摘要
目的:对N-三甲基壳聚糖(TMC60)包衣羟喜树碱脂质体(HCPTL)冻干剂的处方及制备工艺进行优化。方法:采用逆向蒸发法制备HCPTL,并用TMC60包衣,经高压乳匀得到纳米级脂质体。以包封率为考察指标,正交试验优选处方及工艺,并筛选最佳的冻干保护剂进行冷冻干燥。对复水化后脂质体的形态、Zeta电位、粒径等进行考察。结果:TMC60包衣HCPTL的最佳处方及工艺为:药脂比为1:30,胆固醇:卵磷脂为1:3,旋蒸温度为35℃,TMC60浓度为0.35%,最佳冻干保护剂为15%(w/v)的海藻糖。复水化后形态圆整,平均包封率为(82.2±2.3)%(n=3),Zeta电位为(53.2±2.0)mV,平均粒径为(92.4±18.5)nm。结论:TMC60包衣HCPTL冻干剂具有包封率高,表面带正电荷等特点,为其进一步研究奠定了基础。
Objective：To screen the optimal formula and preparation process of lyophilized N-trimethyl chitosan-coated hydroxycamptothecin liposomes（HCPTL）.Method：HCPTL was prepared by reverse phase evaporation,coated by TMC60 and homogenized by a high pressure homogenizer.The entrapment efficient（EE%） as the evaluation index,the formula and preparation process were optimized by orthogonal design.The freeze-drying process was carried out after the optimal protective agent was selected.The morphology, Zeta potential and size of the liposomes were studied after re-hydration.Result：The optimal formula and preparation process were as follows;the ratio of drug and lipids was 1：30,the ratio of lecithin and cholesterol was 1-3,the rotation temperature was 35℃and the concentration of TMC60 was 0.35%.After re-hydration,the morphology of the liposomes was spherical with the average EE%of （82.2±2.3）%,the Zeta potential of（53.2±2.0） mV and the average size of（92.4±18.5） nm.Conclusion：Lyophilized TMC60- coated HCPTL with high EE%and positive potential provides the basis for the further study.
出处
《中国药师》
CAS
2013年第6期791-794,共4页
China Pharmacist
关键词
羟喜树碱
N-三甲基壳聚糖
脂质体
冻干
研制
Hydroxycamptothecin
N-trimethyl chitosan
Liposomes
Lyophilization
Preparation
