【摘要】：目的:制備N-三甲基殼聚糖(TMC)包覆的水飛薊賓脂質體(SLBL)(TMC60-SLBL),并優(yōu)化處方工藝。方法:比較薄膜分散法、復乳法、逆向蒸發(fā)法對SLBL包封率的影響;以磷脂質量濃度、磷脂-膽固醇質量比、藥脂質量比、水合溫度為因素,以包封率為指標,采用正交試驗優(yōu)選TMC60-SLBL的處方工藝,并進行驗證;比較優(yōu)化處方所制TMC60-SLBL在4、25℃下30 d內的穩(wěn)定性,及其與未包覆SLBL的粒徑、Zeta電位。結果:3種方法中,薄膜分散法所制SLBL包封率較高,且包封率在剪切前后差異無統(tǒng)計學意義(P0.05)。TMC60-SLBL最優(yōu)處方工藝為磷脂質量濃度6 mg/ml、磷脂-膽固醇質量比40∶1、藥脂質量比1∶30、水合溫度45℃,其包封率為(82.08±2.6)%,RSD=3.17%(n=3);在4℃下穩(wěn)定性更好。SLBL和TMC60-SLBL的粒徑分別為(131.9±1.9)、(161.2±2.0)nm,Zeta電位分別為(-23.18±1.14)、(36.73±2.84)m V。結論:成功制得TMC60-SLBL,且處方簡單、方法可行,產品包封率較高。
[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，

本文編號：2244140