目的 以非离子表面活性剂为载体材料进行甘草次酸(GA)类脂囊泡(GA-NI)的制备,并对其进行质量评价研究。方法 采用薄膜分散-超声法建立GA-NI的制备方法;采用反透析法和紫外分光光度法测定包封率;通过单因素、星点设计-响应面法优化制备工艺及处方;并对最佳处方类脂囊泡的形态学、平均粒径、Zeta电位及包封率等性质进行考察。结果 最佳处方工艺为司盘80-胆固醇2:1,水合温度为70 ℃、水合时间为51 min、超声时间为60 min,其预测包封率为80.66%,预测值与理论值的偏差4.95%,二项式拟合复相关系数0.989 9。结论 采用星点设计-效应面法优选的GA-NI制备工艺稳定可行、精密度高、可预测性好。

Objective With nonionic surfactants as the carrier material to prepare glycyrrhetinic acid (GC) niosomes (NI) and to evaluate the quality. Methods The thin film dispersion-ultrasound method was used for establishing the preparation process of GC -NI, reverse dialysis method and ultraviolet spectrophotometer method were used to determine the encapsulation efficiency (EE), the prescription and preparation process were optimized through single factor and central composite design-response surface methodology (CCD-RSM), and the properties of morphology, particle size, Zeta potential, and EE in optimized NI were investigated. Results The optimum prescription process as Span 80-cholesterol was 2:1, hydration temperature was 70 ℃, hydration time was 51 min, ultrasonic time was 60 min, its forecast EE was 80.66%, bias between the observed and predicted values was 4.95%, and regression coefficient of binomial fitting complex model was as high as 0.989 9. Conclusion CCD-RSM is used to optimize the preparation, which has the stable, feasible, high precision, and good predictability advantage.

甘肃省科技支撑计划--甘草次酸口服囊泡包裹的纳米载体构建及肝靶向特性研究(1204FKCA183)