LIPID-BASED NANOPARTICLES

Lipid-based nanoparticle compositions are provided. The compositions generally comprise lipid-hydrophilic polymer-amyloid binding ligand conjugates, and may be liposomal compositions. The compositions, including the liposomal compositions, may be useful for imaging and/or the treatment of amyloid-β plaque deposits characteristic of Alzheimer's Disease.

Lipid-Based Nanoparticles

Lipid-based nanoparticle compositions are provided. The compositions generally comprise lipid-hydrophilic polymer-amyloid binding ligand conjugates, and may be liposomal compositions. The compositions, including the liposomal compositions, may be useful for imaging and/or the treatment of amyloid-β plaque deposits characteristic of Alzheimer's Disease.

MRI IMAGING OF AMYLOID PLAQUE USING LIPOSOMES

Provided are aromatic compounds, phospholipid-polymer-aromatic conjugates comprising the aromatic compounds, and liposome compositions including the phospholipid-polymer-aromatic conjugates. The liposomal compositions may be useful for imaging of Alzheimer's Disease, for example, imaging of the amyloid-β plaque deposits characteristic of Alzheimer's Disease. 1. A liposomal composition , comprising: {'br': None, 'sup': '1', '—X—Ar—R-Het\u2003\u2003(I)'}, 'a phospholipid-polymer-aromatic conjugate, the aromatic moiety in the phospholipid-polymer-aromatic conjugate being represented by Structural Formula I, 'a membrane, comprising [{'sup': 2', '2', '3, 'X is —R—O— or —R—N(R)—;'}, {'sup': '1', 'sub': 2', '6, 'Ris C-Calkyl or alkenyl;'}, {'sup': '2', 'Ris a linking group comprising 1 to 6 carbon atoms that is one of: alkylene or alkoxyalkylene;'}, {'sup': '3', 'sub': 1', '6', '1', '6, 'Ris hydrogen, C-Calkyl, or C-Calkoxyalkyl;'}, 'Ar is a monocyclic or polycyclic group comprising at least one aromatic or heteroaromatic ring;', 'Het is a monocyclic or polycyclic group comprising at least one heteroaromatic ring;', {'sup': '2', 'sub': 1', '6', '1', '6, 'Ris substituted with zero, one or more of: hydroxyl, C-Calkyl, and C-Chydroxyalkyl; and'}, {'sup': 1', '3, 'sub': 1-6', '2, 'Ar, Het, R, and Rother than hydrogen are independently substituted with zero, one or more of: halogen; —OH; alkyl, —O-alkyl, aryl, —O-aryl or —(O-alkylene)optionally substituted with —OH or halogen; —NH; —NH-alkyl; —N-dialkyl; carboxyl; sulfonyl; carbamoyl; and glycosyl.'}], 'wherein8. The liposomal composition of claim 1 , further comprising a nonradioactive magnetic resonance imaging (MRI) contrast enhancing agent that is at least one of encapsulated by or bound to the membrane.9. The liposomal composition of claim 1 , the membrane further comprising a first phospholipid and a second phospholipid claim 1 , the second phospholipid being derivatized with a hydrophilic polymer.11. A method for imaging ...

MRI IMAGING OF AMYLOID PLAQUE USING LIPOSOMES

Provided are aromatic compounds, phospholipid-polymer-aromatic conjugates comprising the aromatic compounds, and liposome compositions including the phospholipid-polymer-aromatic conjugates. The liposomal compositions may be useful for imaging of Alzheimer's Disease, for example, imaging of the amyloid-β plaque deposits characteristic of Alzheimer's Disease. 1. A liposomal composition , comprising: {'br': None, 'sup': '1', '—X—Ar—R-Het\u2003\u2003(I)'}, 'a phospholipid-polymer-aromatic conjugate, the aromatic moiety in the phospholipid-polymer-aromatic conjugate being represented by Structural Formula I, 'a membrane, comprising [{'sup': 2', '2', '3, 'X is —R—O— or —R—N(R)—;'}, {'sup': '1', 'sub': 2', '6, 'Ris C-Calkyl or alkenyl;'}, {'sup': '2', 'Ris a linking group comprising 1 to 6 carbon atoms that is one of: alkylene or alkoxyalkylene;'}, {'sup': '3', 'sub': 1', '6', '1', '6, 'Ris hydrogen, C-Calkyl, or C-Calkoxyalkyl;'}, 'Ar is a monocyclic or polycyclic group comprising at least one aromatic or heteroaromatic ring;', 'Het is a monocyclic or polycyclic group comprising at least one heteroaromatic ring;', {'sup': '2', 'sub': 1', '6', '1', '6, 'Ris substituted with zero, one or more of: hydroxyl, C-Calkyl, and C-Chydroxyalkyl; and'}, {'sup': 1', '3, 'sub': 1-6', '2, 'Ar, Het, R, and Rother than hydrogen are independently substituted with zero, one or more of: halogen; —OH; alkyl, —O-alkyl, aryl, —O-aryl or —(O-alkylene)optionally substituted with —OH or halogen; —NH; —NH— alkyl; —N— dialkyl; carboxyl; sulfonyl; carbamoyl; and glycosyl.'}], 'wherein8. The liposomal composition of claim 1 , further comprising a nonradioactive magnetic resonance imaging (MRI) contrast enhancing agent that is at least one of encapsulated by or bound to the membrane.9. The liposomal composition of claim 1 , the membrane further comprising a first phospholipid and a second phospholipid claim 1 , the second phospholipid being derivatized with a hydrophilic polymer.11. A method for ...

MRI Imaging of Amyloid Plaque Using Liposomes

Provided are aromatic compounds, phospholipid-polymer-aromatic conjugates comprising the aromatic compounds, and liposome compositions including the phospholipid-polymer-aromatic conjugates. The liposomal compositions may be useful for imaging of Alzheimer's Disease, for example, imaging of the amyloid-β plaque deposits characteristic of Alzheimer's Disease. 1. A liposomal composition , comprising: {'br': None, 'sup': '1', '—X—Ar—R-Het \u2003\u2003(I)'}, 'a phospholipid-polymer-aromatic conjugate, the aromatic moiety in the phospholipid-polymer-aromatic conjugate being represented by Structural Formula I, 'a membrane, comprising [{'sup': 2', '2', '3, 'X is —R—O— or —R—N(R)—;'}, {'sup': '1', 'sub': 2', '6, 'Ris C-Calkyl or alkenyl;'}, {'sup': '2', 'Ris a linking group comprising 1 to 6 carbon atoms that is one of: alkylene or alkoxyalkylene;'}, {'sup': '3', 'sub': 1', '6', '1', '6, 'Ris hydrogen, C-Calkyl, or C-Calkoxyalkyl;'}, 'Ar is a monocyclic or polycyclic group comprising at least one aromatic or heteroaromatic ring;', 'Het is a monocyclic or polycyclic group comprising at least one heteroaromatic ring;', {'sup': '2', 'sub': 1', '6', '1', '6, 'Ris substituted with zero, one or more of: hydroxyl, C-Calkyl, and C-Chydroxyalkyl; and'}, {'sup': 1', '3, 'sub': 1-6', '2, 'Ar, Het, R, and Rother than hydrogen are independently substituted with zero, one or more of: halogen; —OH; alkyl, —O-alkyl, aryl, —O-aryl or —(O-alkylene)optionally substituted with —OH or halogen; —NH; —NH-alkyl; —N-dialkyl; carboxyl; sulfonyl; carbamoyl; and glycosyl.'}], 'wherein8. The liposomal composition of claim 1 , further comprising a nonradioactive magnetic resonance imaging (MRI) contrast enhancing agent that is at least one of encapsulated by or bound to the membrane.9. The liposomal composition of claim 1 , the membrane further comprising a first phospholipid and a second phospholipid claim 1 , the second phospholipid being derivatized with a hydrophilic polymer.11. A method for ...

TARGETED CONTRAST AGENTS FOR MRI OF ALPHA-SYNUCLEIN DEPOSITION

A liposomal composition (“ADx-003”) is provided, ADx-003 comprising a first phospholipid; a sterically bulky excipient that is capable of stabilizing the liposomal composition; a second phospholipid that is derivatized with a first polymer; a macrocyclic gadolinium-based imaging agent; and a third phospholipid that is derivatized with a second polymer, the second polymer being conjugated to a targeting ligand, the targeting ligand being represented by Formula I: 10. The liposomal composition of claim 9 , wherein the first phospholipid comprises hydrogenated soy L-α-phosphatidylcholine (“HSPC”).11. The liposomal composition of claim 9 , wherein the sterically bulky excipient that is capable of stabilizing the liposomal composition comprises cholesterol (“Chol”).12. The liposomal composition of claim 9 , wherein the second phospholipid that is derivatized with a first polymer comprises 1 claim 9 ,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-(methoxy (polyethylene glycol)-2000) (“DSPE-mPEG2000”).15. The liposomal composition of claim 14 , wherein the variable x is 16 (the conjugate: “Gd(III)-DOTA-DSPE”). This application is a continuation in part of U.S. patent application Ser. No. 17/175,359, filed on Feb. 12, 2021, which claims the benefit of U.S. Provisional Patent Application No. 62/975,265, filed on Feb. 12, 2020. This application also claims the benefit of U.S. Provisional Patent Application No. 63/184,675, filed on May 5, 2021. Each of these applications is incorporated by reference herein in its entirety.Neurodegenerative disorders such as Parkinson's disease (“PD”) and Alzheimer's disease (“AD”) are characterized by pathological deposits of misfolded protein aggregates at different locations in the brain. These misfolded protein aggregates include alpha-synuclein (“α-syn”) aggregates in the form of Lewy bodies (“LB”) and Lewy neurites (“LN”) in PD and amyloid-beta (“Aβ”) plaques and hyperphosphorylated tau tangles in AD. PD is the second most common ...

Targeted contrast agents for mri of amyloid deposition

A liposomal composition (“ADx-001”) is provided, ADx-001 comprising a first phospholipid; a sterically bulky excipient that is capable of stabilizing the liposomal composition; a second phospholipid that is derivatized with a first polymer; a macrocyclic gadolinium-based imaging agent; and a third phospholipid that is derivatized with a second polymer, the second polymer being conjugated to a targeting ligand. The macrocyclic gadolinium-based imaging agent may be conjugated to a fourth phospholipid.

MRI IMAGING OF AMYLOID PLAQUE USING LIPOSOMES

Provided are aromatic compounds, phospholipid-polymer-aromatic conjugates comprising the aromatic compounds, and liposome compositions including the phospholipid-polymer-aromatic conjugates. The liposomal compositions may be useful for imaging of Alzheimer's Disease, for example, imaging of the amyloid-β plaque deposits characteristic of Alzheimer's Disease. 35-. (canceled)8. The liposomal composition of claim 1 , further comprising a nonradioactive magnetic resonance imaging (MRI) contrast enhancing agent that is at least one of encapsulated by or bound to the membrane.9. The liposomal composition of claim 1 , the membrane further comprising a first phospholipid and a second phospholipid claim 1 , the second phospholipid being derivatized with a hydrophilic polymer.12. The method of claim 11 , the detecting comprising detecting using magnetic resonance imaging.13. The method of claim 11 , the nonradioactive magnetic resonance imaging (MRI) contrast enhancing agent being encapsulated by and bound to the membrane.14. The method of claim 13 , the liposomal composition characterized by per-particle relaxivity in mM-s-of at least about one or more of about: 100 claim 13 ,000 claim 13 , 125 claim 13 ,000 claim 13 , 150 claim 13 , 000 claim 13 , 165 claim 13 ,000 claim 13 , 180 claim 13 ,000 claim 13 , 190 claim 13 ,000 claim 13 , and 200 claim 13 ,000.17. The method of claim 11 , further comprising diagnosing the patient with Alzheimer's disease according to detecting the liposomal composition associated with the one or more amyloid deposits.18. The method of claim 11 , further comprising:identifying the patient as potentially having Alzheimer's disease according to detecting the liposomal composition associated with the one or more amyloid deposits;subjecting the patient to an analysis for tau neurofibrillary tangles; andupon determining the presence of tau neurofibrillary tangles in conjunction with detecting the liposomal composition associated with the one or more ...

Targeted contrast agents for mri of amyloid deposition

A liposomal composition (“ADx-001”) is provided, ADx-001 comprising a first phospholipid; a sterically bulky excipient that is capable of stabilizing the liposomal composition; a second phospholipid that is derivatized with a first polymer; a macrocyclic gadolinium-based imaging agent; and a third phospholipid that is derivatized with a second polymer, the second polymer being conjugated to a targeting ligand. The macrocyclic gadolinium-based imaging agent may be conjugated to a fourth phospholipid.

TARGETED CONTRAST AGENTS FOR MRI OF ALPHA-SYNUCLEIN DEPOSITION

A liposomal composition (“ADx-003”) is provided, ADx-003 comprising a first phospholipid; a sterically bulky excipient that is capable of stabilizing the liposomal composition; a second phospholipid that is derivatized with a first polymer; a macrocyclic gadolinium-based imaging agent; and a third phospholipid that is derivatized with a second polymer, the second polymer being conjugated to a targeting ligand, the targeting ligand being represented by Formula I: 10. The liposomal composition of claim 9 , wherein the first phospholipid comprises hydrogenated soy L-α-phosphatidylcholine (“HSPC”).11. The liposomal composition of claim 9 , wherein the sterically bulky excipient that is capable of stabilizing the liposomal composition comprises cholesterol (“Chol”).12. The liposomal composition of claim 9 , wherein the second phospholipid that is derivatized with a first polymer comprises 1 claim 9 ,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-(methoxy (polyethylene glycol)-2000) (“DSPE-mPEG2000”).15. The liposomal composition of claim 14 , wherein the variable x is 16 (the conjugate: “Gd(III)-DOTA-DSPE”). This application claims priority from U.S. Provisional Patent Application No. 62/975,265, filed on Feb. 12, 2020, which is incorporated by reference herein in its entirety.Neurodegenerative disorders such as Parkinson's disease (“PD”) and Alzheimer's disease (“AD”) are characterized by pathological deposits of misfolded protein aggregates at different locations in the brain. These misfolded protein aggregates include alpha-synuclein (“α-syn”) aggregates in the form of Lewy bodies (“LB”) and Lewy neurites (“LN”) in PD and amyloid-beta (“Aβ”) plaques and hyperphosphorylated tau tangles in AD. PD is the second most common neurodegenerative disease after AD and is characterized clinically by motor symptoms, including bradykinesia, rigidity, tremor, and postural instability. The motor symptoms are caused by degeneration of dopaminergic neurons in the substantia nigra, ...

FUNCTIONALIZED LIPOSOMES FOR IMAGING MISFOLDED PROTEINS

Phospholipid-polymer-aromatic conjugates comprising binding ligands, liposome compositions including the phospholipid-polymer-aromatic conjugates, and binding ligands having an affinity for misfolded proteins are described. The phospholipid-polymer-aromatic conjugate may be represented by Structural Formula I: PL-AL-HP-X-BL (I). In Formula I, PL is a phospholipid, AL is an aliphatic linkage, HP is hydrophilic polymer, X is a link between the phospholipid-polymer and the binding ligand, and BL is polycyclic aromatic compound that functions as a binding ligand. The liposomal compositions may be useful for the imaging of misfolded and/or aggregated proteins. 2. The composition of claim 1 , A being one of: thienylene claim 1 , vinylene-thienylene claim 1 , thienylene-vinylene claim 1 , or vinylene-thienylene-vinylene claim 1 , substituted with 0 claim 1 , 1 claim 1 , or 2 of R.3. The composition of claim 1 , wherein:n is 1 to 4;each p is independently 0 or 1;each A is thienylene, phenylene, or ethylenedioxythienylene;{'sup': '3', 'each A is substituted with 0, 1, or 2 R;'}{'sup': '1', 'each Ris independently selected from H, phenyl; and thienyl; and'}{'sup': 1', '4, 'each Ris substituted with 0 or 1 R.'}4. The composition of claim 1 , R claim 1 , R claim 1 , and Reach being independently substituted with zero claim 1 , one or more of: F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , alkyl claim 1 , aryl claim 1 , —OH claim 1 , —O-alkyl claim 1 , —O-aryl claim 1 , —NH claim 1 , —NH-alkyl claim 1 , —N— dialkyl claim 1 , carboxyl claim 1 , sulfonyl claim 1 , carbamoyl claim 1 , and glycosyl.5. The composition of claim 1 , wherein X is —O— or —R—O—.6. The composition of claim 1 , each R claim 1 , Rand Rbeing independently selected from halogen claim 1 , alkoxy claim 1 , carboxy claim 1 , carboxyalkyl claim 1 , alkoxycarbonylalkyl claim 1 , aminoalkyl claim 1 , diaminoalkoxy claim 1 , (amino) (carboxy)alkoxyalkyl claim 1 , (alkylamino) (carboxy)alkoxyalkyl claim 1 , ( ...

Mri imaging of amyloid plaque using liposomes

Provided are aromatic compounds, phospholipid-polymer-aromatic conjugates comprising the aromatic compounds, and liposome compositions including the phospholipid- polymer-aromatic conjugates. The liposomal compositions may be useful for imaging of Alzheimer's Disease, for example, imaging of the amyloid-ß plaque deposits characteristic of Alzheimer's Disease.

Lipid-based nanoparticles.

Se proporcionan composiciones de nanopartículas basadas en lípidos. Las composiciones generalmente comprenden conjugados de ligando de unión a amiloide con polímero hidrofílico y lípido, y pueden ser composiciones liposómicas. Las composiciones, incluyendo las composiciones liposómicas, pueden ser útiles para la formación de Imágenes y para el tratamiento de los depósitos de la placa ß-amiloide característicos de la Enfermedad de Alzheimer.

Lipid-based nanoparticles

Lipid-based nanoparticle compositions are provided. The compositions generally comprise lipid-hydrophilic polymer- amyloid binding ligand conjugates, and may be liposomal compositions. The compositions, including the liposomal compositions, may be useful for imaging and/or the treatment of amyloid-ß plaque deposits characteristic of Alzheimer' s Disease.

amyloid plaque sister imaging using liposomes

são apresentados compostos aromáticos, conjugados de fosfolipídio-polímero-aromático que compreendem os compostos aromáticos e as composições de lipossomas incluindo os conjugados de fosfolipídio-polímero-aromático. as composições lipossomais podem ser úteis para a geração de imagens da doença de alzheimer, por exemplo, geração de imagens de depósitos da placa ß-amiloide característicos da doença de alzheimer. Aromatic compounds, phospholipid-polymer-aromatic conjugates comprising aromatic compounds and liposome compositions including phospholipid-polymer-aromatic conjugates are disclosed. liposomal compositions may be useful for imaging Alzheimer's disease, for example imaging of ß-amyloid plaque deposits characteristic of Alzheimer's disease.

Lipid-based nanoparticles

Lipid-based nanoparticle compositions are provided. The compositions generally comprise lipid-hydrophilic polymer-amyloid binding ligand conjugates, and may be liposomal compositions. The compositions, including the liposomal compositions comprising, may be useful for imaging and/or the treatment of amyloid-β plaque deposits characteristic of Alzheimer's Disease. One such method for imaging amyloid deposits in a patient is provided, the method comprising: introducing into the patient a detectable quantity of a liposomal composition comprising a lipid-hydrophilic polymer-Formula I ligand conjugate.

Lipid-based nanoparticles

Mri imaging of amyloid plaque using liposomes

Provided are aromatic compounds, phospholipid-polymer-aromatic conjugates comprising the aromatic compounds, and liposome compositions including the phospholipid- polymer-aromatic conjugates. The liposomal compositions may be useful for imaging of Alzheimer's Disease, for example, imaging of the amyloid-ß plaque deposits characteristic of Alzheimer's Disease.

Lipid –based nanoparticles

Compounds comprising a phospholipid-polymer-aromatic conjugate are provided. The compounds may be used in liposomal compositions. The liposomal compositions, may be useful for imaging and/or the treatment of amyloid- plaque deposits characteristic of Alzheimer's Disease.

Targeted contrast agents for mri of alpha-synuclein deposition

Targeted contrast agents for MRI of alpha-synuclein deposition

A liposomal composition (“ADx-003”) is provided, ADx-003 comprising a first phospholipid; a sterically bulky excipient that is capable of stabilizing the liposomal composition; a second phospholipid that is derivatized with a first polymer; a macrocyclic gadolinium-based imaging agent; and a third phospholipid that is derivatized with a second polymer, the second polymer being conjugated to a targeting ligand, the targeting ligand being represented by Formula I: wherein X is —CH 2 —, —CH 2 —CH 2 —, —CHO—, or —O—CO—; Y is —CH—CH═CH— or A and B are independently selected from C and N; R 1 , R 2 , R 3 , and R 4 are independently selected from —H, halogen, —OH, and —CH 3 ; and R 5 , R 6 , and R 7 are independently selected from —H, halogen, —OH, —OCH 3 , —NO 2 , —N(CH 3 ) 2 , C 1 -C 6 alkyl, or a substituted or unsubstituted C 4 -C 6 aryl group, except that when A and/or B is N the adjacent R 5 and/or R 7 is —H, or a pharmaceutically acceptable salt thereof.

Hydrophilic fluorinated molecules for liposomal 19f mri probes with unique mr signatures

Readily available hydrophilic and small organofluorine moieties were condensed via "click chemistry" to generate nonionic hydrophilic fluorinated molecules with unique 19F MR signatures. These were used to fabricate stable liposome formulations for imaging various tissue types. This approach was tailored to exploit the broad spectrum of organic 19F molecular species and to generate probes with distinct 19F MRI signatures for simultaneous assessment of multiple molecular targets within the same target volume.

アミロイド沈着のｍｒｉのための標的造影剤

【課題】アミロイド沈着物をイメージングする方法に用いるリポソーム組成物の提供。【解決手段】アミロイド沈着物をイメージングする方法は以下を含む：（Ａ）患者に検出可能な量のリポソーム組成物を導入すること、ただし該リポソーム組成物は以下を含む：（１）特定のリン脂質又はその塩にコンジュゲートされている大環状ガドリニウム系イメージング剤、（２）下式で表される標的化リガンド、（Ｂ）十分な時間を与え、リポソーム組成物を、１つ又は２つ以上のアミロイド沈着物と会合させること；及び（Ｃ）１つ又は２つ以上のアミロイド沈着物に会合したリポソーム組成物を検出すること。JPEG2024037760000024.jpg55166【選択図】なし

Targeted contrast agents for mri of amyloid deposition

A liposomal composition (“ADx-001”) is provided, ADx-001 comprising a first phospholipid; a sterically bulky excipient that is capable of stabilizing the liposomal composition; a second phospholipid that is derivatized with a first polymer; a macrocyclic gadolinium-based imaging agent; and a third phospholipid that is derivatized with a second polymer, the second polymer being conjugated to a targeting ligand. The macrocyclic gadolinium-based imaging agent may be conjugated to a fourth phospholipid.

Targeted contrast agents for MRI of amyloid deposition

A liposomal composition (“ADx-001”) is provided, ADx-001 comprising a first phospholipid; a sterically bulky excipient that is capable of stabilizing the liposomal composition; a second phospholipid that is derivatized with a first polymer; a macrocyclic gadolinium-based imaging agent; and a third phospholipid that is derivatized with a second polymer, the second polymer being conjugated to a targeting ligand. The macrocyclic gadolinium-based imaging agent may be conjugated to a fourth phospholipid.

Targeted contrast agents for mri of alpha-synuclein deposition

A liposomal composition ("ADx-003") is provided, ADx-003 comprising a first phospholipid; a sterically bulky excipient that is capable of stabilizing the liposomal composition; a second phospholipid that is derivatized with a first polymer; a macrocyclic gadolinium-based imaging agent; and a third phospholipid that is derivatized with a second polymer, the second polymer being conjugated to a targeting ligand, the targeting ligand being represented by Formula (I): wherein X is -CH 2 -, -CH 2 -CH 2 -, -CHO-, or -O-CO-; Y is -CH-CH=CH- or (II); A and B are independently selected from C and N; R 1 , R 2 , R 3 , and R 4 are independently selected from - H, halogen, -OH, and -CH 3 ; and R 5 , R 6 , and R 7 are independently selected from -H, halogen, -OH, -OCH 3 , -NO 2 , -N(CH 3 ) 2 , C 1 -C 6 alkyl, or a substituted or unsubstituted G 4 -C 6 aryl group, except that when A and/or B is N the adjacent R 5 and/or R 7 is -H, or a pharmaceutically acceptable salt thereof.

Targeted contrast agents for mri of alpha-synuclein deposition

A liposomal composition (“ADx-003”) is provided, ADx-003 comprising a first phospholipid; a sterically bulky excipient that is capable of stabilizing the liposomal composition; a second phospholipid that is derivatized with a first polymer; a macrocyclic gadolinium-based imaging agent; and a third phospholipid that is derivatized with a second polymer, the second polymer being conjugated to a targeting ligand, the targeting ligand being represented by Formula I:wherein X is —CH2—, —CH2—CH2—, —CHO—, or —O—CO—; Y is —CH—CH═CH— orA and B are independently selected from C and N; R1, R2, R3, and R4 are independently selected from —H, halogen, —OH, and —CH3; and R5, R6, and R7 are independently selected from —H, halogen, —OH, —OCH3, —NO2, —N(CH3)2, C1-C6 alkyl, or a substituted or unsubstituted C4-C6 aryl group, except that when A and/or B is N the adjacent R5 and/or R7 is —H, or a pharmaceutically acceptable salt thereof.

Composição lipossomal compreendendo um conjugado fosfolipídiopolímero-aromático e um agente potencializador de contraste de imagem de ressonância magnética não radioativo para geração de imagem de depósitos amiloides

GERAÇÃO DE IMAGEM DE IRM DE PLACA AMILOIDE USANDO LIPOSSOMAS. São apresentados compostos aromáticos, conjugados de fosfolipídio-polímero-aromático que compreendem os compostos aromáticos e as composições de lipossomas incluindo os conjugados de fosfolipídio- polímero-aromático. As composições lipossomais podem ser úteis para a geração de imagens da Doença de Alzheimer, por exemplo, geração de imagens de depósitos da placa Beta-amiloide característicos da Doença de Alzheimer.

Hydrophilic fluorinated molecules for liposomal 19f mri probes with unique mr signatures

Readily available hydrophilic and small organofluorine moieties were condensed via “click chemistry” to generate nonionic hydrophilic fluorinated molecules with unique 19 F MR signatures. These were used to fabricate stable liposome formulations for imaging various tissue types. This approach was tailored to exploit the broad spectrum of organic 19 F molecular species and to generate probes with distinct 19 F MRI signatures for simultaneous assessment of multiple molecular targets within the same target volume.

MRI Imaging Of Amyloid Plaque Using Liposomes

Provided are aromatic compounds, phospholipid-polymer-aromatic conjugates comprising the aromatic compounds, and liposome compositions including the phospholipid polymer-aromatic conjugates. The liposomal compositions may be useful for imaging of Alzheimer's Disease, for example, imaging of the amyloid-p plaque deposits characteristic of Alzheimer's Disease.

<smallcaps/>? ? ?functionalized liposomes for imaging misfolded proteins

Phospholipid-polymer-aromatic conjugates comprising binding ligands, liposome compositions including the phospholipid-polymer-aromatic conjugates, and binding ligands having an affinity for misfolded proteins are described. The phospholipid-polymer-aromatic conjugate may be represented by Structural Formula I: PL — AL — HP — X — BL (I). In Formula I, PL is a phospholipid, AL is an aliphatic linkage, HP is hydrophilic polymer, X is a link between the phospholipid-polymer and the binding ligand, and BL is polycyclic aromatic compound that functions as a binding ligand. The liposomal compositions may be useful for the imaging of misfolded and/or aggregated proteins.

Lipid-based nanoparticles

Lipid-based nanoparticle compositions are provided. The compositions generally comprise lipid-hydrophilic polymer-amyloid binding ligand conjugates, and may be liposomal compositions. The compositions, including the liposomal compositions, may be useful for imaging and/or the treatment of amyloid-β plaque deposits characteristic of Alzheimer's Disease.

MRI imaging of amyloid plaque using liposomes

Provided are aromatic compounds, phospholipid-polymer-aromatic conjugates comprising the aromatic compounds, and liposome compositions including the phospholipid-polymer-aromatic conjugates. The liposomal compositions may be useful for imaging of Alzheimer's Disease, for example, imaging of the amyloid-β plaque deposits characteristic of Alzheimer's Disease.