Liposome compositions
First Claim
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1. A targeted liposome comprising one or more phosphatidylcholines, 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 phosphatidylcholines is 40-60 mol %, the mol % of the cholesterol is 35-55 mol %, and the mol % of the total of the N-(ω
)-dicarboxylic acid-derivatized phosphatidyl ethanolamine plus targeting factor-modified N-(ω
)-dicarboxylic acid-derivatized phosphatidyl ethanolamine is 2-8 mol %, where the total mol % of the phosphatidylcholines, the cholesterol, and the derivatized phosphatidylethanolamines is 100%wherein the targeting factor-modified N-(ω
)-dicarboxylic acid-derivatized phosphatidyl ethanolamine comprises transferrin linked to a second N-(ω
)-dicarboxylic acid-derivatized phosphatidyl ethanolamine; and
whereinthe N-(ω
)-dicarboxylic acid-derivatized phosphatidyl ethanolamine is represented by Formula 1,
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Abstract
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.
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Citations
48 Claims
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1. A targeted liposome comprising one or more phosphatidylcholines, 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 phosphatidylcholines is 40-60 mol %, the mol % of the cholesterol is 35-55 mol %, and the mol % of the total of the N-(ω
)-dicarboxylic acid-derivatized phosphatidyl ethanolamine plus targeting factor-modified N-(ω
)-dicarboxylic acid-derivatized phosphatidyl ethanolamine is 2-8 mol %, where the total mol % of the phosphatidylcholines, the cholesterol, and the derivatized phosphatidylethanolamines is 100%wherein the targeting factor-modified N-(ω
)-dicarboxylic acid-derivatized phosphatidyl ethanolamine comprises transferrin linked to a second N-(ω
)-dicarboxylic acid-derivatized phosphatidyl ethanolamine; andwherein the N-(ω
)-dicarboxylic acid-derivatized phosphatidyl ethanolamine is represented by Formula 1, - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 48)
- )-dicarboxylic acid-derivatized phosphatidyl ethanolamine, a targeting factor-modified N-(ω
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45. A targeted liposome comprising one or more phosphatidylcholines, 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 phosphatidylcholines is 40-60 mol %, the mol % of the cholesterol is 35-55 mol %, and the mol % of the total of the N-(ω
)-dicarboxylic acid-derivatized phosphatidyl ethanolamine plus targeting factor-modified N-(ω
)-dicarboxylic acid-derivatized phosphatidyl ethanolamine is 2-8 mol %, where the total mol % of the phosphatidylcholines, the cholesterol, and the derivatized phosphatidylethanolamines is 100%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; andwherein the N-(ω
)-dicarboxylic acid-derivatized phosphatidyl ethanolamine is represented by Formula 1, - View Dependent Claims (46, 47)
- )-dicarboxylic acid-derivatized phosphatidyl ethanolamine, a targeting factor-modified N-(ω
Specification