摘要
目的:以pH梯度法制备伊立替康脂质体,研究两种铵盐对伊立替康脂质体主动载药行为的影响。方法:采用薄膜分散-高压乳匀法制备空白脂质体,通过pH梯度法将药物包封入脂质体中,建立铵离子的测定方法;研究pH梯度、孵化温度对脂质体包封率及药物释放的影响。结果:以硫酸铵和磷酸氢二铵建立脂质体膜内外梯度制备的空白脂质体主动载药后,包封率分别为(98.2±1.5)%和(87.6±2.3)%,两种脂质体的包封率均随pH梯度增加而增加,其中以硫酸铵制备的载药脂质体药物的释放较慢。结论:pH梯度法适合制备伊立替康脂质体,pH相同时,铵盐的类型对脂质体主动载药后的包封率和释放均有一定影响。
Aim： To prepare irinotecan （CPT-11） liposomes by pH-gradient method, and to investigate the effect of the type of ammonium sahs on the active loading process. Methods： Drug-free liposomes were prepared by thin-film dispersion and high pressure homogenization, and CPT-11 was encapsulated into the blank liposomes by pH-gradient method. The method for determining amino gradient was established. Effect of pH gradient and the incubation temperature on the encapsulation efficiency （EE） and the release of CPT-11 from the liposomes were investigated. Results： The EE of liposomes by using ammonium sulfate and ammonium phosphate dibasic as inner phase was （ 87.6 ± 2. 3） % and （98.2 ± 1.5） %, respectively. The EE of the liposomes was increased in propor- tion to the increase in pH gradient, and the release rate of CPT-11 from liposomes with ammonium phosphate dibasic as inner phase was slower than that with ammonium sulfate as inner phase. Conclusion： The preparation of CPT-11 liposomes by pH-gradient method is feasible. The type of ammonium salts affect both the encapsulation efficiency and the release behavior of liposomes if exposed to the same pH gradient.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2008年第4期312-316,共5页
Journal of China Pharmaceutical University
关键词
伊立替康
PH梯度法
脂质体
硫酸铵梯度
磷酸氢二铵梯度
irinotecan
pH-gradient method
liposome
ammonium sulfate gradient
ammonium phosphate dibasic gradient
