LIPIDS, LIPID COMPOSITIONS, LIPOSOMES, AND LIPOPLEXES

摘要

This invention pertains to certain lipids and lipid compositions, liposomes and lipoplexes formed therefrom, methods for their synthesis and preparation, compositions and medicaments comprising such liposomes and lipoplexes, and methods of cellular delivery, transfection, and medical treatment employing such liposomes and lipoplexes. Preferred lipid compositions comprise: (a) a cationic lipid fraction; and, (b) a non-ionic lipid fraction; wherein said cationic lipid fraction comprises one of the following: (A) a mixture of different cationic lipids, and which mixture includes: (i) 3ß-[N-(N',N'-dimethylaminoethyl)carbamoyl] cholesterol (DC-Chol); and, (ii) an amine diether lipid, or an amine diester lipid, or a mixture thereof; (B) an amino acid amide of an amine diether lipid, or an amino acid amide of an amine diester lipid, or a mixture thereof; (C) a mixture of different cationic lipids, and which mixture includes: (i) DC-Chol; and, (ii) an amino acid amide of an amine diether lipid, or an amino acid amide of an amine diester lipid, or a mixture thereof; (D) a mixture of different cationic lipids, and which mixture includes: (i) one or more of: (i-a) DC-Chol; (i-b) an amine diether lipid or an amine diester lipid, or a mixture thereof; and, (i-c) an amino acid amide of an amine diether lipid, or an amino acid amide of an amine diester lipid, or a mixture thereof; and, (ii) a peptide amide of an amine diether lipid, or a peptide amide of an amine diester lipid, or a mixture thereof.