Lipophilic-polycationic delivery systems
First Claim
1. A lipophilic biomolecular complex comprising:
- a) a polycationic carrier selected from the group consisting of poly-lysine, poly-arginine and poly-ornithine containing a minimum of 5 monomeric amino acid units and wherein said polycationic carrier has 2-20 eicosapentaenoic acid moieties attached to the terminal amino or guanidino groups of their constitutive monomers, b) a biologically active agent and c) one or more additional eicosapentaenoic acid moieties.
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Abstract
The present invention describes site-specific biomolecular complexes comprising a therapeutic, prophylactic and diagnostic agent, called also biologically active molecule and an omega-3 fatty acid and derivatives thereof. The complexes are further covalently bonded with cationic carriers and permeabilizer peptides for delivery across the blood-brain barrier and with targeting moieties for uptake by target brain cells. Said complexes are particularly useful for delivery of a biologically active agent to the glial tissue of the brain as well as to the cortical, cholinergic and adrenergic neurons. The preferred therapeutic complexes or conjugates comprise an omega-3 fatty acid such as alpha-linolenic acid, eicosapentaenoic acid or docosahexaenoic acid and derivatives thereof.
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Citations
24 Claims
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1. A lipophilic biomolecular complex comprising:
a) a polycationic carrier selected from the group consisting of poly-lysine, poly-arginine and poly-ornithine containing a minimum of 5 monomeric amino acid units and wherein said polycationic carrier has 2-20 eicosapentaenoic acid moieties attached to the terminal amino or guanidino groups of their constitutive monomers, b) a biologically active agent and c) one or more additional eicosapentaenoic acid moieties. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10)
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11. A lipophilic biomolecular complex comprising:
a) a polycationic carrier selected from the group consisting of poly-lysine, poly-arginine and poly-ornithine containing a minimum of 5 monomeric amino acid units and wherein said polycationic carrier has 2-20 docosahexaenoic acid moieties attached to the terminal amino or guanidino groups of their constitutive monomers, b) a biologically active agent and c) one or more additional docosahexaenoic acid moieties. - View Dependent Claims (12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24)
Specification