目的 采用星点设计-效应面法优化传明酸传递体的处方。方法 逆向旋蒸法制备传明酸传递体；通过考察膜材比、脂药比及脱氧胆酸钠用量对包封率、载药量的影响，并对结果进行二项式方程拟合，用效应面法预测最佳处方，并对其稳定性进行研究。结果 确定最优处方为膜材比2∶1、脂药比6∶1、脱氧胆酸钠用量为20 mg；以该处方制备所得传明酸传递体的包封率为（81.28±1.06）%、载药量为（4.67±0.28）%、平均粒径为（105.3±7.2）nm、Zeta电位为（?38.5±2.3）mV，且实测值与预测值的偏差较小。结论 星点设计-效应面优化法筛选传明酸传递体是一种简便、可行的实验设计方法。

Objective To optimize the formulation and prepration of tranexamic acid (TA) transfersomes by central composite design-response surface method. Methods The transfersomes were prepared using the reverse rotary evaporation method. The effects of phosphatidylcholine (SPC)-cholesterol (CH) ratio, SPC-drug ratio, and the concentration of sodium deoxycholic acid on the entrapment efficiency (EE) were investigated, the results were fitted with binomial equation, and the optimal formulation was predicted by response surface method. Results The preparation conditions were optimized as SPC-CH (2∶1), SPC-drug (6∶1), and the concentration of sodium deoxycholic acid 20 mg. Under these conditions, the evaluated EE, drug-loading, average partical size, and Zeta potential of TA transfersomes were (81.28 ± 1.06)%, (4.67 ± 0.28)%, (105.3 ± 7.2) nm, and (?38.5 ± 2.3) mV. The deviation of measured and predicated values was smaller. Conclusion The central composite design-response surface method is applicable for the optimization of TA transfersomes and the resulting optimal preparation technique is stable and feasible.

陕西省教育厅产业化中试项目（2010jc20）