发明名称 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.
申请公布号 US8758810(B2) 申请公布日期 2014.06.24
申请号 US201012891568 申请日期 2010.09.27
申请人 Mebiopharm Co., Ltd. 发明人 Okada Kazushi;Ibuki Tadayuki;Kim Donghyun;Fujisawa Tadashi
分类号 A61K9/127 主分类号 A61K9/127
代理机构 Morrison & Foerster LLP 代理人 Morrison & Foerster LLP
主权项 1. A targeted liposome comprising one or more phosphatidylcholines selected from the group consisting of DMPC, DPPC, POPC, and 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 phosphatidylcholines is 30-70 mol %, the cholesterol is 30-60 mol %, and the total of the N-(ω)-dicarboxylic acid-derivatized phosphatidyl ethanolamine plus targeting factor-modified N-(ω)-dicarboxylic acid-derivatized phosphatidyl ethanolamine is 2-12 mol %, and where the total mol % of the phosphatidylcholines, 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 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, andwherein R1 and R2 are the same, and R5 and R6 are the same; andm and p are 3; and,wherein the targeted liposomes 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 used to enhance the circulatory half-life of liposomes.
地址 Minato-ku, Tokyo JP