NOVEL LIPOSOME COMPOSITIONS

摘要

The present disclosure provides lipid-containing compositions, including targeted liposomes encapsulating drug, and pharmaceutical formulations thereof, as well as methods for the making and using the lipid-containing compositions, including the use of the targeted liposomes in the treatment of cancer and other diseases.

主权项

1. A targeted liposome comprising one or more phosphatidylcholines is DOPC or DSPC, an N-(ω)-dicarboxylic acid-derivatized phosphatidyl ethanolamine, a targeting factor-modified N-(ω)-dicarboxylic acid-derivatized phosphatidyl ethanolamine, an encapsulated drug and, at least one additional lipid, which is cholesterol;
wherein the mol % of the one or more phosphatidylcholines is 30-70 mol %; wherein the targeting factor-modified N-(ω)-dicarboxylic acid-derivatized phosphatidyl ethanolamine comprises a transferrin linked to a second N-(ω)-dicarboxylic acid-derivatized phosphatidyl ethanolamine; and wherein the N-(ω)-dicarboxylic acid-derivatized phosphatidyl ethanolamine is represented by Formula 1,and
the second N-(ω)-dicarboxylic acid-derivatized phosphatidyl ethanolamine is represented by Formula 3, wherein R1, R2, R5 and R6 are each an acyl group,wherein the acyl groups are acyl groups from saturated or unsaturated aliphatic carboxylic acids having 16-18 carbon atoms,wherein R1, R2, R5 and R6 are the same; andm and p are equal and are an integer from 2 to 4; and; wherein the targeted liposome contains from about 10 μg transferrin/mg lipid to about 50 μg transferrin/mg lipid; and, wherein the liposome does not comprise a non-derivatized phosphatidyl ethanolamine, egg phosphatidylcholine or a hydrophilic polymer.