卡铂前体脂质体的制备及安全性的初步评价  

Preparation and preliminary safety evaluation of carboplatin proliposomes

作　　者：田维维[1] 刘清飞[1] 罗国安[1] 王义明[1] 苏强[1] 

机构地区：[1]清华大学药物研究所,北京100084

出　　处：《中国新药杂志》2006年第13期1070-1073,共4页Chinese Journal of New Drugs

基　　金：863计划资助项目(2003BA310A03)

摘　　要：目的:制备卡铂前体脂质体,并对用药安全性进行初步评价。方法:采用薄膜挤压法制备卡铂脂质体,加入冻干支持制冷冻干燥后得到卡铂前体脂质体。对豚鼠全身用药的过敏性、家兔全身用药的血管刺激性以及溶血性进行考察。结果:制备所得的卡铂前体脂质体水合后的包封率为72．0%,载药量为24．0%,平均粒径为125．1mm。卡铂前体脂质体不引起豚鼠过敏反应,不引起家兔溶血和红细胞凝集反应,静脉注射对家兔血管无刺激性。结论:制备所得的卡铂前体脂质体有较高的包封率和载药量,水合后粒径均匀,形态圆整,且具有较好的用药安全性。Objective： To investigate the preparation and safety of carboplatin proliposomes. Methods： Carboplatin liposomes were prepared by film extrusion. Mannitol was incorporated into the liposome to prevent the liposome vesicles from aggregation. The carboplatin proliposomes were obtained by lyophilization. Allergic reactions to carboplatin proliposomes were evaluated in Guinea pigs. The vein irritation and hemolysis post the administration of liposomes in rabbits were characterized. Results： The inclusion efficiency and drug delivery ratio of the rehydrated carboplatin proliposomes were 72.0% and 24.0% , respectively. The particle size of the liposomes was well-distributed and in well-rounded shape, averaging 125.1 nm. No allergic reactions were found in Guinea pigs. None of hemolysis, hemagglutination and vein irritation was reported, either, after intravenous injections into rabbits. Conclusion： The highly efficient and safe carboplatin proliposomes were achieved.

关 键 词：卡铂 前体脂质体 冷冻干燥 薄膜挤压 安全性 

分 类 号：R943.42[医药卫生—药剂学] R979.1[医药卫生—药学]