Ligand-targeted emulsions carrying bioactive agents
First Claim
1. A composition for use in delivering a bioactive agent to targeted tissues or cells comprising:
- (a) a lipid-encapsulated oil in water emulsion of fluorochemical particles, wherein the particles have an outer monolayer of lipid and wherein the lipid outer monolayer further comprises a primer material;
(b) a bioactive agent in or on the surface of the lipid outer monolayer of the particles; and
(c) a site-specific targeting ligand, wherein the ligand is covalently coupled to the primer material;
wherein the primer material is selected from the group consisting of 1-ethyl-3-(3-N-N-dimethylaminopropyl)carbodiimide hydrochloride, 1-cyclohexyl-3-(2-morpholinoethyl)carbodiimide methyl-p-toluenesulfonate, and 1,2-diacyl-sn-glycerol-3-phosphoethanolamine-N-(4-p-maleimidephenyl)-butyramide.
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Accused Products
Abstract
A composition for use in delivering a bioactive agent to targeted tissues or cells comprises: (a) a site-specific targeting ligand; (b) a lipid encapsulated oil in water emulsion; and (c) a bioactive agent in or on the surface of the outer monolayer of the emulsion; the ligand being conjugated directly or indirectly to the emulsion and the composition providing facilitated delivery of the bioactive agent through prolonged association and increased contact of the ligand-bound lipid encapsulated emulsion particles with the lipid bilayer of the target tissues or cells. The composition may also comprise a lipid encapsulated oil in water emulsion and a combination site-specific targeting ligand/bioactive agent. Methods for improved delivery of a bioactive agent to targeted tissues or cells are also disclosed.
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Citations
60 Claims
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1. A composition for use in delivering a bioactive agent to targeted tissues or cells comprising:
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(a) a lipid-encapsulated oil in water emulsion of fluorochemical particles, wherein the particles have an outer monolayer of lipid and wherein the lipid outer monolayer further comprises a primer material;
(b) a bioactive agent in or on the surface of the lipid outer monolayer of the particles; and
(c) a site-specific targeting ligand, wherein the ligand is covalently coupled to the primer material;
wherein the primer material is selected from the group consisting of 1-ethyl-3-(3-N-N-dimethylaminopropyl)carbodiimide hydrochloride, 1-cyclohexyl-3-(2-morpholinoethyl)carbodiimide methyl-p-toluenesulfonate, and 1,2-diacyl-sn-glycerol-3-phosphoethanolamine-N-(4-p-maleimidephenyl)-butyramide. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17)
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18. A composition for use in delivering a bioactive agent to targeted tissues or cells comprising:
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(a) a lipid-encapsulated oil in water emulsion of fluorochemical particles, wherein the particles have an outer monolayer of lipid and wherein the lipid outer monolayer further comprises a primer material; and
(b) a combination site-specific targeting ligand/bioactive agent in or on the surface of the lipid outer monolayer of the particles;
wherein said combination ligand/bioactive agent is covalently coupled to the primer material;
wherein the primer material is selected from the group consisting of 1-ethyl-3-(3-N-N-dimethylaminopropyl)carbodiimide hydrochloride, 1-cyclohexyl-3-(2-morpholinoethyl)carbodiimide methyl-p-toluenesulfonate, and 1,2-diacyl-sn-glycerol-3-phosphoethanolamine-N-(4-p-maleimidephenyl)-butyramide.- View Dependent Claims (19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 58)
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30. A method for improved delivery of a bioactive agent to targeted tissues or cells comprising administering to said tissues or cells a composition comprising:
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(a) a lipid-encapsulated oil in water emulsion of fluorochemical particles, wherein the particles have an outer monolayer of lipid and wherein the lipid outer monolayer further comprises a primer material;
(b) a bioactive agent in or on the surface of the lipid outer monolayer of the particles; and
(c) a site-specific targeting ligand, wherein the ligand is covalently coupled to the primer material;
wherein the primer material is selected from the group consisting of 1-ethyl-3-(3-N-N-dimethylaminopropyl)carbodiimide hydrochloride, 1-cyclohexyl-3-(2-morpholinoethyl)carbodiimide methyl-p-toluenesulfonate, and 1,2-diacyl-sn-glycerol-3-phosphoethanolamine-N-(4-p-maleimidephenyl)-butyramide. - View Dependent Claims (31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 59)
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46. A method for improved delivery of a bioactive agent to targeted tissues or cells comprising administering to said tissues or cells a composition comprising:
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(a) a lipid-encapsulated oil in water emulsion of fluorochemical particles, wherein the particles have an outer monolayer of lipid and wherein the lipid outer monolayer further comprises a primer material; and
(b) a combination site-specific targeting ligand/bioactive agent in or on the surface of the lipid outer monolayer of the particles;
wherein said combination ligand/bioactive agent is covalently coupled to the primer material;
wherein the primer material is selected from the group consisting of 1-ethyl-3-(3-N-N-dimethylaminopropyl)carbodiimide hydrochloride, 1-cyclohexyl-3-(2-morpholinoethyl)carbodiimide methyl-p-toluenesulfonate, and 1,2-diacyl-sn-glycerol-3-phosphoethanolamine-N-(4-p-maleimidephenyl)-butyramide.- View Dependent Claims (47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 60)
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Specification