摘要
目的 制备包封率高和缓释作用好的顺铂缓释多囊脂质体 ,并与反相蒸发法制备的顺铂普通脂质体比较其体外释药性能。方法 用复乳法制备顺铂多囊脂质体 ,非火焰原子吸收分光光度法测定顺铂含量 ,磷脂酶试剂法测定脂质体中磷脂的浓度。测定包封率和体外释药性。结果 顺铂多囊脂质体平均粒径为 16 6μm ,跨距为 1 0。顺铂包封率可高达 80 %以上。顺铂缓释多囊脂质体的体外释药符合一级释药规律 ,释药t1 2 为 3 7 7h ,比反相蒸发法制备的顺铂普通脂质体延长 8 4倍。经差示热分析发现辅助膜稳定剂有明显的膜稳定作用。结论 顺铂多囊脂质体包封率高 。
Aim To prepare cisplatin multivesicular liposomes with high encapsulation efficiency and sustained release character, and compare the release characteristics with conventional liposomes prepared by reverse phase evaporation method. Methods Cisplatin multivesicular liposomes were prepared using multiple emulsion method. The concentrations of cisplatin and lipids in the liposomes were measured by flameless atomic absorbance spectroscopy (FAAS) and phosphalipid enzyme reagent method, respectively. The encapsulation efficiency, size and release of the cisplatin from the liposomes were studied in vitro . Results The mean diameter of cisplatin multivesicular liposomes was (16 6±1 0) μm. The encapsulation efficiency of cisplatin was more than 80%. The release profile in vitro fitted with a first order equation. The releasing t 1/2 of cisplatin multivesicular liposomes is 37 7 h, which is 8 4 that of conventional liposomes. Co membrane stabilizer has remarkable stabilizing effect on the multivesicular liposomal membrane confirmed by differential scattering calorimetry (DSC). Conclusion The cisplatin multivesicular liposomes showed high encapsulation efficiency and sustained release character.
出处
《药学学报》
CAS
CSCD
北大核心
2003年第2期133-137,共5页
Acta Pharmaceutica Sinica
关键词
顺铂
缓释多囊脂质体
制备
体外释放性能
研究
cisplatin
multivesicular liposomes
preparation
sustained release
encapsulation efficiency
