姜黄素眼用脂质体的制备及晶状体抗氧化作用考察

目的：制备N-三甲基壳聚糖（TMC）包覆姜黄素眼用脂质体并考察其抑制大鼠硒性白内障晶状体氧化作用。方法：采用乙醇注入法制备姜黄素脂质体（Cur-TCL），通过星点设计-效应面法优化脂质体处方工艺；采用过膜法、透射电镜、粒径电位测定仪测定Cur-TCL的理化性质；建立大鼠硒性白内障模型，考察Cur-TCL对白内障形成过程中晶状体氧化的抑制作用。结果：最佳处方为姜黄素1.41 mg，磷脂质量分数4%，胆固醇-磷脂（1：5.44）。经0.5%TMC溶液包覆后脂质体呈球形，粒径增大，电位显著提高，药物包封率基本不变。与未包覆脂质体相比，Cur-TCL组大鼠晶状体中SOD活力提高30.3%，MDA摩尔浓度减少52.4%，GSH含量增加1.29倍。结论：Cur-TCL可显著抑制硒性白内障导致的晶状体氧化过程，为该制剂治疗白内障提供参考。

Preparation of Curcumin-Loaded Ophthalmic Liposomes and Investigation of Its Lenses Antioxidant Efficacy

Objective: To prepare N-trimethyl chitosan(TMC)-coated liposomes loaded with curcumin (Cur-TCL) and investigate its in vivo antioxidant effect on selenite-induced cataract lenses. Method: Cur-TCL were prepared by ethanol injection method and formulation was optimized by central composite design-response surface methodology;Membrane filter,transmission electron microscope,dynamic light scattering and electrophoretic light scattering were employed to determined physicochemical parameters of Cur-TCL;Selenite cataract model in rats was established,inhibition of Cur-TCL on oxidation process in selenite cataract formation was investigated. Result: Optimal formulation was as following:phospholipids concentration 4%,cholesterol-phospholipid(1:5.44),curcumin 1.41 mg and the concentration of TMC solution 0.5%.Cur-TCL was spherical-shaped with increasing of mean particle sizes,signigicantly improving of Zeta potential and drug encapsulation efficiency basically unchanged(92.5±0.35)% after coating liposomes with TMC.Compared with uncoated liposomes,SOD activity was elevated by 30.3%,molar concentration of MDA decreased by 52.4% and the content of GSH increased 1.29-fold. Conclusion: Cur-TCL could significantly delay lenses oxidation process of selenite cataract.This work was useful for further research on application of Cur-TCL for cataract therapy.