and in which the first polymer and/or the second polymer are/is crosslinked. As a result, the crosslinked vesicle is made to contain the target substance. 1. An adsorbent-encapsulating vesicle comprising:a vesicle composed of a membrane comprising a first polymer, which is block copolymer having an uncharged hydrophilic segment and a first charged segment, and a second polymer, which has a second charged segment having a charge opposite to the charge of the first charged segment; andan adsorbent particle encapsulated in the vesicle,wherein at least either the first polymer or the second polymer is adsorbed by the adsorbent particle.2. The adsorbent-encapsulating vesicle according to claim 1 , wherein the first and/or second polymer(s) is(are) crosslinked.3. The adsorbent-encapsulating vesicle according to claim 1 , wherein the adsorbent particle is a silica particle.4. The adsorbent-encapsulating vesicle according to claim 1 , wherein the adsorbent particle has an average particle size of between 40 nm and 10 μm.5. The adsorbent-encapsulating vesicle according to claim 1 , wherein the adsorbent particle has been surface-treated.6. The adsorbent-encapsulating vesicle according to claim 1 , wherein a low-molecular compound is adsorbed by the adsorbent particle.7. A method of producing the adsorbent-encapsulating vesicle of claim 1 , said method comprising the steps of:(a) mixing one of the first and second ...

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Номер записи: 40
11-01-2018 дата публикации

SUBSTANCE-CONTAINING VESICLE, AND PRODUCTION METHOD THEREFOR

Номер: US20180008550A1
Автор: Anraku Yasutaka, Goto Akinori, Kataoka Kazunori, Kishimura Akihiro
Принадлежит:

Provided is a monodisperse agglomerate of a substance-containing vesicle filled with a substance at a concentration higher than conventionally possible. A mixed solution, in which a target substance is included in an aqueous medium, is mixed with a monodisperse agglomerate of a crosslinked vesicle comprising a prescribed polymer which includes a first polymer, i.e. a block copolymer having uncharged hydrophilic segments and first charged segments, and a second polymer having second charged segments carrying a charge opposite to that of the first charged segments, and in which the first polymer and/or the second polymer are/is crosslinked. As a result, the crosslinked vesicle is made to contain the target substance. 1. A method of producing a target substance-encapsulating vesicle , comprising the steps of:(a) obtaining an enzyme-encapsulating vesicle comprising a membrane containing a first polymer, which is a block copolymer having an uncharged hydrophilic segment and a first charged segment, and a second polymer, which has a second charged segment having a charge opposite to the charge of the first charged segment, and an enzyme encapsulated in the vesicle; and(b) mixing the enzyme-encapsulating vesicle with a precursor of a target substance in an aqueous medium under conditions which provide a lower water solubility for the target substance than for the precursor such that when the enzyme converts the precursor into the target substance, the target substance precipitates and is encapsulated in the enzyme-encapsulating vesicle, thereby forming the target substance-encapsulating vesicle.2. The method according to claim 1 , wherein step (b) is carried out by mixing the enzyme-encapsulating vesicle with an aqueous solution of the precursor.3. The method according to claim 2 , further comprising crosslinking the first and/or the second polymer(s) of the enzyme-encapsulating vesicle before step (b).4. A substance-encapsulating vesicle produced by the method according ...

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Номер записи: 41
14-01-2021 дата публикации

A PHARMACEUTICAL FORMULATION FOR INTRADUODENAL ADMINISTRATION COMPRISING MELEVODOPA AND CARBIDOPA

Номер: US20210007984A1
Автор: CAIVANO Grazia, FONT Isabel Sole, INACIO Ricardo, MEHTA Bhanvi, MUEHLHOELZL-ODOERFER Kathrin, SAUNDERS Mark
Принадлежит: CHIESI FARMACEUTICI S.p.A.

A pharmaceutical formulation for intraduodenal administration comprising melevodopa and carbidopa as active ingredients and one or more excipients. Once dispersed in an aqueous medium, melevodopa is completely dissolved, and carbidopa is present as nanoparticles. 1. An aqueous pharmaceutical formulation for intraduodenal administration , comprising carbidopa and melevodopa as active ingredients in a ratio of 1:5 by weight , and one or more excipients , wherein said melevodopa is completely dissolved , and said carbidopa is present as nanoparticles having a volume diameter of 100 to 1000 nm.2. The formulation according to claim 1 , wherein said nanoparticles have a volume diameter of 200 to 900 nm.3. The formulation according to claim 1 , wherein said one or more excipients comprise a component selected from the group consisting of a stabilization agent claim 1 , a wetting agent claim 1 , and mixtures thereof.4. The formulation according to claim 3 , wherein said stabilization agent is selected from the group consisting of hydroxypropyl methylcellulose claim 3 , polyvinylpyrrolidone claim 3 , a vinylpyrrolidone-vinyl acetate copolymer claim 3 , a methacrylic copolymer claim 3 , carboxymethylcellulose claim 3 , a carbomer claim 3 , a plant gum claim 3 , and a plant colloid claim 3 , and mixtures thereof.5. The formulation according to claim 3 , wherein said wetting agent is selected from the group consisting of a pharmaceutically acceptable salt of a fatty acid claim 3 , a poloxamer claim 3 , a polysorbate claim 3 , sorbitan monolaurate claim 3 , and mixtures thereof.6. The formulation according to claim 1 , which further comprises one or more additional excipients selected from the group consisting of an antioxidant claim 1 , a preserving agent claim 1 , a pH regulating agent claim 1 , and mixtures thereof.7. The formulation according to claim 1 , wherein said carbidopa nanoparticles are prepared by a process comprising:i) suspending carbidopa in the presence of one ...

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Номер записи: 42
10-01-2019 дата публикации

A method for the preparation of a delivery drug delivery system and a composition therefor

Номер: US20190008790A1
Автор: Dong Wang
Принадлежит: Element Six UK Ltd

A method for the preparation of a delivery drug delivery system, the drug having one or more active pharmaceutical ingredients having solubility in water of less than 1 g in 30 ml of water and nano-diamond, comprises the steps of dissolving the active pharmaceutical ingredient(s) into a polar non-aqueous solvent to form a first mixture, dissolving a surfactant in deionized water to form a surfactant solution, adding a plurality of nano-diamond particles to the surfactant solution to disperse the nano-diamond particles in the surfactant solution thereby forming a nano-diamond dispersion, adding the first mixture to the nano-diamond dispersion whilst agitating the dispersion to form a second mixture; and drying the second mixture to produce a dry powder for use as a drug delivery system.

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Номер записи: 43
10-01-2019 дата публикации

NUCLEIC ACID VACCINES

Номер: US20190008948A1
Автор: BOUCHON Axel, Ciaramella Giuseppe, Huang Eric Yi-Chun
Принадлежит: ModernaTX, Inc.

The invention relates to compositions and methods for the preparation, manufacture and therapeutic use ribonucleic acid vaccines (NAVs) comprising polynucleotide molecules encoding one or more antigens. 1. A nucleic acid vaccine , comprising:one or more RNA polynucleotides having an open reading frame encoding an antigenic polypeptide, formulated in a cationic lipid nanoparticle having a molar ratio of about 20-60% cationic lipid: about 5-25% non-cationic lipid: about 25-55% sterol; and about 0.5-15% PEG-modified lipid.2. The vaccine of claim 1 , wherein the cationic lipid nanoparticle comprises a cationic lipid claim 1 , a PEG-modified lipid claim 1 , a sterol and a non-cationic lipid.3. (canceled)4. The vaccine of claim 2 , wherein the cationic lipid nanoparticle has a molar ratio of about 20-60% cationic lipid: about 5-25% non-cationic lipid: about 25-55% sterol; and about 0.5-15% PEG-modified lipid.58-. (canceled)9. The vaccine of claim 1 , wherein the antigenic polypeptide is derived from an infectious agent.10. (canceled)11. The vaccine of claim 1 , wherein the one or more RNA polynucleotides encode a further antigenic polypeptide.12. The vaccine of claim 1 , wherein the one or more RNA polynucleotides comprise at least one chemical modification.13. The vaccine of claim 1 , wherein the antigenic polypeptide is selected from those proteins listed in Tables 6-14 claim 1 , Tables 29-30 claim 1 , or antigenic fragments thereof.14. The vaccine of claim 1 , wherein the open reading frame of the one or more RNA polynucleotides encodes an antigenic polypeptide selected from Tables 6-11 claim 1 , Tables 22-23 claim 1 , or antigenic fragments thereof.1528-. (canceled)29. The vaccine of claim 1 , wherein the nucleic acid vaccine is multivalent.3036-. (canceled)37. A nucleic acid vaccine claim 1 , comprising:one or more RNA polynucleotides having an open reading frame encoding a first antigenic polypeptide, formulated within a nanoparticle, wherein the nanoparticle has a ...

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Номер записи: 44
09-01-2020 дата публикации

FORMULATION AND METHOD FOR INCREASING ORAL BIOAVAILABILITY OF DRUGS

Номер: US20200009067A1
Автор: CHERNIAKOV Irina, Domb Abraham J., ELGART Anna, HOffman Amnon
Принадлежит: YISSUM Research Development Company of the Hebrew University of Jerusalem LTD.

Provided is a formulation and method for increasing bioavailability of an orally administered drug. 131.-. (canceled)32. A method for increasing the bioavailability of at least one orally administered drug in a subject in need of said drug , the method comprising orally administering to said subject:(1) said drug, and a dispersible concentrate comprising:', '(i) at least one surfactant;', '(ii) at least one solid component at room temperature, the at least one solid component having a melting temperature above 25° C. and is selected from the group consisting of fatty acids, fatty acid esters, fatty amines, fatty amides and fatty alcohols; and', '(iii) an amphiphilic solvent,', 'wherein upon contact of said concentrate with the gastrointestinal (GI) tract fluids, the concentrate transforms into a dispersion of nanoparticles having a size of less than about 500 nm, the nanoparticles comprising the at least one surfactant, the at least one solid component at room temperature, and the amphiphilic solvent; such that the bioavailability of said at least one orally administered drug is increased, as determined by measuring the total systemic drug concentrations over time after administration of said composition as compared to after administration of the drug alone,', 'and wherein the composition does not comprise curcumin., '(2) a composition, comprising33. The method according to claim 32 , wherein said composition being administered substantially simultaneously with the drug.34. The method according to claim 32 , wherein said composition and drug are sequentially administered.35. The method according to claim 32 , wherein the drug is administered in at least one dose within 24 hrs after administration of the composition.3638.-. (canceled)39. The method according to claim 32 , for treatment of at least one disease or disorder.4048.-. (canceled)49. The method according to claim 32 , wherein said at least one drug is a cannabinoid claim 32 , a derivative or a synthetic ...

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Номер записи: 45
09-01-2020 дата публикации

MEROPENEM DERIVATIVES AND USES THEREOF

Номер: US20200010470A1
Автор: Bourassa James, Chen Hongming, Cu Yen, Enlow Elizabeth M., KIM Jinsoo, Nowak Pawel Wojciech, Ong Winston Zapanta, Popov Alexey
Принадлежит:

The present invention provides novel derivative of β-lactam antibiotics, such as meropenem. The inventive compounds include compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. Also provided are particles (e.g., nanoparticles) and pharmaceutical compositions thereof that are mucus penetrating. The inventive particles and pharmaceutical compositions may be useful in delivering an inventive compound to the respiratory tract of a subject. The invention further provides methods of using and kits including the inventive compounds, particles thereof, and/or pharmaceutical compositions thereof for treating and/or preventing a pulmonary disease (e.g., a respiratory tract infection). 127-. (canceled)31. The compound of claim 30 , wherein Ris unsubstituted aliphatic claim 30 , unsubstituted carbocyclyl claim 30 , substituted aryl claim 30 , or unsubstituted aryl.32. The compound of claim 30 , wherein Ris unsubstituted aliphatic claim 30 , unsubstituted carbocyclyl claim 30 , aryl substituted with halogen claim 30 , or unsubstituted aryl.35. The compound of claim 34 , wherein Ris unsubstituted aliphatic claim 34 , unsubstituted carbocyclyl claim 34 , substituted aryl claim 34 , or unsubstituted aryl.36. The compound of claim 34 , wherein Ris unsubstituted aliphatic claim 34 , unsubstituted carbocyclyl claim 34 , aryl substituted with halogen claim 34 , or unsubstituted aryl.40. A composition claim 28 , comprising the compound of .41. A composition claim 29 , comprising the compound of .42. A composition claim 30 , comprising the compound of .43. A composition claim 31 , comprising the compound of .44. A composition claim 32 , comprising the compound of .45. A composition claim 33 , comprising the compound of .46. A composition claim 34 , comprising the compound of .47. A composition claim 35 , comprising the compound of . The present ...

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Номер записи: 46
03-02-2022 дата публикации

NANOPARTICLE FORMULATIONS AND METHODS OF THEIR USE

Номер: US20220031630A1
Автор: ADAY Sezin, Joshi Nitin, Karp Jeffrey M., Langer Robert S., Li Wen, MANNIX Rebekah, Qiu Jianhua
Принадлежит:

Disclosed are pharmaceutical compositions formulated for delivery to the brain of a subject. The compositions include a plurality of nanoparticles (NPs) containing a brain therapeutic agent, poly(lactic-co-glycolic acid) (PLGA), and a pharmaceutically acceptable excipient selected from the group consisting of a surfactant, peptide, and combinations thereof. Also disclosed are methods of their use. 1. A pharmaceutical composition formulated for delivery to the brain of a subject , the composition comprising a plurality of nanoparticles (NPs) comprising a brain therapeutic agent , poly(lactic-co-glycolic acid) (PLGA) , and a pharmaceutically acceptable excipient selected from the group consisting of a surfactant , peptide , and combinations thereof.2. The pharmaceutical composition of claim 1 , wherein the brain therapeutic agent treats a functional disorder.3. The pharmaceutical composition of claim 1 , wherein the brain therapeutic agent treats a physical disorder.4. The pharmaceutical composition of claim 3 , wherein the physical disorder is a traumatic brain injury.5. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition comprises a surfactant.6. The pharmaceutical composition of claim 5 , wherein the surfactant is a polysorbate claim 5 , polyethylene glycol claim 5 , or poloxamer.7. The pharmaceutical composition of claim 6 , wherein the surfactant is a polysorbate.8. The pharmaceutical composition of claim 7 , wherein the polysorbate is polysorbate 80.9. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition comprises 0.001-0.2% (w/v) of the surfactant.10. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition comprises 0.1-0.2% (w/v) of the surfactant.12. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition comprises a peptide.1311. The pharmaceutical composition of claim claim 1 , wherein the peptide is glutathione claim 1 , transferrin claim 1 , ...

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Номер записи: 47
03-02-2022 дата публикации

HIGH-PURITY PEG LIPIDS AND USES THEREOF

Номер: US20220031631A1
Автор: Almarsson Örn, CHEUNG Eugene, Lim Jin, Milton Jaclyn
Принадлежит: ModernaTX, Inc.

The present disclosure is based, at least in part, on the discovery that high-purity PEG lipids exhibit superior physical and biological properties, particularly when used in lipid nanoparticle (LNP) formulations. Therefore, the present disclosure provides PEG lipids at a recommended purity, e.g., for use in formulations, such as LNP formulations. The present disclosure also provides LNPs comprising the high-purity PEG lipids, and methods for delivering therapeutic agents to a subject using the same. 2. The plurality of compounds of claim 1 , wherein r is independently an integer from 40-50 claim 1 , inclusive.3. The plurality of compounds of claim 1 , wherein r is independently an integer from 42-48 claim 1 , inclusive.4. The plurality of compounds of claim 1 , wherein r is independently an integer from 44-46 claim 1 , inclusive.5. The plurality of compounds of claim 1 , wherein r is 45.6. The plurality of compounds of any one of - claim 1 , wherein the purity is greater than 87%.7. The plurality of compounds of any one of - claim 1 , wherein the purity is greater than 90%.8. The plurality of compounds of any one of - claim 1 , wherein the purity is greater than 95%.9. The plurality of compounds of any one of - claim 1 , wherein the purity is greater than 98%.10. The plurality of compounds of any one of - claim 1 , wherein the purity is greater than 99%.11. The plurality of compounds of any one of - claim 1 , wherein the purity is from 90-100% claim 1 , inclusive.12. The plurality of compounds of any one of - claim 1 , wherein the purity is from 90-95% claim 1 , inclusive.13. The plurality of compounds of any one of - claim 1 , wherein the purity is from 95-100% claim 1 , inclusive.15. The plurality of compounds of claim 15 , comprising less than 10% of total impurities.16. The plurality of compounds of claim 15 , comprising less than 5% of total impurities.17. The plurality of compounds of claim 15 , comprising less than 2% of total impurities.18. The plurality of ...

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Номер записи: 48
03-02-2022 дата публикации

Anti-proprotein convertase subtilisin kexin type 9 (anti-pcsk9) nano-formulation of compounds and methods of using the same

Номер: US20220031665A1
Автор: Harold V. Meyers, Nabil A. Elshourbagy, Shaker A. Mousa, Sherin Salaheldin Abdel-Meguid
Принадлежит: Shifa Biomedical Corp

Disclosed are Nanoformulated compounds that modulate the physiological action of the proprotein convertase subtilisin kexin type 9 (PCSK9), as well as therapeutic methods for use of such compounds to reduce LDL- and related cholesterol levels and/or for the treatment and/or prevention of cardiovascular disease (CVD), including treatment of hypercholesterolemia.

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Номер записи: 49
19-01-2017 дата публикации

High delivery rates for lipid based drug formulations, and methods of treatment thereof

Номер: US20170014342A1
Автор: Brian S. Miller, Lawrence T. Boni, Vladimir Malinin, Xingong Li, Zhili Li
Принадлежит: Insmed Inc

Provided is a method of preparing lipid based drug formulations with low lipid/drug ratios using coacervation techniques. Also provided are methods of delivering such lipid based drug formulations at high delivery rates, and methods of treating patients with pulmonary diseases comprising administering such lipid based drug formulations.

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Номер записи: 50
03-02-2022 дата публикации

POLYNUCLEOTIDE AGENTS TARGETING PROGRAMMED CELL DEATH 1 LIGAND 1 (PD-L1) AND METHODS OF USE THEREOF

Номер: US20220033825A1
Автор: Hinkle Gregory
Принадлежит:

The invention relates to polynucleotide agents targeting programmed cell death 1 ligand 1 (PD-L1) gene, and methods of using such polynucleotide agents to inhibit expression of PD-L1 and to treat subjects having a PD-L1-associated disorder. 1. A single-stranded antisense polynucleotide agent for inhibiting expression of a Programmed cell death 1 ligand 1 (PD-L1) gene , wherein the agent comprises 4 to 50 contiguous nucleotides , wherein at least one of the contiguous nucleotides is a modified nucleotide , and wherein the nucleotide sequence of the agent is 80% complementary over its entire length to the equivalent region of the nucleotide sequence of any one of SEQ ID NOs:1-5.2. The agent of claim 1 , wherein the agent comprises 4 to 50 contiguous nucleotides claim 1 , wherein at least one of the contiguous nucleotides is a modified nucleotide claim 1 , and wherein the nucleotide sequence of the agent is 80% complementary over its entire length to the equivalent region of the nucleotide sequence of any one of residues 10-29; 44-75; 44-141; 78-141; 187-305; 309-349; 351-467; 309-467; 472-503; 505-570; 472-570; 571-590; 505-590; 606-647; 681-755; 769-788; 793-811; 815-834; 859-911; 1000-1019; 1044-1076; 1100-1152; 1177-1196; 1211-1241; 1242-1261; 1211-1261; 1277-1307; 1309-1328; 1277-1328; 1342-1373; 1374-1407; 1418-1450; 1462-1493; 1497-1582; 1650-1713; 1650-1756; 1716-1756; 1781-1879; 1915-1945; 1958-1977; 1990-2009; 2112-2131; 2167-2186; 2211-2230; 2288-2307; 2332-2351; 2364-2383; 2552-2571; 2575-2594; 2552-2594; 2652-2671; 2739-2801; 2826-2878; 2904-2933; 2970-2989; 3013-3032; 3035-3054; 3113-3142; 3158-3199 of SEQ ID NO:136.-. (canceled)7. The agent of claim 1 , wherein substantially all of the nucleotides are modified nucleotides.8. The agent of claim 1 , wherein all of the nucleotides are modified nucleotides.9. The agent of claim 1 , which is 10 to 40 nucleotides in length; 10 to 30 nucleotides in length; 18 to 30 nucleotides in length; 10 to 24 nucleotides in ...

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Номер записи: 51
18-01-2018 дата публикации

CFTR MRNA COMPOSITIONS AND RELATED METHODS AND USES

Номер: US20180015116A1
Автор: DeRosa Frank, GUILD Braydon Charles, Heartlein Michael, Plank Christian, Rudolph Carsten, Smith Lianne
Принадлежит:

Materials, formulations, production methods, and methods for delivery of CFTR mRNA for induction of CFTR expression, including in the mammalian lung are provided. The present invention is particularly useful for treating cystic fibrosis. 147-. (canceled)48. A method of producing cystic fibrosis transmembrane conductance regulator (CFTR) protein in a lung of a mammal , the method comprising:administering to the lung of the mammal by aerosolization a composition comprising an mRNA-loaded nanoparticle, wherein the nanoparticle is a liposome, wherein the mRNA is an in vitro transcribed mRNA and has a coding sequence at least 80% identical to SEQ ID NO: 3, wherein the mRNA encodes a human CFTR protein comprising the amino acid sequence of SEQ ID NO: 1, and wherein the mRNA is unmodified.49. The method of claim 48 , wherein the mRNA has the coding sequence at least 90% identical to SEQ ID NO: 3.50. The method of claim 48 , wherein the mRNA has the coding sequence 100% identical to SEQ ID NO: 3.51. The method of claim 48 , wherein the mRNA comprises a 5′ untranslated region (UTR) and/or a 3′ UTR.52. The method of claim 51 , wherein the 5′-UTR comprises SEQ ID NO: 4 and/or the 3′-UTR comprises SEQ ID NO: 5.53. The method of claim 51 , wherein the mRNA further comprises a poly-A tail.54. The method of claim 53 , wherein the poly-A tail is of at least 70 claim 53 , 100 claim 53 , 120 claim 53 , 150 claim 53 , 200 claim 53 , or 250 residues in length.55. The method of claim 51 , wherein the mRNA further comprises a 5′ cap.56. The method of claim 48 , wherein the aerosolization is nebulization.57. The method of claim 48 , wherein the human CFTR protein is expressed in the epithelial cells of the lung.58. The method of claim 48 , wherein the composition further comprises a pharmaceutically acceptable carrier.59. The method of claim 48 , wherein the liposome comprises one or more PEGylated lipids.60. The method of claim 48 , wherein the liposome further comprises one or more ...

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Номер записи: 52
15-01-2015 дата публикации

METHOD AND SYSTEM FOR SYNTHESIZING NANOCARRIER BASED LONG ACTING DRUG DELIVERY SYSTEM FOR MORPHINE

Номер: US20150017228A1
Автор: Hamidi Mehrdad
Принадлежит: KIMIA ZIST PARSIAN CO

The embodiments herein provide a nano-carrier system for delivering a long-acting injectable drug of morphine and a method of synthesising the same. The morphine entrapped nanoparticles are prepared using a lipid/phospholipid core which is coated by a polymer. The lipid and phospholipid are dissolved in organic solvent. This solution is transferred into an aqueous phase consisting of distilled water or a buffer. A solution of polymer is added drop wise. The drug entrapped nanoparticle formation is achieved by diffusion of the organic solvent within the aqueous solvent to obtain the nanoparticles. The drug gets entrapped within the nanoparticles via the anti-solvency effect of the aqueous matrix. The resulting drug nanocarriers are capable of releasing the drug in a slow rate upon injection. The synthesized drug carrying nanoparticles are cryopreserved stored for future administration. For better storage, the nanodispersion is dried to form a powder. 1. A method for synthesizing slow and controlled release of a morphine entrapped in nanoparticle or nanocarrier , the method comprising steps of:dissolving a morphine in an organic solvent to get an organic solution, wherein the morphine is dissolved at a concentration of 0.1 to 10 mg/ml in the organic solvent, and wherein a concentration of the organic solvent is 0.1 to 5 mg/ml;adding a phospholipid to the organic solution to form a bilayer around the morphine;adding a lipid to the organic solution to obtain an organic solution mixture, wherein the organic solution mixture comprises organic solvent with the morphine, phospholipid and lipid;adding the organic solution mixture by dropwise to an aqueous solution to form a lipid core, and wherein the aqueous solution is a water or a buffer, and wherein pH of the aqueous solution is in a range of 3-11, and wherein a volume ratio of the organic solution mixture to the aqueous solution is within 0.05 to 3; andadding a buffered solution of a polymer to the aqueous solution with ...

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Номер записи: 53
18-01-2018 дата публикации

SYNTHETIC NANOPARTICLES FOR DELIVERY OF IMMUNOMODULATORY COMPOUNDS

Номер: US20180015174A1
Автор: DANE Eric, Irvine Darrell J.
Принадлежит:

The present disclosure provides a synthetic nanoparticle comprising a peptide nucleic acid (PNA) oligomer conjugated to a lipid, wherein the PNA oligomer noncovalently complexes with an immunomodulatory compound, thereby forming a nanoparticle. The nanoparticles are useful to elicit immune responses and can be used to treat a broad range of cancers and infectious diseases. 1. A synthetic nanoparticle comprising a PNA-amphiphile conjugate and an immunomodulatory compound , wherein the PNA-amphiphile conjugate comprises (i) a peptide nucleic acid (PNA) oligomer comprising at least one guanine nucleoside , or an analog thereof , (ii) one or more lipids , and optionally , (iii) a polymer , wherein the immunomodulatory compound is a cyclic dinucleotide (CDN) , and wherein the CDN is noncovalently complexed with the PNA oligomer , thereby forming a synthetic nanoparticle.2. The synthetic nanoparticle of claim 1 , wherein the PNA oligomer comprises 3 guanine nucleosides claim 1 , or analogs thereof claim 1 , or at least one positively charged amino acid.3. (canceled)4. The synthetic nanoparticle of claim 1 , wherein the positively charged amino acid is lysine or arginine.5. The synthetic nanoparticle of claim 1 , wherein the PNA oligomer is represented from N- to C-terminus by the formula: Xaa-(G)-Xaa claim 1 , wherein Xaais selected from the group consisting of lysine and arginine claim 1 , wherein G is guanine and n is 1 to 12 claim 1 , and wherein Xaais selected from the group consisting of lysine and arginine.6. The synthetic nanoparticle of claim 5 , wherein Xaaand Xaaare lysine and n is 3 to 6.7. The synthetic nanoparticle of claim 1 , wherein the PNA oligomer is lysine-(G)-lysine claim 1 , wherein G is guanine.8. The synthetic nanoparticle of claim 1 , wherein the one or more lipids is a diacyl lipid tail.9. The synthetic nanoparticle of claim 1 , wherein the CDN is cyclic di-guanine mono phosphate (cdGMP) claim 1 , an agonist of STING (STimulator of Interferon ...

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Номер записи: 54
17-01-2019 дата публикации

HEPATOPROTECTIVE PARTICLES AND SYSTEMS AND METHODS OF USE THEREOF

Номер: US20190015335A1
Автор: Durymanov Mikhail, Permyakova Anastasia, Reineke Joshua
Принадлежит:

Compositions for targeted delivery of a protective agent to the liver, and systems and methods for administering the compositions are described. When administered prior to or in combination with one or more chemotherapeutic agents, the compositions containing the protective agent protect the liver without adversely affecting the efficacy of the chemotherapeutic agent(s). Additionally, the use of these compositions enables the administration of higher doses of the chemotherapeutic agent(s). The compositions contain particles, comprising nanoparticles, microparticles, or combinations thereof, which contain a hepatoprotective agent. The systems contain a first formulation comprising particles that contain a protective agent to the liver and a second formulation comprising a chemotherapeutic agent. The particles containing the hapatoprotective agent are short circulating particles. 1. A system for chemotherapy comprising:a first formulation, comprising short-circulating particles containing a hepatoprotectant, wherein the particles are nanoparticles, microparticles, or combinations thereof, anda second formulation comprising a chemotherapeutic agent.2. The system of claim 1 , wherein the particles comprise a metal organic framework (MOF).3. The system of claim 2 , wherein the MOF comprises a metal ion selected from the group consisting of Fe claim 2 , Fe claim 2 , Zn claim 2 , Na claim 2 , K claim 2 , Mg claim 2 , Al claim 2 , and Ca.4. The system of claim 2 , wherein the MOF comprises a linker selected from the group consisting of fumaric acid claim 2 , trimesic acid claim 2 , terephthalic acid claim 2 , citric acid claim 2 , malic acid claim 2 , tartaric acid claim 2 , methanoic acid claim 2 , ethanoic acid claim 2 , propanoic acid claim 2 , butanoic acid claim 2 , valeric acid claim 2 , caproic acid claim 2 , caprylic acid claim 2 , capric acid claim 2 , lauric acid claim 2 , mylistic acid claim 2 , palmitic acid claim 2 , stearic acid claim 2 , oleic acid claim 2 , ...

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Номер записи: 55
17-01-2019 дата публикации

Multifunctional Nanoparticles For Prevention And Treatment Of Atherosclerosis

Номер: US20190015351A1
Автор: Nong Jia, Wang Zhicheng, Zhong Yinghui
Принадлежит:

This disclosure relates to nanoparticles for preventing, treating and reversing atherosclerosis. 1. Nanoparticles having a hydrodynamic diameter of from about 10 to about 400 nm , comprising a polymer comprising positively charged polymer and at least one anionic polymer comprising sulfate groups , phosphate groups , carboxyl groups , or a combination thereof.2. The nanoparticles of claim 1 , wherein said at least one anionic polymer comprises sulfate groups.3. The nanoparticles of claim 2 , wherein said at least one anionic polymer is dextran sulfate claim 2 , cellulose sulfate claim 2 , heparin claim 2 , heparin sulfate claim 2 , chondroitin sulfate claim 2 , dermatan sulfate claim 2 , keratan sulfate claim 2 , alginate sulfate claim 2 , aggrecan claim 2 , fucoidan claim 2 , or polystyrene sulfonate.4. The nanoparticles of claim 1 , wherein said at least one anionic polymer comprises phosphate groups.5. The nanoparticles of claim 4 , wherein said at least one anionic polymer comprises polyphosphate claim 4 , DNA claim 4 , or RNA.6. The nanoparticles of claim 1 , wherein said at least one anionic polymer comprises carboxyl groups.7. The nanoparticles of claim 6 , wherein said at least one anionic polymer is hyaluronic acid claim 6 , pectin claim 6 , carboxymethyl dextran claim 6 , carboxymethyl amylose claim 6 , carboxymethyl cellulose claim 6 , carboxymethyl beta-cyclodextrin claim 6 , poly(acrylic acid) claim 6 , or combinations thereof.8. The nanoparticles of claim 1 , wherein polymer comprising positively charged groups is chitosan claim 1 , glycol chitosan claim 1 , gelatin type A claim 1 , or PEI.9. The nanoparticles of claim 8 , wherein the chitosan has an average molecular weight (M) of from about 10 to about 400 kDa.10. The nanoparticles of claim 1 , wherein the at least one anionic polymer has a Mof greater than about 1 kDa.11. The nanoparticles of claim 1 , further comprising an active agent that is an antibiotic claim 1 , an oxygen scavenger claim 1 , ...

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Номер записи: 56
17-01-2019 дата публикации

NUCLEIC ACID VACCINES

Номер: US20190015501A1
Автор: BOUCHON Axel, Ciaramella Giuseppe, Huang Eric Yi-Chun
Принадлежит: ModernaTX, Inc.

The invention relates to compositions and methods for the preparation, manufacture and therapeutic use ribonucleic acid vaccines (NAVs) comprising polynucleotide molecules encoding one or more antigens. 1. A nucleic acid vaccine , comprising:one or more RNA polynucleotides having an open reading frame encoding a first antigenic polypeptide that is derived from an infectious agent, at least one 5′ terminal cap and at least one chemical modification, formulated within a cationic lipid nanoparticle.2. The nucleic acid vaccine of claim 1 , wherein the vaccine is one RNA polynucleotide.3. The nucleic acid vaccine of claim 1 , wherein the cationic lipid nanoparticle has a molar ratio of about 20-60% ionizable cationic lipid:about 5-25% non-cationic lipid:about 25-55% sterol; and about 0.5-15% PEG-modified lipid.4. The nucleic acid vaccine of claim 1 , wherein the RNA polynucleotide has at least two chemical modifications.5. The nucleic acid vaccine of claim 1 , wherein the open reading frame is codon-optimized.6. The nucleic acid vaccine of claim 3 , wherein the cationic lipid nanoparticle has a polydispersity value of less than 0.4.7. The nucleic acid vaccine of claim 1 , wherein the polynucleotide has a poly-A tail of 80-250 nucleotides in length.8. The nucleic acid vaccine of claim 1 , wherein the nucleic acid vaccine is multivalent.9. The nucleic acid vaccine of claim 1 , wherein the open reading frame of the one or more RNA polynucleotides encode at least 2 claim 1 , 3 claim 1 , or 4 antigenic polypeptides.10. The nucleic acid vaccine of claim 1 , wherein the open reading frame of the one or more RNA polynucleotides encode 1 antigenic polypeptide.11. The nucleic acid vaccine of claim 1 , wherein the cationic lipid nanoparticle comprises a molar ratio of about 55% ionizable cationic lipid claim 1 , about 2.5% PEG lipid claim 1 , about 32.5% cholesterol and about 10% non-cationic lipid.12. The nucleic acid vaccine of claim 1 , wherein the nanoparticle has a mean ...

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Номер записи: 57
19-01-2017 дата публикации

LOW MOLECULAR WEIGHT CATIONIC LIPIDS FOR OLIGONUCLEOTIDE DELIVERY

Номер: US20170015998A1
Автор: BAWIEC, DENG Zhengwu J., III John A.
Принадлежит: Sirna Therapeutics, Inc.

The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA. 2. The cationic lipid of claim 1 , wherein Rand Rare independently selected from the group consisting of H claim 1 , methyl claim 1 , ethyl and propyl.3. The cationic lipid of claim 2 , wherein Rand Reach are methyl.4. The cationic lipid of claim 3 , wherein Ris H or methyl.5. The cationic lipid of claim 4 , wherein Ris H.611. The cationic lipid of claim 1 , wherein is 0 claim 1 , 1 or 2.7. The cationic lipid of claim 6 , wherein n is 0 or 1.8. The cationic lipid of claim 7 , wherein n is 0.9. A lipid nanoparticle comprising a cationic lipid of .10. The lipid nanoparticle of claim 9 , wherein the lipid nanoparticle further comprises an oligonucleotide.11. The lipid nanoparticle of claim 10 , wherein the oligonucleotide is an siRNA or miRNA.12. The lipid nanoparticle of claim 11 , wherein the oligonucleotide is an siRNA.13. The lipid nanoparticle of claim 9 , wherein the lipid nanoparticle further comprises cholesterol and PEG-DMG.14. The lipid nanoparticle of claim 9 , wherein the lipid nanoparticle further comprises cholesterol claim 9 , PEG-DMG and DSPC.15. The lipid nanoparticle of claim 9 , wherein the lipid nanoparticle further comprises cholesterol claim 9 , PEG-C-DMA and DSPC. The present invention relates to novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides, to facilitate the cellular ...

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Номер записи: 58
21-01-2021 дата публикации

DRUG DELIVERY BY PORE-MODIFIED MESOPOROUS SILICA NANOPARTICLES

Номер: US20210015757A1
Автор: CHAN Hardy Wai Hong, Chen Yi-Ping, Mou Chung-Yuan, WU Cheng-Hsun, WU Si-Han, ZHANG Rong-Lin
Принадлежит:

The present disclosure relates to mesoporous silica nanoparticles having modifications on the surface of the (extended) mesopores, which can be further loaded with one or more types of bioactive ingredients within the (extended) mesopores mesopores, processes of preparing the same and applications of the same. 1. A mesoporous silica nanoparticle , characterized in that it comprises organic modification on the surface of its pores and has a particle size of no greater than 100 nm and a hydrodynamic size in a medium , measured by Dynamic Light Scattering (DLS) , of no greater than 150 nm , wherein the organo modification comprises at least one terminal hydrocarbyl moiety , and wherein the medium is biologically similar to or equivalent to phosphate buffered saline (PBS).2. The mesoporous silica nanoparticle of claim 1 , wherein the pore size of the mesoporous silica nanoparticle is no greater than 50 nm.3. The mesoporous silica nanoparticle of claim 1 , wherein the hydrodynamic size of the mesoporous silica nanoparticle is no greater than 100 nm.4. The mesoporous silica nanoparticle of claim 1 , wherein the terminal hydrocarbyl moiety comprises a terminal aromatic moiety claim 1 , a terminal aliphatic moiety or combinations thereof.5. The mesoporous silica nanoparticle of claim 4 , wherein the terminal aromatic moiety is derived from a silane source selected from the group consisting of trimethoxyphenylsilane (TMPS) claim 4 , triethoxyphenylsilane claim 4 , diphenyldiethoxysilane claim 4 , 1-naphthyl trimethoxysilane claim 4 , 2-hydroxy-4-(3-triethoxy silylpropoxy)diphenylketone claim 4 , O-4-methylcoumarinyl-N-[3-(triethoxysilyl)propyl]carbamate claim 4 , 7-triethoxysilylpropoxy-5-hydroxyflavone claim 4 , 3-carbazolylpropyltriethoxysilane claim 4 , bis(2-diphenylphosphinoethyl)methylsilylethyltriethoxysilane and 2-(diphenylphosphino)ethyl triethoxysilane.6. The mesoporous silica nanoparticle of claim 4 , wherein the terminal aliphatic moiety is derived from a silane ...

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Номер записи: 59
15-01-2015 дата публикации

HIGH THROUGHPUT FABRICATION OF NANOPARTICLES

Номер: US20150018412A1
Автор: DEWITT DAVID M.
Принадлежит:

This application provides a high throughput method of making nanoparticles that utilizes plates comprising wells (e.g., 96-well plates). 1. A method of preparing nanoparticles comprising: (i) a first stock solution comprising an active agent and polymers admixed with one or more organic solvents;', '(ii) a second stock solution comprising a surfactant and a solvent in aqueous phase;', '(iii) a third stock solution comprising a water or buffer quench solution; and', '(iv) a fourth stock solution comprising an aqueous carrier and beta-cyclodextrin;, '(a) providing(b) combining a volume of said first stock solution and a volume of said second stock solution to form an emulsification solution;(c) emulsifying said emulsification solution;(d) combining the emulsion formed in step (c) with a volume of the third stock solution;(e) adding a volume of the fourth stock solution to the solution formed in step (d); and separating beta-cyclodextrin and dissolved unencapsulated active agent from the resulting solution; and(f) collecting the nanoparticles from the solution formed in step (e).2. The method according to claim 1 , wherein said active agent is selected from penicillins claim 1 , aminopenicillins claim 1 , penicillins in conjunction with penicillinase inhibitor and/or anti-fungal agents claim 1 , cephalosporins claim 1 , cephamycins claim 1 , carbapenems claim 1 , fluoroquinolones claim 1 , tetracyclines claim 1 , macrolides claim 1 , aminoglycosides claim 1 , erythromycin claim 1 , bacitracin zinc claim 1 , polymyxin claim 1 , polymyxin B sulfates claim 1 , neomycin claim 1 , gentamycin claim 1 , tobramycin claim 1 , gramicidin claim 1 , ciprofloxacin claim 1 , trimethoprim claim 1 , ofloxacin claim 1 , levofloxacin claim 1 , gatifloxacin claim 1 , moxifloxacin claim 1 , norfloxacin claim 1 , sodium sulfacetamide claim 1 , chloramphenicol claim 1 , tetracycline claim 1 , azithromycin claim 1 , clarithyromycin claim 1 , trimethoprim sulfate claim 1 , bacitracin claim 1 ...

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Номер записи: 60
21-01-2021 дата публикации

COMPOSITIONS AND METHODS FOR THE TREATMENT OF A BETA-CATENIN-ASSOCIATED DISEASE OR DISORDER

Номер: US20210015820A1
Автор: Abrams Marc, Ganesh Shanthi
Принадлежит:

Disclosed herein are methods for the treatment of cancer, comprising administering to a subject β-catenin nucleic acid inhibitor molecule and a therapeutically effective amount of an MEK inhibitor or a c-Myc nucleic acid inhibitor molecule. Also disclosed herein is a pharmaceutical composition comprising a therapeutically effective amount of β-catenin nucleic acid inhibitor molecule; a therapeutically effective amount of an MEK inhibitor or a c-Myc nucleic acid inhibitor molecule and at least one pharmaceutical carrier. 144.-. (canceled)45. A method of treating β-catenin-associated cancer in a subject , comprising administering to the subject: a therapeutically effective amount of β-catenin nucleic acid inhibitor molecule; and a therapeutically effective amount of a c-Myc nucleic acid inhibitor molecule.46. The method of claim 45 , wherein the β-catenin-associated cancer is colorectal cancer claim 45 , hepatocellular carcinoma claim 45 , or melanoma.47. The method of claim 45 , wherein the subject is a human.48. The method of claim 45 , wherein the β-catenin nucleic acid inhibitor molecule is a dsRNAi inhibitor molecule.49. The method of claim 45 , wherein the β-catenin nucleic acid inhibitor molecule is a dsRNAi inhibitor molecule claim 45 , wherein the double-stranded region of the molecule is between 15 and 40 nucleotides in length.50. The method of claim 45 , wherein the β-catenin nucleic acid inhibitor molecule is a dsRNAi inhibitor molecule comprising a sense and an antisense strand and a duplex region of between 18 and 40 nucleotides claim 45 , wherein the sense strand is 25-34 nucleotides in length and the antisense strand is 26-38 nucleotides in length and comprises 1-5 single-stranded nucleotides at its 3′ terminus.51. The method of claim 50 , wherein the sense strand comprises the sequence of SEQ ID NO: 1.52. The method of claim 50 , wherein the antisense strand comprises the sequence of SEQ ID NO: 2.53. The method of claim 45 , wherein the c-Myc nucleic ...

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Номер записи: 61
17-01-2019 дата публикации

COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS

Номер: US20190016669A1
Автор: BENENATO Kerry E., CORNEBISE Mark
Принадлежит:

The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression. 2. The compound of claim 1 , wherein Ris selected from the group consisting of NH claim 1 , alkylamino claim 1 , and dialkylamino.3. The compound of claim 1 , wherein Ris selected from the group consisting of methylamino claim 1 , and dimethylamino.4. The compound of claim 1 , wherein Rand Rare the same.5. The compound of claim 4 , wherein Rand Rare Calkyl.6. The compound of claim 1 , wherein n is 3.8. The compound of claim 7 , wherein R′ is C9 alkyl.9. The compound of claim 7 , wherein l is 5.10. The compound of claim 7 , wherein o is 5.11. The compound of claim 7 , wherein Ris selected from the group consisting of NH claim 7 , alkylamino claim 7 , and dialkylamino.12. The compound of claim 7 , wherein Ris selected from the group consisting of methylamino and dimethylamino.14. A nanoparticle composition comprising a lipid component comprising a compound of .15. The nanoparticle composition of claim 14 , wherein the lipid component further comprises a phospholipid selected from the group consisting of 1 claim 14 ,2-dilinoleoyl-sn-glycero-3-phosphocholine (DLPC) claim 14 , 1 claim 14 ,2-dimyristoyl-sn-glycero-phosphocholine (DMPC) claim 14 , 1 claim 14 ,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) claim 14 , 1 claim 14 ,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) claim 14 , 1 claim 14 ,2-distearoyl-sn-glycero-3-phosphocholine (DSPC) claim 14 , 1 claim 14 ,2-diundecanoyl-sn-glycero-phosphocholine (DUPC) claim 14 , 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) claim 14 , 1 claim 14 ,2-di-O-octadecenyl-sn ...

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Номер записи: 62
28-01-2016 дата публикации

Novel Formulation of Indomethacin

Номер: US20160022637A1
Автор: Aaron Dodd, Adrian Russell, Felix Meiser, H. William Bosch, Marck Norret
Принадлежит: Iceutica Pty Ltd

The present invention relates to methods for producing particles of indomethacin using dry milling processes as well as compositions comprising indomethacin, medicaments produced using indomethacin in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of indomethacin administered by way of said medicaments.

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Номер записи: 63
28-01-2016 дата публикации

LIPID NANOMATERIAL CONTAINING LYSOPHOSPHATIDYLCHOLINE OR DERIVATIVE THEREOF AND METHOD FOR PREPARING SAME

Номер: US20160022711A1
Автор: Choung Jai Jun, KIM Myung Hwa, Kim Young Sam, Ku sae Kwang, SEOL Du Jin, Sung Soo Hyun
Принадлежит:

The present invention relates to a lipid nanomaterial containing lysophosphatidylcholine or an ether derivative thereof, a method for preparing the same, a method for reducing erythrocyteolysis and hemagglutination using the compound, and a pharmaceutical agent containing the lipid nanomaterial. The present invention contains lysophosphatidylcholine or an ether derivative thereof as an active ingredient, and can be useful as a treatment agent for septicemia, bacterial infection diseases, and the like. 1. A lipid nanomaterial , comprising:(a) a lipid construct containing a triglyceride, oil, and lecithin; and(b) lysophosphatidylcholine or an ether derivative thereof, as a pharmaceutically active ingredient.3. The lipid nanomaterial of claim 1 , wherein the triglyceride is a middle chain triglyceride.4. The lipid nanomaterial of claim 1 , wherein the weight ratio of triglyceride:oil:lecithin is 1:0.5-3:2-10.5. The lipid nanomaterial of claim 1 , wherein the weight ratio of the lysophosphatidylcholine or ether derivative thereof and the lipid construct is 1:1-50.6. The lipid nanomaterial of claim 1 , wherein the lipid nanomaterial is nanoparticles having a size of 1-1000 nm.7. The lipid nanomaterial of claim 1 , wherein the lipid nanomaterial exhibits claim 1 , compared with the lysophosphatidylcholine or ether derivative thereof claim 1 , (i) the improvement in solubility claim 1 , (ii) the reduction in toxicity claim 1 , (iii) the reduction in hemolysis claim 1 , or (iv) the reduction in erythrocyte aggregation.8. A method for preparing a lipid nanomaterial containing lysophosphatidylcholine or an ether derivative thereof claim 1 , the method comprising:(a) obtaining a lipid mixture solution by mixing lysophosphatidylcholine or an ether derivative thereof with an aqueous solvent, a triglyceride, oil, and lecithin;(b) homogenizing the lipid mixture solution in step (a);(c) adjusting the homogenized lipid mixture solution in step (b) to pH 3-7; and(d) emulsifying the ...

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Номер записи: 64
17-04-2014 дата публикации

SILVER NANOPLATE COMPOSITIONS AND METHODS

Номер: US20140105982A1
Автор: Miranda Martin G., Oldenburg Steven J., Sebba David S.
Принадлежит: NANOCOMPOSIX, INC.

Embodiments of the present invention relate to methods for preparing high optical density solutions of nanoplates, such as silver nanoplates or silver platelet nanoparticles, and to nanoparticles, solutions and substrates prepared by said methods. The process can include the addition of stabilizing agents (e.g., chemical or biological agents bound or otherwise linked to the nanoparticle surface) that stabilize the nanoparticle before, during, and/or after concentration, thereby allowing for the production of a stable, high optical density solution of silver nanoplates. The process can also include increasing the concentration of silver nanoplates within the solution, and thus increasing the solution optical density. 1. (canceled)2. A process for increasing the optical density of a solution of stable , silver nanoplates , comprising:{'sup': '−1', 'providing a solution comprising silver nanoplates having a plate shape, an extinction spectra, and a first peak optical density between 0.1-10 cm;'}adding a concentration stabilizing chemical agent to the solution of silver nanoplates; and{'sup': '−1', 'increasing the concentration of silver nanoplates using tangential flow filtration, thereby increasing the optical density of the solution to a second peak optical density greater than 10 cm,'}{'sup': '−1', 'wherein the silver nanoplates retain the plate shape and the extinction spectra at the second peak optical density greater than 10 cm.'}3. The process of claim 2 , wherein the stabilizing agent comprises at least one of the group consisting of polyvinyl pyrollidone claim 2 , polyvinyl alcohol claim 2 , polyethylene glycol claim 2 , and dextran.4. The process of claim 2 , wherein the stabilizing agent comprises at least one of the group consisting of polysulphonates claim 2 , ethylene oxides claim 2 , phenols claim 2 , and carbohydrates.5. The process of claim 2 , wherein the concentration stabilizing chemical agent is a water soluble polymer.6. The process of claim 2 , ...

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Номер записи: 65
25-01-2018 дата публикации

COMPOSITIONS AND METHODS FOR NANOPARTICLE-BASED DRUG DELIVERY AND IMAGING

Номер: US20180021265A1
Автор: GRIMM Jan, Kaittanis Charalambos, SHAFFER Travis M.
Принадлежит: Memorial Sloan Kettering Cancer Center

Methods and compositions described herein use polysaccharide nanoparticles (or polysaccharide-coated nanoparticles) to retain and deliver unaltered therapeutic agents to sites of disease. The polysaccharide nanoparticles are non-covalently associated with the unaltered therapeutic agent. The polysaccharide is able to retain cargo (drugs, diagnostics, etc.) without chemical modification of the agent. The nanoparticle maintains its association with the agent through non-covalent interactions but releases its agent in response to changes in the microenvironment, e.g., at the site of cancer cells or cancer tissue. 1. A method of delivering one or more agents to a site in a subject , the method comprising:administering a nanoparticle composition comprising:one or more unaltered agents associated with nanoparticles comprising a polysaccharide wherein an intensity-weighted average diameter of the nanoparticles as determined by dynamic light scattering is from 1 nm to 500 nm.2. (canceled)3. The method of claim 1 , wherein the nanoparticles are at least 50 wt. % polysaccharide (e.g. claim 1 , at least 60 wt. % claim 1 , at least 70 wt. % claim 1 , at least 80 wt. % claim 1 , at least 90 wt. %).4. The method of claim 1 , wherein each of the nanoparticles have a surface comprising the polysaccharide.56-. (canceled)7. The method of claim 1 , wherein the polysaccharide comprises a member selected from the group consisting of dextran claim 1 , amylose claim 1 , amylopectin claim 1 , glycogen claim 1 , cellulose claim 1 , arabonixylan claim 1 , and pectin.8. The method of claim 1 , wherein the disease claim 1 , disorder claim 1 , or condition is a member selected from the group consisting of cancer claim 1 , rheumatoid arthritis claim 1 , atherosclerosis claim 1 , cystic fibrosis claim 1 , diabetic ketoacidosis claim 1 , cardiac arrest claim 1 , stroke claim 1 , renal failure claim 1 , malaria claim 1 , lactic acid acidosis claim 1 , and inflammation.922-. (canceled)23. A ...

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Номер записи: 66
22-01-2015 дата публикации

LYMPH NODE-TARGETING NANOPARTICLES

Номер: US20150023909A1
Автор: Abraham Soman, Leong Kam, St. John Ashley, Staats Herman
Принадлежит:

Provided are nanoparticles comprising heparin, chitosan, and at least one immunomodulatory agent, e.g. a cytokine. The cytokine can be selected from the group consisting of TNF, IL-12, IL-2, IL-23, IL-1α, IL-10, IL-18, and combinations thereof. Further provided are methods of making a nanoparticle comprising mixing a first composition comprising heparin with a second composition comprising chitosan in the presence of at least one cytokine to form a third composition. Further provided are methods of modulating an immune response comprising co-administering to a subject an antigen or vaccine with nanoparticles comprising heparin, chitosan, and at least one cytokine. 129-. (canceled)30. A method of treating a disease claim 33 , disorder claim 33 , or a condition associated with a disease or disorder comprising attenuating an immune response according to the method of .3132-. (canceled)33. A method of attenuating an immune response comprising administering to a subject a nanoparticle comprising:heparin; andchitosan,wherein the heparin and the chitosan nanoparticle encapsulates IL-12.34. A method of treating an allergic condition comprising attenuating an immune response according to the method of .35. (canceled)3637-. (canceled)38. The method of claim 33 , wherein the nanoparticle further comprises an antigen.39. The method of claim 33 , wherein the nanoparticle further comprises at least one immunomodulatory agent selected from the group consisting of TNF claim 33 , IL-1α claim 33 , IL-2 claim 33 , IL-23 claim 33 , IL-18 claim 33 , IL-10 claim 33 , and IFN.40. The method of claim 34 , wherein the allergic condition is selected from the group consisting of food allergies and asthma. This application is a divisional of and claims priority to U.S. patent application Ser. No. 13/252,516, filed Oct. 4, 2011, which claims the benefit of U.S. Provisional Patent Application No. 61/389,457, filed Oct. 4, 2010, and are incorporated herein by reference in their entireties.This ...

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Номер записи: 67
10-02-2022 дата публикации

Methods and Compositions of Treating an Ophthalmic Condition

Номер: US20220040166A1
Автор: Wayne Rothbaum
Принадлежит: Kartos Therapeutics

Therapeutic methods and pharmaceutical compositions for treating an ophthalmic condition including age-related macular degeneration in a human subject are described. In certain embodiments, the invention includes therapeutic methods using an MDM2 inhibitor.

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Номер записи: 68
10-02-2022 дата публикации

Composition and Method of mRNA Vaccines Against Novel Coronavirus Infection

Номер: US20220040292A1
Автор: HE Jiaxi, HE Ziyang, Lu Chun, Lu Patrick Y., SHEN Dong, TANG Shenggao
Принадлежит:

Compositions and methods are provided for potent mRNA vaccines for prevention and treatment of 2019 novel Coronavirus (2019-nCoV) infections. The compositions include a pharmaceutical composition containing one or more mRNA molecules encoding spike protein epitopes, including mutated epitopes, or mRNA cocktails that encode critical viral genes together with pharmaceutically acceptable polymeric nanoparticle carriers and liposomal nanoparticle carriers. Methods for stimulating system immune responses and treatment are provided, including subcutaneous, intraperitoneal and intramuscular injections. 1. A composition comprising an effective amount of a messenger ribonucleic acid (mRNA) that comprises an open reading frame (ORF) encoding a 2019-nCoV protein or protein fragment formulated in a pharmaceutically acceptable carrier , wherein said mRNA and said carrier form a polymeric nanoparticle.2. The composition of claim 1 , wherein the 2019-nCoV protein is a spike (S) protein or spike (S) subunit.3. The composition of claim 1 , wherein the ORF encoding the 2019-nCoV protein or protein fragment is selected from the group consisting of mRNA molecules encoding the protein or fragment selected from SEQ ID NOs: 11 claim 1 , 13 to 31 claim 1 , 50 to 66 claim 1 , 68 claim 1 , 70 claim 1 , 72 claim 1 , 74 or 90.45-. (canceled)6. The composition of claim 1 , wherein the 2019-nCoV protein or protein fragment is encoded by any one of SEQ ID NOs: 1-4 claim 1 , 10 claim 1 , 12 claim 1 , 32 to 49 claim 1 , 67 claim 1 , 69 claim 1 , 71 claim 1 , 73 claim 1 , 89 claim 1 , 91 to 95 or 108.7. (canceled)8. The composition of claim 6 , wherein said ORF encoding the 2019-nCoV protein or protein fragment comprises any one of SEQ ID NOs: 96 to 106.911-. (canceled)12. The composition of claim 1 , further comprising an mRNA comprising all or part of orf1a or orf1b or both claim 1 , wherein said mRNA encodes a 2019-nCoV non-structural protein polymerase or RdRp or both.13. The composition of ...

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Номер записи: 69
10-02-2022 дата публикации

Lipid nanoparticle compositions and methods for mrna delivery

Номер: US20220040330A1
Автор: Braydon Charles Guild, Frank DeRosa, Michael Heartlein
Принадлежит: Translate Bio Inc

Disclosed herein are compositions and methods for modulating the production of a protein in a target cell. The compositions and methods disclosed herein are capable of ameliorating diseases associated with protein or enzyme deficiencies.

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Номер записи: 70
26-01-2017 дата публикации

NOVEL LOW MOLECULAR WEIGHT CATIONIC LIPIDS FOR OLIGONUCLEOTIDE DELIVERY

Номер: US20170022146A1
Автор: Colletti Steven L., Stanton Matthew G.
Принадлежит: Sirna Therapeutics, Inc.

The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA. 2. The cationic lipid of claim 1 , wherein Rand Rare independently selected from the group consisting of H claim 1 , methyl claim 1 , ethyl and propyl.3. The cationic lipid of claim 2 , wherein Rand Reach are methyl.4. The cationic lipid of claim 3 , wherein Ris H or methyl.5. The cationic lipid of claim 4 , wherein Ris H.6. The cationic lipid of claim 1 , wherein n is 2 claim 1 , 3 or 4.7. The cationic lipid of claim 6 , wherein n is 3.8. The cationic lipid of claim 1 , wherein X is O claim 1 , NR″ claim 1 , (C═O)O claim 1 , NR″(C═O) claim 1 , o(C•O)O claim 1 , NR″(C═O)NR″ claim 1 , O(C═O)NR″ or NR″(C═O)O.9. The cationic lipid of claim 8 , wherein X is (C═O)O.10. The cationic lipid of claim 1 , wherein Lis C-Calkyl or C-Calkenyl.11. The cationic lipid of claim 10 , wherein Lis C-Calkyl or C-Calkenyl.12. A lipid nanoparticle comprising a cationic lipid of .13. The lipid nanoparticle of claim 12 , wherein the lipid nanoparticle further comprises an oligonucleotide.14. The lipid nanoparticle of claim 13 , wherein the oligonucleotide is an siRNA or miRNA.15. The lipid nanoparticle of claim 14 , wherein the oligonucleotide is an siRNA.16. The lipid nanoparticle of claim 12 , wherein the lipid nanoparticle further comprises cholesterol and PEG-DMG.17. The lipid nanoparticle of claim 12 , wherein the lipid nanoparticle further comprises cholesterol claim 12 , PEG-DMG and DSPC.18. The lipid nanoparticle ...

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Номер записи: 71
24-01-2019 дата публикации

POLYNUCLEOTIDES ENCODING METHYLMALONYL-CoA MUTASE

Номер: US20190022019A1
Автор: Paolo Martini, Vladimir PRESNYAK
Принадлежит: ModernaTx Inc

The disclosure relates to polynucleotides comprising an open reading frame of linked nucleosides encoding human methylmalonyl-CoA mutase precursor, human methylmalonyl-CoA mutase (MCM) mature form, or functional fragments thereof. In some embodiments, the disclosure includes methods of treating methylmalonic acidemia in a subject in need thereof comprising administering an mRNA encoding an MCM polypeptide.

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Номер записи: 72
23-01-2020 дата публикации

Dry powder formulations for messenger rna

Номер: US20200022921A1
Автор: Ashish Sarode, Frank DeRosa, Michael Heartlein, Shrirang KARVE, Zarna Patel
Принадлежит: Translate Bio Inc

The present invention provides stable, dry powder messenger RNA formulations for therapeutic use, and methods of making and using the same.

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Номер записи: 73
23-01-2020 дата публикации

LIPID-BASED NANOPARTICLES AND METHODS USING SAME

Номер: US20200022922A1
Автор: Geho W. Blair
Принадлежит:

The invention provides an improved lipid-based nanoparticle, which can be used to deliver a therapeutic agent to a subject, such as but not limited to a mammal, such as but not limited to a human. In certain embodiments, the nanoparticle of the invention has reduced aggregation properties as compared to those taught in the prior art. 1. A composition comprising a lipid-based nanoparticle ,wherein the nanoparticle is enclosed by a bipolar lipid membrane, which comprises cholesterol, dicetyl phosphate, 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC), and 2,3-diacetoxypropyl 2-(5-((3aS,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamido) ethyl phosphate (biotin DHPE);wherein the membrane further comprises at least one agent selected from the group consisting of stearoyl lysophosphatidylcholine and m-cresol; (a) about 9.4:18.1:56.8:14.1:0.0:1.5,', '(b) about 7.7:15.0:58.6:0.0:17.4:1.3, and', '(c) about 8.4:16.2:47.5:7.6:19.0:1.3;, 'wherein the membrane comprises cholesterol, dicetyl phosphate, DSPC, stearoyl lysophosphatidylcholine, m-cresol, and biotin DHPE in a % (w/w) ratio selected from the group consisting ofwherein the biotin-DHPE extends outward from the nanoparticle; andwherein the size of the nanoparticle ranges from about 10 nm to about 150 nm.2. The composition of claim 1 , wherein a therapeutic agent is dispersed within the nanoparticle.3. The composition of claim 2 , wherein the therapeutic agent is covalently bound to the nanoparticle or wherein the therapeutic agent is not covalently bound to the nanoparticle.4. The composition of claim 2 , wherein the therapeutic agent comprises at least one selected from the group consisting of insulin claim 2 , insulin analogs claim 2 , interferon claim 2 , parathyroid hormone claim 2 , calcitonin claim 2 , serotonin claim 2 , serotonin agonist claim 2 , serotonin reuptake inhibitor claim 2 , human growth hormone claim 2 , GIP claim 2 , anti-GIP monoclonal antibody claim 2 , metformin claim 2 , ...

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Номер записи: 74
28-01-2021 дата публикации

COMPOSITIONS FOR THE DELIVERY OF tRNA AS NANOPARTICLES AND METHODS OF USE THEREWITH

Номер: US20210023120A1
Автор: Johnson Arthur E., Miller Jason B., SIEGWART Daniel J., Thomas Philip J., Torres Michael J.
Принадлежит: The Board of Regents of the University of Texas System

In some aspects, the present disclosure provides a nanoparticle composition comprising tRNA and an aminolipid delivery compound. The aminolipid delivery compound may be a dendrimer, dendron, or dendritic lipid, a polymer such as a polyamide or polyester, or a lipid with one or more hydrophobic components. In some embodiments, these compositions may be administered to a patient to treat a genetic disease or disorder such as cystic fibrosis, Duchene muscular dystrophy, or cancer. 1. A method for delivering a transfer ribonucleic acid (tRNA) into a cell of a subject , the method comprising contacting said cell with a composition comprising an aminolipid compound coupled to said tRNA , thereby delivering said tRNA into said cell of said subject.2. The method of claim 1 , wherein said aminolipid compound comprises a group that is positively charged at a physiological pH.3. The method of claim 1 , wherein said tRNA introduces an amino acid into a growing peptide chain of a protein in said cell at a position that corresponds to a mutation in a gene encoding said protein.4. The method of claim 3 , wherein said mutation is a nonsense mutation.5. The method of claim 3 , wherein said tRNA reduces an amount of a non-functional variant of said protein in said cell as compared to an amount of said non-functional variant of said protein generated in absence of said contacting.6. The method of claim 3 , wherein said mutation in said gene is associated with a genetic disease or disorder.7. The method of claim 1 , wherein said tRNA is a suppressor tRNA.8. The method of claim 7 , wherein said suppressor tRNA is an amber suppressor tRNA claim 7 , an opal suppressor tRNA claim 7 , an ochre suppressor tRNA claim 7 , or a frameshift suppressor tRNA.9. The method of claim 1 , wherein said aminolipid compound is a dendrimer claim 1 , a polymer claim 1 , a zwitterionic aminolipid claim 1 , or a cationic aminolipid.13. The method of claim 10 , wherein Aand Aare each independently —O— or —NR—. ...

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Номер записи: 75
24-01-2019 дата публикации

POLYNUCLEOTIDE AGENTS TARGETING FACTOR XII (HAGEMAN FACTOR) (F12) AND METHODS OF USE THEREOF

Номер: US20190024088A1
Автор: Hinkle Gregory
Принадлежит: Alnylam Phaarmaceuticals, Inc.

The invention relates to polynucleotide agents targeting Factor XII (F12) gene, and methods of using such polynucleotide agents to inhibit expression of Factor XII and to treat subjects having a Factor XII-associated disease, e.g., heredity angioedema (HAE), prekallikrein deficiency, malignant essential hypertension, hypertension, end stage renal disease, or Fletcher Factor Deficiency. 1. An antisense polynucleotide agent for inhibiting expression of a Factor XII (F12) gene , wherein the agent comprises 4 to 50 contiguous nucleotides , wherein at least one of the contiguous nucleotides is a modified nucleotide , and wherein the nucleotide sequence of the agent is 80% complementary over its entire length to the equivalent region of the nucleotide sequence of any one of SEQ ID NOs:1-4.2. An antisense polynucleotide agent for inhibiting expression of a Factor XII (F12) gene , wherein the agent comprises 4 to 50 contiguous nucleotides , wherein at least one of the contiguous nucleotides is a modified nucleotide , and wherein the nucleotide sequence of the agent is 80% complementary over its entire length to the equivalent region of the nucleotide sequence of any one of residues 21-74 , 87-106 , 143-183 , 209-239 , 254-273 , 287-315 , 320-350 , 352-392 , 395-414 , 352-414 , 430-470 , 472-568 , 595-680 , 595-669 , 682-701 , 736-899 , 793-843 , 793-899 , 804-899 , 901-942 , 736-942 , 968-987 , 990-1097 , 990-1042 , 1100-1197 , 1100-1206 , 1210-1252 , 1210-1240 , 1253-1272 , 1298-1406 , 1308-1406 , 1430-1515 , 1430-1482 , 1541-1560 , 1583-1602 , 1683-1714 , 1727-1768 , 1737-1756 , 1781-1976 , 1816-1868 , 1902-1967 , 1891-1957 , 1992-2043 , and 1992-2033 of SEQ ID NO:1.3. The agent of or , wherein the equivalent region is one of the target regions of SEQ ID NO:1 provided in Table 3.4. The agent of claim 3 , wherein the equivalent region is one of the target regions selected from the group consisting of the regions targeted by antisense agent A-145669 claim 3 , A-145668 claim ...

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Номер записи: 76
04-02-2016 дата публикации

On-demand drug release using magneto-electric nanoparticles

Номер: US20160030724A1
Автор: Ping Liang, Rakesh GUDURU, Sakhrat Khizroev
Принадлежит: Florida International University FIU

Disclosed herein are methods of delivering drugs to a subject in a controlled release fashion by administering a magneto-electric nanoparticle having ionic bonds to a drug then applying a magnetic field to weaken the ionic bonds and release the drug.

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Номер записи: 77
01-02-2018 дата публикации

Compositions and Methods for the Delivery of Therapeutics

Номер: US20180028457A1
Автор: Gendelman Howard E., Liu Xin-Ming
Принадлежит:

The present invention provides compositions and methods for the delivery of antivirals to a cell or subject. 1. A nanoparticle comprising at least one CCR5 receptor antagonist , at least one hydrophobic polymer , and at least one surfactant.2The nanoparticle of claim 1 , wherein said hydrophobic polymer is poly(lactic-co-glycolic acid).3. The nanoparticle of claim 1 , wherein said surfactant is a glycerophospholipid.4. The nanoparticle of claim 3 , wherein said glycerophospholipid is selected from the group consisting of 1 claim 3 ,2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE) claim 3 , 1 claim 3 ,2-distearoyl-sn-glycero-3-phosphocholine (DSPC) claim 3 , and 1 claim 3 ,2-distearoyl-sn-glycero-3-phosphoglycerol (DSPG).5. The nanoparticle of claim 4 , wherein said glycerophospholipid is conjugated to polyethylene glycol.6. The nanoparticle of claim 1 , wherein said CCR5 receptor antagonist is maraviroc.7. The nanoparticle of claim 1 , wherein said nanoparticle comprises a surfactant linked to at least one targeting ligand.8. The nanoparticle of claim 7 , wherein claim 7 , said targeting ligand is a macrophage targeting ligand.9. The nanoparticle of claim 8 , wherein said macrophage targeting ligand is folate.10. The nanoparticle of claim 1 , wherein said CCR5 receptor antagonist is maraviroc claim 1 , wherein said hydrophobic polymer is poly(lactic-co-glycolic acid) claim 1 , wherein said surfactant is a glycerophospholipid claim 1 , optionally conjugated to polyethylene glycol.11. The nanoparticle of claim 10 , wherein said glycerophospholipid is selected from the group consisting of 1 claim 10 ,2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE) claim 10 , 1 claim 10 ,2-distearoyl-sn-glycero-3-phosphocholine (DSPC) claim 10 , and 1 claim 10 ,2-distearoyl-sn-glycero-3-phosphoglycerol (DSPG).12. A pharmaceutical composition comprising at least one nanoparticle of and at least one pharmaceutically acceptable carrier.13. The pharmaceutical composition of claim ...

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Номер записи: 78
29-01-2015 дата публикации

METHOD FOR PREPARING NANO PARTICLES

Номер: US20150031707A1
Автор: Kim Kab Sig, Park Joo Won
Принадлежит: BIO-SYNECTICS INC.

The present invention relates to a method for manufacturing nano-scale particles of an active material. More particularly, the present invention relates to a method which uniformly mixes a surfactant having an HLB value of 8 or more and a melting point or glass transition temperature of 80° C. or lower and an active material, and mills the mixture using a roller mill, to thereby prepare nanoparticle powder from the active material. 1. A method for preparing nanoparticle powder of an active ingredient , comprising:(1) uniformly mixing an active ingredient with a surfactant having an HLB value of 8 or more and a melting point or a glass transition temperature of 80° C. or lower; and(2) grinding the mixture obtained in step (1) by using a roller mill.2. The method for preparing nanoparticle powder of an active ingredient according to claim 1 , wherein the mixture obtained in step (1) further comprises a biocompatible polymer.3. The method according to claim 1 , wherein the mixture obtained in step (1) further comprises a saccharide or a salt.4. The method according to claim 1 , wherein the active ingredient is one or more selected from the group consisting of physiologically active organic compounds claim 1 , organometallic compounds claim 1 , natural extracts claim 1 , peptides claim 1 , proteins and polysaccharides.5. The method according to claim 1 , wherein the surfactant is selected from the group consisting of phospholipids claim 1 , benzalkonium chloride claim 1 , glycerin esters of fatty acid claim 1 , cetomacrogol claim 1 , polyoxyethylene alkyl ethers claim 1 , polyoxyethylene stearate claim 1 , polyoxyethylene fatty acid esters claim 1 , sorbitan esters claim 1 , polyoxyethylene castor oil derivatives claim 1 , polyoxyethylene sorbitan fatty acid esters claim 1 , sucrose fatty acid esters claim 1 , PEG-cholesterol claim 1 , PEG-vitamin E and mixtures thereof.6. The method according to claim 2 , wherein the biocompatible polymer is selected from the group ...

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Номер записи: 79
17-02-2022 дата публикации

PEG LIPIDS AND USES THEREOF

Номер: US20220047518A1
Автор: Benenato Kerry, Hennessy Edward J.
Принадлежит: Moderna TX, Inc.

The present disclosure in part provides compounds (i.e., PEG lipids) which are useful in pharmaceutical compositions, cosmetic compositions, and drug delivery systems, e.g, for use in lipid nanoparticle (LNP) formulations. The present disclosure also provides LNP formulations comprising PEG lipids described herein, and methods of using the same. For example, the LNPs provided herein are useful for the delivery of an agent (e.g, therapeutic agent) to a subject. The PEG lipids and LNPs provided herein, in certain embodiments, exhibit increased PEG shedding compared to existing PEG lipids and LNP formulations. 30. The LNP of any one of the preceding claims , wherein Lis L.32. The LNP of any one of the preceding claims , wherein Yis —O— , —NR— , or —S—.33. The LNP of any one of the preceding claims , wherein Ris hydrogen.34. The LNP of any one of the preceding claims , wherein Ris optionally substituted Calkyl.35. The LNP of any one of the preceding claims , wherein Ris unsubstituted Calkyl.36. The LNP of any one of the preceding claims , wherein m is 12 , 13 , 14 , or 15.37. The LNP of any one of the preceding claims , wherein s is 12 , 13 , 14 , 15 , 16 , 17 , or 18.38. The LNP of any one of the preceding claims , wherein Ris hydrogen or methyl.39. The LNP of any one of the preceding claims , wherein r is an integer from 35-55 , inclusive.40. The LNP of any one of the preceding claims , wherein r is an integer from 40-50 , inclusive.41. The LNP of any one of the preceding claims , wherein the LNP comprises about 0.15-15% of the PEG lipids.42. The LNP of any one of the preceding claims , wherein the LNP comprises about 1-2% of the PEG lipids.43. The LNP of any one of the preceding claims , wherein the LNP comprises about 1.5% of the PEG lipids.44. The LNP of any one of the preceding claims , further comprising an ionizable amino lipid.51. The LNP of claim any one of - , wherein the ionizable amino lipid is present in a molar ratio of about 25-65% with respect to other ...

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Номер записи: 80
17-02-2022 дата публикации

METHOD OF LYOPHILIZING LIPID NANOPARTICLES

Номер: US20220047519A1
Автор: Bao Yanjie, Karmali Priya Prakash, Sagi Amit
Принадлежит:

Methods of preparing lyophilized lipid nanoparticle-nucleic acid compositions are provided. The methods comprise preparing a suspension of lipid nanoparticles with a monosaccharide and one or more excipients selected from thiosulfate, potassium sorbate, sodium benzoate, and iodixanol. Lyophilized lipid nanoparticle-nucleic acid compositions and methods of reconstituting and administering the same are further provided. 195.-. (canceled)96. A lyophilized composition comprising lipid nanoparticles encapsulating an RNA , poloxamer , potassium sorbate , and a sugar.97. The composition of claim 96 , wherein the poloxamer is poloxamer 188.98. The composition of claim 96 , wherein the lyophilized composition comprises about 0.001 to about 1.0% w/w of the RNA.99103.-. (canceled)104. The composition of claim 96 , wherein the lyophilized composition comprises about 0.5 to about 5.0% w/w lipids.105106.-. (canceled)107. The composition of claim 96 , wherein the lyophilized composition further comprises about 0.5 to about 2.5% w/w of TRIS buffer.108109.-. (canceled)110. The composition of claim 96 , wherein the lyophilized composition further comprises about 0.75 to about 2.75% w/w of NaCl.111112.-. (canceled)113. The composition of claim 96 , wherein the lyophilized composition comprises about 85 to about 96% w/w of the sugar.114115.-. (canceled)116. The composition of claim 96 , wherein the sugar is sucrose.117. The composition of claim 96 , wherein the lyophilized composition comprises about 0.01 to about 1.0% w/w of the poloxamer.118124.-. (canceled)125. The composition of claim 96 , wherein the poloxamer is poloxamer 188.126. The composition of claim 96 , wherein the lyophilized composition comprises about 0.5 to about 5.0% w/w of potassium sorbate.127129-. (canceled)130. A method of preserving a lyophilized composition of comprising storing the lyophilized product at a temperature of about 2° C. to about 8° C.131. A method of preserving a lyophilized composition of ...

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Номер записи: 81
17-02-2022 дата публикации

AEROSOLIZED FLUOROQUINOLONES AND USES THEREOF

Номер: US20220047604A1
Автор: Bostian Keith A., Dudley Michael N., Griffith David C., Rodny Olga, Surber Mark W.
Принадлежит:

Disclosed herein are formulations of fluoroquinolones suitable for aerosolization and use of such formulations for aerosol administration of fluoroquinolone antimicrobials for the treatment of pulmonary bacterial infections. In particular, inhaled levofloxacin specifically formulated and delivered for bacterial infections of the lungs is described. Methods include inhalation protocols and manufacturing procedures for production and use of the compositions described. 122-. (canceled)23Pseudomonas aeruginosa, Mycobacterium tuberculosis, Mycobacterium avium, Mycobacterium intracellulareMycobacterium leprae. A method of treating a bacterial lung infection caused by one or more of the following bacteria: , and , comprising administering a pharmaceutical aerosol for nasal , sinunasal or pulmonary administration comprising a dispersed liquid phase and a continuous gas phase , wherein the dispersed liquid phase:(a) consists essentially of aqueous droplets comprising levofloxacin, and at least one excipient comprising a multivalent metal ion;(b) has a mass median diameter from about 1 to about 5 sm; and(c) has a droplet size distribution exhibiting a geometrical standard deviation less than or equal to about 3.0 sm.24. The method of claim 23 , wherein at least about 20 mg of levofloxacin is administered to the lung.25. The method of claim 24 , wherein at least about 100 mg of levofloxacin is administered to the lung.26. The method of claim 25 , wherein at least about 125 mg of levofloxacin is administered to the lung.27. The method of claim 26 , wherein at least about 150 mg of levofloxacin is administered to the lung.28. The method of claim 23 , wherein the aerosol is administered to the lung in less than about 10 minutes.29. The method of claim 28 , wherein the aerosol is administered to the lung in less than about 5 minutes.30. The method of claim 29 , wherein the aerosol is administered to the lung in less than about 3 minutes.31. The method of claim 30 , wherein the ...

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Номер записи: 82
01-02-2018 дата публикации

COMPOSITIONS AND METHODS TO MODIFY CELLS FOR THERAPEUTIC OBJECTIVES

Номер: US20180030153A1
Автор: Stephan Matthias
Принадлежит:

The present disclosure provides compositions and methods that rapidly and selectively modify cells of the immune system to achieve therapeutic objectives. The methods can be practiced in vivo and any cell type that expresses a known marker can be targeted for a therapeutic objective. 142-. (canceled)43. A method of selectively transfecting T cells with a polynucleotide in vivo through receptor-mediated endocytosis , the method comprising: (i) a negatively-charged coating surrounding a porous core;', '(ii) a lymphocyte-directing agent extending from the surface of the nanocarrier wherein the lymphocyte-directing agent comprises a binding domain consisting of an ScFv fragment of a CD3 antibody or an ScFv fragment of a CD8 antibody that induces receptor-mediated endocytosis upon binding to CD3 or CD8 on the surface of a T cell; and', '(iii) a polynucleotide encoding a chimeric antigen receptor (CAR) targeting agent within the pores of the core;, 'Infusing a nanocarrier into the bloodstream of a subject wherein the nanocarrier comprises'}thereby selectively transfecting T cells with the polynucleotide in vivo through receptor-mediated endocytosis.44. A method of wherein the binding domain consists of SEQ ID NO. 1.45. A method of wherein the polynucleotide is a plasmid claim 43 , a minicircle plasmid claim 43 , or an mRNA molecule.46. A method of wherein the CAR is P28z.47. A method of wherein the nanocarrier further comprises an endosomal release agent extending from the surface of the nanocarrier and (ii) a nuclear localization signal (NLS) within the pores of the core.48. A method of wherein the endosomal release agent is selected from any one of SEQ ID NOs. 29-50.49. A method of wherein the NLS is selected from any one of SEQ ID NOS. 51-93.50. A method of wherein the nanocarrier further comprises a S/MAR element claim 43 , a PiggyBac transposase-containing plasmid claim 43 , or a Sleeping Beauty transposase-containing plasmid.51. A method of wherein the CAR targeting ...

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Номер записи: 83
31-01-2019 дата публикации

FATTY ACID CONJUGATED NANOPARTICLES AND USES THEREOF

Номер: US20190029970A1
Автор: LEE Wai Yip, Li Ho Yin
Принадлежит:

The present invention provides fatty acid-conjugated nanoparticles and methods of making and using the same. Methods for improving delivery of therapeutic agents (e.g., drugs) contained within the fatty acid conjugated nanoparticles to the central nervous system (e.g., across the blood brain barrier) are disclosed. 1. A nanoparticle comprising a fatty acid conjugated to the surface of the nanoparticle and containing within the nanoparticle a therapeutic agent.2. The nanoparticle of claim 1 , wherein the fatty acid is selected from the group consisting of lauric acid (C12) claim 1 , myristic acid (C14) claim 1 , palmitic acid (C16) claim 1 , steric acid (C18) claim 1 , alpha-linolenic acid (ALA) claim 1 , linoleic acid (LA) claim 1 , oleic acid (OA) claim 1 , docosahexaenoic acid (DHA) claim 1 , erucic acid (EA) claim 1 , formic acid claim 1 , acetic acid claim 1 , propionic acid claim 1 , butyric acid claim 1 , isobutyric acid claim 1 , valeric acid claim 1 , isovaleric acid claim 1 , and derivatives that contain one long alkyl chain in which the number of carbon varies from 2 to 5 claim 1 , crotonic acid claim 1 , myristoleic acid claim 1 , palmitoleic acid claim 1 , sapienic acid claim 1 , oleic acid claim 1 , elaidic acid claim 1 , vaccenic acid claim 1 , gadoleic acid claim 1 , eicosenoic acid claim 1 , erucic acid claim 1 , nervonic acid claim 1 , linoleic acid claim 1 , eicosadienoic acid claim 1 , docosadienoic acid claim 1 , linolenic acid claim 1 , pinolenic acid claim 1 , eleostearic acid claim 1 , mead acid claim 1 , stearidonic acid claim 1 , arachidonic acid and derivatives that contain one long alkyl chain in which the number of carbon varies from 6 to 12 claim 1 , oxalic acid claim 1 , malonic acid claim 1 , succinic acid claim 1 , glutaric acid claim 1 , adipic acid claim 1 , pimelic acid claim 1 , suberic acid claim 1 , azelaic acid claim 1 , sebacic acid and derivatives that contain one long alkyl chain in which the number of carbon varies from 8 ...

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Номер записи: 84
04-02-2021 дата публикации

COATED BIOLOGICAL COMPOSITION

Номер: US20210030688A1
Автор: ANDERSON TRACY SCOTT, Ganey Timothy
Принадлежит:

A coated biological composition has a mixture of biologic material and a volume of a liquid protectant. The mixture of biologic material has non-whole cellular components or whole cells or combinations of the non-whole cellular components and whole cells, wherein the mixture is compatible with biologic function. The volume of a liquid protectant is intermixed with the mixture of biologic material, wherein the liquid protectant forms a coating externally enveloping each of the non-whole cellular components, if any, and each of the whole cells, if any, of the mixture of biologic material, to form the coated biological composition. The coated biological composition is frozen and thereafter thawed and then frozen a second time for storage or frozen at least once and thawed and stored under refrigeration above freezing, or frozen and thawed and then concentrated by drying, or while frozen without thawing lyophilized for ambient or room temperature storage. 1. A method of making a coated biological composition comprises the steps of:collecting, recovering and processing bone marrow from a cadaver donor;mechanically separating cellular and non-cellular components of bone marrow from cadaverous bone;concentrating by centrifugation and filtering;separation by density gradient centrifugation;collecting non-cellular fractions or non-cellular components or combinations thereof of predetermined density;washing the non-cellular fractions or non-cellular components or combinations thereof to create a mixture;quantifying non-whole cell fraction concentration exceeds zero;suspending the mixture to a predetermined concentration in a liquid protectant to coat the mixture and form the coated biological composition;freezing the suspended mixture at a predetermined controlled rate; andthereafter thawing and then freezing a second time for storage or frozen at least once thawed and stored under refrigeration above freezing, or frozen and thawed and then concentrated by drying, or while ...

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Номер записи: 85
31-01-2019 дата публикации

NON-LIPOSOMAL SYSTEMS FOR NUCLEIC ACID DELIVERY

Номер: US20190032051A1
Автор: JEFFS LLOYD B., PALMER LORNE R., Yaworski Ed
Принадлежит:

The present invention provides novel, stable lipid particles having a non-lamellar structure and comprising one or more active agents or therapeutic agents, methods of making such lipid particles, and methods of delivering and/or administering such lipid particles. More particularly, the present invention provides stable nucleic acid-lipid particles (SNALP) that have a non-lamellar structure and that comprise a nucleic acid (such as one or more interfering RNA), methods of making the SNALP, and methods of delivering and/or administering the SNALP. 1. A composition comprising:a plurality of nucleic acid-lipid particles, wherein each particle in the plurality of particles comprises:(a) a nucleic acid;(b) a cationic lipid comprising from about 50 mol % to about 85 mol % of the total lipid present in the particle;(c) a non-cationic lipid comprising from about 13 mol % to about 49.5 mol % of the total lipid present in the particle; and(d) a conjugated lipid that inhibits aggregation of particles comprising from about 0.5 mol % to about 10 mol % of the total lipid present in the particle,wherein at least about 95% of the particles in the plurality of particles have a non-lamellar morphology.2. The composition of claim 1 , wherein the nucleic acid is an interfering RNA selected from the group consisting of siRNA claim 1 , aiRNA claim 1 , miRNA claim 1 , Dicer-substrate dsRNA claim 1 , shRNA claim 1 , ssRNAi oligonucleotides claim 1 , and combinations thereof.3. The composition of claim 2 , wherein the interfering RNA is an siRNA.4. The composition of claim 3 , wherein the siRNA comprises from about 15 to about 60 nucleotides.5. The composition of claim 3 , wherein one or more of the nucleotides in the double-stranded region of the siRNA comprise modified nucleotides.6. The composition of claim 5 , wherein the modified nucleotides comprise 2′-O-methyl (2′OMe) nucleotides.7. The composition of claim 5 , wherein less than about 50% of the nucleotides in the double-stranded ...

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Номер записи: 86
09-02-2017 дата публикации

STABILIZED HIGH DRUG LOAD NANOCARRIERS, METHODS FOR THEIR PREPARATION AND USE THEREOF

Номер: US20170035701A1
Автор: HO HSIU-O, HO YUAN SOON, LIU Jun-Jen, SHEN SHING CHUAN, Sheu Ming-Thau
Принадлежит:

The present invention relates to generally to pharmaceutical formulations. Particularly, the present invention relates to a drug nanocarrier that is stabilized by lipids, preferably lecithins and/or lipid-terminated polyalkylene glycol, for the delivery of poorly soluble drugs with high drug loading and its utility in the fields of pharmaceutical formulation, drug delivery, medicine and diagnosis. 1. A nanocarrier comprising a lipid shell enclosing a micellar core encapsulating an active agent or a diagnostic agent , wherein the lipid shell comprises one or more amphiphilic lipids , and the micellar core comprises one or more amphiphilic polymers wherein the core optionally comprises an emulsifier.2. The nanocarrier of claim 1 , wherein the diameter of the nanocarrier is in the range of about 50 nm to about 500 nm.3. The nanocarrier of claim 1 , which has an encapsulating efficiency in the range of about 50 to about 100%.4. The nanocarrier of claim 1 , wherein the amphiphilic lipid is selected from the group consisting of lipid-polyethyleneglycol conjugate claim 1 , phospholipid claim 1 , or cholesterol or a combination thereof.5. The nanocarrier of claim 4 , wherein the phospholipid is lecithin claim 4 , soybean lecithin claim 4 , egg yolk lecithin claim 4 , a synthetic phospholipid or a pegylated phospholipid.6. The nanocarrier of claim 5 , wherein the synthetic phospholipid is phosphatidylcholine claim 5 , phosphatidic acid claim 5 , phosphatidylethanolamine claim 5 , phosphatidylglycerol claim 5 , phosphatidylserine claim 5 , phosphatidylinositol claim 5 , or a combination thereof. In a further embodiment claim 5 , the amphiphilic lipid is a lipid-polyethyleneglycol conjugate claim 5 , pegylated phospholipid claim 5 , or a combination thereof.7. The nanocarrier of claim 1 , wherein the lipid shell comprises a phospholipid and another amphiphilic lipid selected from pegylated phospholipid and cholesterol.8. The nanocarrier of claim 1 , wherein the lipid shell ...

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Номер записи: 87
08-02-2018 дата публикации

NOVEL RNAi MOLECULE DELIVERY PLATFORM BASED ON SINGLE-siRNA AND shRNA NANOCAPSULES

Номер: US20180036254A1
Автор: Chen Irvin S.Y., Kamata Masakazu, Liang Min, Lu Yunfeng, Wen Jing, Yan Ming
Принадлежит:

Novel siRNA and shRNA nanocapsules and delivery methods are disclosed herein. These siRNA and shRNA nanocapsules and delivery methods are highly robust and effective. This invention provides a platform for RNAi delivery with low toxicity and long intracellular half-life for practical therapeutic applications. 1. A polymer shell comprising:a. one or more positively charged monomers selected from the group consisting of: N-(3-((4-((3-aminopropyl)amino)butyl)amino)propyl)acrylamide, N-(3-((4-((3-aminopropyl)amino)butyl)amino)propyl)methacrylamide, N-(3-((4-aminobutyl)amino)propyl)acrylamide, N-(3-((4-aminobutyl)amino)propyl)methacrylamide, N-(2-((2-aminoethyl)(methyl)amino)ethyl)acrylamide, N-(2-((2-aminoethyl)(methyl)amino)ethyl) methacrylamide, N-(piperazin-1-ylmethyl)acrylamide, N-(piperazin-1-ylmethyl)methacrylamide, N-(2-(bis(2-aminoethyl)amino)ethyl)acrylamide, N-(2-(bis(2-minoethyl)amino)ethyl)methacryl amide, (3-acrylamidopropyl) trimethylammonium hydrochloride, and 2-aminoethyl methacrylate;b. one or more crosslinkers selected from the group consisting of: 1,3-glycerol dimethacrylate, glycerol 1,3-diglycerolate diacrylate, N,N′-bis(acryloyl)cystamine, bis[2-(methacryloyloxy)ethyl] phosphate, N,N′-Methylenebisacrylamide, bisacryloylated polypeptide, andc. one or more neutral monomers selected from the group consisting of: N-(1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl)acrylamide, acrylamide, N-(hydroxymethyl)acrylamide, 2-hydroxyethyl acrylate, 2-hydroxyethyl methacrylate.2. A polymer shell according to claim 1 , wherein one or more crosslinkers comprise:a) a degradable crosslinker selected from the group consisting of: 1,3-glycerol dimethacrylate, glycerol 1,3-diglycerolate diacrylate, N,N′-bis(acryloyl)cystamine, bis[2-(methacryloyloxy)ethyl] phosphate and bisacryloylated polypeptide; andb) a non-degradable crosslinker, wherein said non-degradable cross linker is N,N′-methylenebisacrylamide,wherein the ratio of degradable crosslinker to non-degradable ...

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Номер записи: 88
08-02-2018 дата публикации

PHASE TRANSITION BIOPOLYMERS AND METHODS OF USE

Номер: US20180037609A1
Автор: Amiram Miriam, Chilkoti Ashutosh, Garcia Quiroz Felipe
Принадлежит:

The present disclosure describes environmentally responsive polypeptides capable of displaying stimuli-triggered conformational changes in a reversible or irreversible manner that may be accompanied by aggregation. Polypeptides include a number of repeated motifs and may be elastomeric or non-elastomeric. The polypeptides may be used to deliver therapeutics to a biological site and to develop bioactive polypeptides that are environmentally responsive. 1. A environmentally responsive polypeptide comprising at least ten sequences selected from VGAPVG , LGAPVG , VPSALYGVG , VGPAVG , VTPAVG , VPSDDYGQG , VPSDDYGVG , TPVAVG , VPSTDYGVG , VPAGVG , VPTGVG , VPAGLG , VPHVG , VHPGVG , VPGAVG , VPGVAG , VRPVG , GRGDSPY , GRGDSPH , GRGDSPV , GRGDSPYG , RPLGYDS , RPAGYDS , RPXGYDS , GRGDSYP , GRGDSPYQ , GRGNSPYG , GRGDAPYQ , VPXSRNGG , VPHSRNGG , VPHSRNGL , VPGHSHRDFQPVLHLVALNSPL SGGMRG , HTHQDFQPVLHLVALNTPLSGGMRGIRPGG , FEWTPGWYQPYG or a combination thereof , wherein X is from zero to four amino acid residues , and wherein the polypeptide upon stimulation undergoes a conformational change that is accompanied by aggregation.2. The polypeptide of claim 1 , wherein the at least ten sequences are consecutive.3. The polypeptide of claim 1 , further comprising a spacer sequence between at least two of the at least ten sequences.4. The polypeptide of claim 3 , wherein the spacer sequence comprises from one to twenty-six amino acids.5. The polypeptide of claim 1 , wherein the polypeptide exhibits phase separation when exposed to a threshold temperature that is (i) above a lower critical solution temperature of the polypeptide claim 1 , or (ii) below an upper critical solution temperature of the polypeptide claim 1 , or exhibits phase separation when exposed to a threshold temperature that is above the lower critical solution temperature claim 1 , and when exposed to a threshold temperature that is below the upper critical solution temperature.6. The polypeptide of claim 5 , wherein ...

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Номер записи: 89
08-02-2018 дата публикации

NOVEL LOW MOLECULAR WEIGHT CYCLIC AMINE CONTAINING CATIONIC LIPIDS FOR OLIGONUCLEOTIDE DELIVERY

Номер: US20180037893A1
Автор: Beutner Gregory L., Stanton Matthew G.
Принадлежит: Sirna Therapeutics, Inc.

The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA. 2. A lipid nanoparticle comprising a cationic lipid according to .3. The lipid nanoparticle according to further comprises an oligonucleotide.4. The lipid nanoparticle according to wherein the oligonucleotide is siRNA or miRNA.5. The lipid nanoparticle according to wherein the oligonucleotide is siRNA. This application is a Continuation of U.S. patent application Ser. No. 14/719,513 filed, May 22, 2015, which is a Continuation of U.S. patent application Ser. No. 13/883,487 filed May 3, 2013, now U.S. Pat. No. 9,0678,82 issued Jun. 30, 2015, which is 371 National Phase Entry of International Patent Application No. PCT/US2011/058498 filed on Oct. 31, 2011, which claims benefit under 35 U.S.C. § 119(e) of the U.S. Provisional Application No. 61/410,472, filed Nov. 5, 2010, the contents of each of which are incorporated herein by reference in their entirety.The instant application contains a Sequence Listing which has been submitted electronically in ASCII format and is hereby incorporated by reference in its entirety. Said ASCII copy, created on Aug. 26, 2017 is named MRLMIS00047WOPCTSEQ.txt and is 3,671 bytes.The present invention relates to novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides, to facilitate the cellular uptake and endosomal escape, and to knockdown target mRNA both in ...

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Номер записи: 90
24-02-2022 дата публикации

Methods for the preparation of biologically active compounds in nanoparticulate form

Номер: US20220054418A1
Автор: Cammarano Raffaele, Caruso Frank, Meiser Felix, Postma Almar
Принадлежит:

A method for producing a composition comprising nanoparticles of a biologically active compound. 1. A method for producing a composition comprising nanoparticles of a biologically active compound , comprising the step of:dry milling a solid biologically active compound and a millable grinding compound in a mill comprising a plurality of milling bodies, for a time period sufficient to produce a solid dispersion comprising nanoparticles of the biologically active compound dispersed in an at least partially milled grinding compound.2. The method of claim 1 , wherein the nanoparticles have an average size less than a size selected from the group consisting of 200 nm claim 1 , 100 nm claim 1 , 75 nm claim 1 , 50 nm claim 1 , and 40 nm.3. The method of claim 2 , wherein the particle size of at least 50% of the nanoparticles is within the average size range.4. The method of claim 3 , wherein the particle size of at least 75% of the nanoparticles is within the average size range.5. The method of any preceding claim claim 3 , wherein the time period is a range selected from the group consisting of between 5 minutes and 2 hours claim 3 , between 5 minutes and I hour claim 3 , between 5 minutes and 45 minutes claim 3 , between 5 minutes and 30 minutes claim 3 , and between 10 minutes and 25 minutes.6. The method of any of - claim 3 , wherein the milling medium is selected from the group consisting of ceramics claim 3 , glasses claim 3 , polymers claim 3 , ferromagnetics claim 3 , and metals.7. The method of claim 6 , wherein the milling medium is steel balls having a diameter selected from the group consisting of between 1 and 20 mm claim 6 , between 2 and 15 mm claim 6 , and between 3 and 10 mm.8. The method of any preceding claim wherein the biologically active compound is selected from the group consisting of biologics claim 6 , amino acids claim 6 , proteins claim 6 , peptides claim 6 , nucleotides claim 6 , nucleic acids claim 6 , and analogs claim 6 , homologs and first ...

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Номер записи: 91
24-02-2022 дата публикации

Drug delivery systems containing oxidized cholesterols

Номер: US20220054423A1
Автор: James DAHLMAN, Kalina PAUNOVSKA
Принадлежит: Georgia Tech Research Corp

Lipid nanoparticles and compositions thereof are disclosed herein. An exemplary nanoparticle composition includes an ionizable lipid, a phospholipid, a PEG-lipid, and a cholesterol modified with a hydroxyl group near the D-sterol ring. The disclosed nanoparticle compositions can target liver Kupffer cells and endothelial cells more preferentially than hepatocytes which should be beneficial in treating liver diseases in which dysfunctional Kupffer cells and endothelial cells are involved in disease pathogenesis.

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Номер записи: 92
24-02-2022 дата публикации

MODIFIED MRNA FOR THE TREATMENT OF PROGRESSIVE FAMILIAL INTRAHEPATIC CHOLESTASIS DISORDERS

Номер: US20220054653A1
Автор: CAO Jingsong, Martini Paolo, Presnyak Vladimir
Принадлежит: ModernaTX, Inc.

The present disclosure provides compositions of nucleic acids relating to biliary epithelial transporters. For example, the present disclosure relates to nucleic acids capable of regulating the biliary secretion of phospholipids, including phosphatidylcholine, e.g., those encoded by ATP binding cassette subfamily B member 4 (ABCB4) or a biologically active fragment thereof, in a target cell. In a preferred embodiment, the present disclosure provides compositions comprising modified mRNA encoding ABCB4 formulated in a lipid nanoparticle (LNP) carrier and derivative constructs, which are useful for treating or preventing progressive familial intrahepatic cholestasis type 3 (PFIC3). 1. A composition comprising a modified polynucleotide having an open reading frame (ORF) encoding ATP binding cassette subfamily B member 4 (ABCB4) formulated in a lipid nanoparticle (LNP) carrier.2. The composition of claim 1 , wherein the ABCB4 polynucleotide comprises at least one chemically modified nucleobase claim 1 , sugar claim 1 , backbone claim 1 , or any combination thereof3. The composition of - claim 1 , wherein the modified polynucleotide comprises at least one modified nucleoside.4. The composition of claim 2 , wherein the at least one modified nucleoside is selected from the group consisting of: pseudouridine claim 2 , 1-methyl-pseudouridine claim 2 , 5-methylcytidine claim 2 , 5-methyluridine claim 2 , 2′-O-methyluridine claim 2 , 2-thiouridine claim 2 , 5-methoxyuridine and N6-methyladenosine.5. The composition of claim 3 , wherein the at least one modified nucleoside is a 5-methoxyuridine.6. The composition of claim 4 , wherein at least 30% of the uridine residues are 5-methoxyuridines.7. The composition of any of the preceding claims claim 4 , wherein the modified polynucleotide comprises a poly-A region claim 4 , a Kozak sequence claim 4 , a 3′ untranslated region claim 4 , a 5′ untranslated region claim 4 , an miRNA binding site claim 4 , or any combination thereof.8. ...

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Номер записи: 93
18-02-2021 дата публикации

NANOSTRUCTURED FORMULATIONS FOR THE DELIVERY OF SILIBININ AND OTHER ACTIVE INGREDIENTS FOR TREATING OCULAR DISEASES

Номер: US20210046083A1
Автор: "BONDI Maria Luisa", BLANCO Anna Rita, CAVALLARO Gennara, CEIDDA Irene, CONSOLI Grazia Maria Letizia, CRAPARO Emanuela Fabiola, Cuzzocrea Salvatore, ESPOSITO Emanuela, GIAMMONA Gaetano, GRANATA Guiseppe, GUARNERI Patrizia, LA MARCA Clara, LICCIARDI Mariano, PAPASERGI Salvatore, PITARRESI Giovanna, SALADINO Patrizia, VIOLA Santa
Принадлежит:

Formulations are described, containing silibinin or other active ingredients incorporated in lipid nanoparticle systems of the SLN and NLC type, and based on calixarenes, possibly mucoadhesive, or in micellar and nanoparticle systems based on amphiphilic inulin copolymers for use in the treatment of neurodegenerative ocular diseases. The versatility of the calixarene compound is also described, capable of charging and releasing active ingredients characterized by low water solubility, easy chemical and enzymatic degradation, low bioavailability, either of natural origin or not, to be used in the treatment of ocular diseases. 1. A method for the treatment of ocular diseases comprising the topical application of formulations comprising silibinin or sorafenib or curcumin incorporated in calixarene-based nanostructured systems.3. The method of claim 1 , wherein said calixarene-based nanostructured systems have an average diameter in the range between 50 and 200 nm with a polydispersity index below 0.5.4. The method of claim 1 , wherein said systems incorporate an amount in the range between 1 and 15% w/w of silibinin or sorafenib or curcumin.5. The method of claim 1 , wherein said ocular diseases are neurodegenerative ocular diseases.6. The method of claim 5 , wherein said neurodegenerative ocular diseases are selected from: choroidal neovascularization (CNV) claim 5 , age-related macular degeneration (AMD) claim 5 , macular edema claim 5 , neovascular glaucoma claim 5 , macular edema claim 5 , retinopathy of prematurity (ROP) claim 5 , diabetic retinopathy (DR) claim 5 , uveitis claim 5 , endophthalmitis claim 5 , retinitis claim 5 , choroiditis claim 5 , chorioretinitis claim 5 , retinal complications of systemic diseases. This application is a divisional of prior filed U.S. application Ser. No. 15/517,018, filed Apr. 5, 2017, which is the U.S. National Stage of International Application No. PCT/IB2015/057732, filed Oct. 9, 2015, which designated the United States and ...

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Номер записи: 94
16-02-2017 дата публикации

Co-encapsulation of antimicrobials and adjuvants in nanocarriers

Номер: US20170042823A1
Автор: Hoang D. Lu, Robert K. Prud'homme
Принадлежит: PRINCETON UNIVERSITY

Microbial infections have become increasingly difficult to treat due to the emergence of drug resistant microbes. Adjunctive therapies can be used to better treat resistant microbes, where multiple drugs are concurrently used to overcome resistant mechanisms and to synergistically treat infections. The practice of adjunctive therapies is limited by the ability to precisely control the pharmacokinetic profiles of the multiple actives. Composite particle-based approaches to enable and enhance adjunctive antimicrobial infections by simultaneous encapsulation and delivery of all components are described herein.

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Номер записи: 95
16-02-2017 дата публикации

GM3 FUNCTIONALIZED NANOPARTICLES

Номер: US20170042824A1
Автор: Gummuluru Suryaram, Reinhard Bjoern Markus
Принадлежит: TRUSTEES OF BOSTON UNIVERSITY

Embodiments disclosed herein relates to ganglioside GM3-containing mixed lipids nanoparticles having an overall size between 60-100 nm, the making thereof and the uses. The nanoparticles selectively targeted to CD169+ expressing cells such as dendritic cells and macrophage. The nano-particles are endocytosed by the CD169+ expressing cells. 1. A nanoparticle comprising:a) a core having a largest diameter between 50-90 nm;b) a coating layer encasing the core; andc) a ganglioside GM3-containing mixed lipid layer comprising of dipalmitoylphosphatidylcholine (DPPC), cholesterol, phosphatidylserine (PS), and aNeu5Ac(2-3)bDGalp(1-4)bDGlcp(1-1)Cer (GM3);wherein the ganglioside GM3-mixed lipid layer is exterior of the coating layer and is integrated into the coating layer, and wherein the nanoparticles have an overall particle size between 60-100 nm.2. The nanoparticle of claim 1 , wherein the core is a solid core.3. The nanoparticle of claim 1 , wherein the core is has a shape that is selected from the group consisting of ellipsoid claim 1 , spherical claim 1 , rod-like claim 1 , octahedral claim 1 , and cube-like.4. The nanoparticle of claim 1 , wherein the core comprises a material selected from the group consisting of gold claim 1 , silver claim 1 , a gold alloy claim 1 , a silver alloy claim 1 , silica claim 1 , mesoporous silica claim 1 , polystyrene claim 1 , and titania.5. The nanoparticle of claim 1 , wherein the coating layer is a thiolated lipid claim 1 , a silane with long alkyl chains claim 1 , or polyethylene glycol thiol.610.-. (canceled)11. The nanoparticle of claim 1 , wherein the ganglioside GM3 containing mixed lipid layer consists of 40%-60% of DPPC.12. The nanoparticle of claim 1 , wherein the ganglioside GM3 containing mixed lipid layer consists of 40%-60% of cholesterol.13. The nanoparticle of claim 1 , wherein the ganglioside GM3 containing mixed lipid layer consists of 0.5%-5% of PS.14. The nanoparticle of claim 1 , wherein the ganglioside GM3 ...

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Номер записи: 96
16-02-2017 дата публикации

LIPID NANO PARTICLES COMPRISING CATIONIC LIPID FOR DRUG DELIVERY SYSTEM

Номер: US20170042825A1
Автор: Era Tomohiro, Kuboyama Takeshi, Naoi Tomoyuki
Принадлежит:

The present invention provides a lipid nano-particles, which allow nucleic acids to be easily introduced into cells, comprising a cationic lipid represented by formula (I) 120-. (canceled)22. The lipid nano particles for drug delivery according to claim 21 , wherein Rand Rare dodecyl claim 21 , tetradecyl claim 21 , (Z)-dodec-7-enyl claim 21 , (Z)-tetradec-7-enyl claim 21 , (Z)-hexadec-4-enyl claim 21 , (Z)-hexadec-7-enyl claim 21 , (E)-hexadec-7-enyl claim 21 , (Z)-hexadec-9-enyl claim 21 , (7Z claim 21 ,10Z)-hexadec-7 claim 21 ,10-dienyl claim 21 , (7Z claim 21 ,10Z claim 21 ,13Z)-hexadec-7 claim 21 ,10 claim 21 ,13-trienyl claim 21 , (Z)-octadec-9-enyl or (9Z claim 21 ,12Z)-octadec-9 claim 21 ,12-dienyl.23. The lipid nano particles for drug delivery according to claim 21 , wherein Rand Rare tetradecyl claim 21 , hexadecyl claim 21 , (Z)-tetradec-9-enyl claim 21 , (Z)-hexadec-9-enyl claim 21 , (Z)-octadec-6-enyl claim 21 , (Z)-octadec-9-enyl claim 21 , (E)-octadec-9-enyl claim 21 , (Z)-octadec-11-enyl claim 21 , (9Z claim 21 ,12Z)-octadeca-9 claim 21 ,12-dienyl claim 21 , (9Z claim 21 ,12Z claim 21 ,15Z)-octadeca-9 claim 21 ,12 claim 21 ,15-trienyl claim 21 , (Z)-icos-11-enyl or (11Z claim 21 ,14Z)-icosa-11 claim 21 ,14-dienyl.24. The lipid nano particles for drug delivery according to claim 21 , wherein Ris a hydrogen atom claim 21 , methyl claim 21 , pyrrolidin-3-yl claim 21 , piperidin-3-yl claim 21 , piperidin-4-yl claim 21 , or alkyl having a carbon number of from 1 to 6 or alkenyl having a carbon number of from 3 to 6 claim 21 , each substituted with 1 to 3 substituent(s) claim 21 , which is(are) claim 21 , the same or different claim 21 , amino claim 21 , monoalkylamino claim 21 , dialkylamino claim 21 , trialkylammonio claim 21 , hydroxy claim 21 , alkoxy claim 21 , carbamoyl claim 21 , monoalkylcarbamoyl claim 21 , dialkylcarbamoyl claim 21 , pyrrolidinyl claim 21 , piperidyl or morpholinyl.25. The lipid nano particles for drug delivery according to claim ...

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Номер записи: 97
16-02-2017 дата публикации

NANOLIPIDIC PARTICLE ASSEMBLY POPULATIONS

Номер: US20170042826A1
Автор: Fountain Michael W.
Принадлежит: DERMAZONE SOLUTIONS, INC.

Nanolipidic Particles (NLPs) having average mean diameters of 1 nm to 20 nm are made from a precursor solution. NLPs can be loaded with a desired passenger molecule. Assemblies of these particles, called NLP assemblies, result in a vehicle population of a desired size. Single application or multifunction NLP assemblies are made from the loaded NLPs and range in size from about 30 to about 200 nm. A method of using preloaded NLPs to make larger carrier vehicles or a mixed population provides increased encapsulation efficiency. NLPs have application in the cosmetics, pharmaceutical, and food and beverage industries. 1. An NLP (Nanolipidic Particle) assembly population comprising:nanolipidic particles (NLPs), said nanolipidic particles formed from a hydrous monophasic precursor solution having phospholipids, a first concentration of aqueous solvent and a first concentration of non-aqueous solvent selected from the group consisting of ethanol, 1-propanol, and 2-propanol;said hydrous monophasic precursor solution having been diluted by one or more dilution of a second concentration non-aqueous solvent resulting in a solvent-diluted precursor; andsaid solvent-diluted precursor having been diluted with a second concentration of aqueous solvent;wherein the dilution with said second concentration of aqueous solvent results in formation of one or more NLP assembly having a mean size from about 30 nm to about 200 nm, said nanolipidic particles in said assembly having a mean size of about 1 nm to about 20 nm and retaining a concentration of said non-aqueous solvent from about 0.5% to 14%.2. The NLP assembly population of claim 1 , wherein the mean size of said assembly is from about 80 nm to about 110 nm.3. The NLP assembly population of claim 1 , wherein the mean size of said assembly is from about 110 nm to about 140 nm.4. The NLP assembly population of claim 1 , wherein the mean size of said assembly is from about 150 nm to about 200 nm.5. The NLP assembly population of ...

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Номер записи: 98
16-02-2017 дата публикации

Therapeutic nanoparticles comprising a therapeutic agent and methods of making and using same

Номер: US20170042828A1
Автор: Christina Van Geen Hoven, David Dewitt, Erick Peeke, Greg Troiano, Hong Wang, James Wright, Maria Figueiredo, Young-Ho Song
Принадлежит: PFIZER INC

The present disclosure generally relates to nanoparticles comprising a substantially hydrophobic acid, a basic therapeutic agent having a protonatable nitrogen, and a polymer. Other aspects include methods of making and using such nanoparticles.

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Номер записи: 99
03-03-2022 дата публикации

OCULAR LENS, PHARMACEUTICAL COMPOSITION, AND USES THEREOF

Номер: US20220062169A1
Автор: CHANG Hong-Shong, CHEN Yun-Yu, Cherng Juin-Hong, LAI Wei-Chung, Li Kuan-Jung
Принадлежит: GoldRed Nanobiotech CO., LTD.

Disclosed herein are an ocular lens and a pharmaceutical composition. The ocular lens of the present disclosure is characterized in having a dihydrolipoic acid (DHLA) coated gold nanoclusters absorbed thereon. The pharmaceutical composition of the present disclosure comprises a DHLA coated gold nanocluster, and a pharmaceutically acceptable excipient. According to some embodiments of the present disclosure, the DHLA coated gold nanoclusters are capable of reducing intracellular ROS levels, promoting tissue repair, and inhibiting pathological angiogenesis. Accordingly, also disclosed herein are methods of treating ocular conditions by uses of the present contact lens or pharmaceutical composition.

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Номер записи: 100