N-三甲基壳聚糖包覆的水飞蓟宾脂质体的制备及处方工艺优化

发布时间：2018-09-15 07:10

【摘要】：目的:制备N-三甲基壳聚糖(TMC)包覆的水飞蓟宾脂质体(SLBL)(TMC60-SLBL),并优化处方工艺。方法:比较薄膜分散法、复乳法、逆向蒸发法对SLBL包封率的影响;以磷脂质量浓度、磷脂-胆固醇质量比、药脂质量比、水合温度为因素,以包封率为指标,采用正交试验优选TMC60-SLBL的处方工艺,并进行验证;比较优化处方所制TMC60-SLBL在4、25℃下30 d内的稳定性,及其与未包覆SLBL的粒径、Zeta电位。结果:3种方法中,薄膜分散法所制SLBL包封率较高,且包封率在剪切前后差异无统计学意义(P0.05)。TMC60-SLBL最优处方工艺为磷脂质量浓度6 mg/ml、磷脂-胆固醇质量比40∶1、药脂质量比1∶30、水合温度45℃,其包封率为(82.08±2.6)%,RSD=3.17%(n=3);在4℃下稳定性更好。SLBL和TMC60-SLBL的粒径分别为(131.9±1.9)、(161.2±2.0)nm,Zeta电位分别为(-23.18±1.14)、(36.73±2.84)m V。结论:成功制得TMC60-SLBL,且处方简单、方法可行,产品包封率较高。
[Abstract]:Aim: to prepare silybin liposome (SLBL) (TMC60-SLBL coated with N-trimethyl chitosan (TMC) and optimize its formulation. Methods: the effects of film dispersion method, double emulsion method and reverse evaporation method on the entrapment efficiency of SLBL were compared, and the entrapment efficiency was determined by the mass concentration of phospholipids, the mass ratio of phospholipid to cholesterol, the mass ratio of lipids and lipids, and the hydration temperature. The formulation process of TMC60-SLBL was optimized by orthogonal test, and the stability of TMC60-SLBL prepared by the optimized formulation was compared with that of uncoated SLBL within 30 days at 4 ~ 25 鈩，

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