公开(公告)号：US20080113015A1

公开(公告)日：2008-05-15

申请号：US11569514

申请日：2005-05-24

申请人： Hermann Katinger ,  Andreas Wagner ,  Karola Vorauer-Uhl ,  Renate Kunert ,  Stefanie Strobach

发明人： Hermann Katinger ,  Andreas Wagner ,  Karola Vorauer-Uhl ,  Renate Kunert ,  Stefanie Strobach

IPC分类号： A61K9/127 ,  A61K38/16 ,  A61K31/715 ,  A61P43/00

CPC分类号： A61K9/1271

摘要： The present invention relates to liposomes for drug delivery, wherein a liposome includes molecules of at least one desired drug distributed within an aqueous phase in the interior of the liposome and wherein the liposome further includes molecules of the same or of another drug attached to either or both sides of the liposomal membrane. More specifically, the invention relates to liposomes, wherein at least a part of the molecules of a desired drug bear a functional group that is reactive with a functional group present in at least one lipid fraction, and wherein the drug is covalently linked to the membrane lipids by chemical bonding, e.g. by ester bonding of a hydroxyl group of a lipid molecule and an acidic residue of the drug. In a preferred embodiment, the desired drug is a glycoprotein such as erythropoietin. The invention further relates to a method of manufacture of said liposomes and to pharmaceutical compositions containing them.

摘要翻译： 本发明涉及用于药物递送的脂质体，其中脂质体包括分布在脂质体内部的水相内的至少一种所需药物的分子，并且其中所述脂质体还包括与所述脂质体或其它药物相连接的分子， 脂质体膜两侧。 更具体地，本发明涉及脂质体，其中所需药物的至少一部分分子具有与存在于至少一种脂质部分中的官能团反应的官能团，并且其中所述药物与膜共价连接 脂质通过化学键合，例如 通过脂质分子的羟基和药物的酸性残基的酯键合。 在优选的实施方案中，所需药物是糖蛋白，例如红细胞生成素。 本发明还涉及制备所述脂质体的方法和含有它们的药物组合物。