卡铂前体脂质体的制备及安全性的初步评价

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,加入冻干支持剂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125.1 nm.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.

Preparation and preliminary safety evaluation of carboplatin proliposomes

Objective:To investigate the preparation and safety of carboplatin proliposomes Methods:Carboplatin liposomes were prepared by film extrusion.Mannitol was incorporated into the li- posome 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 ir- ritation and hemolysis post the administration of liposomes in rabbits were characterized.Results:The in- clusion 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,hemagglutina- tion and vein irritation was reported,either,after intravenous injections into rabbits.Conclusion:The highly efficient and safe carboplatin proliposomes were achieved.