申请人:NeXstar Pharmaceuticals, Inc.
公开号:EP0661044A1
公开(公告)日:1995-07-05
Unilamellar liposomes having a diameter of from 30 to 150 nm are described, comprising a liposomal membrane including distearoylphosphatidylcholine (DSPC) and cholesterol, in a DSPC:cholesterol molar ratio of about 2:1, the liposomes encapsulating an antineoplastic selected from vincristine and vinblastine and an anion of low liposomal membrane permeability including a carboxylate moiety, for example a monocarboxylate, dicarboxylate, tricarboxylate or polycarboxylate anion, more particularly gluceptate, fumarate, gluconate, lactobionate, maleate, succinate, glutarate, tartrate, citrate or carbopol.
本发明描述了直径为 30 至 150 nm 的单层脂质体,该脂质体由包括二硬脂酰磷脂酰胆碱 (DSPC) 和胆固醇的脂质体膜组成,DSPC:胆固醇的摩尔比约为 2:脂质体包封选自长春新碱和长春碱的抗肿瘤药物,以及脂质体膜渗透性低的阴离子,包括羧酸盐分子,例如单羧酸盐、二羧酸盐、三羧酸盐或多羧酸盐阴离子,特别是葡糖酸盐、富马酸盐、葡糖酸盐、乳糖酸盐、马来酸盐、琥珀酸盐、戊二酸盐、酒石酸盐、柠檬酸盐或卡波尔盐。