大黄素传递体的制备和质量评价研究

Study on preparation of emodin transfersomes

目的 制备大黄素传递体,并建立其有关质量评价标准.方法 采用薄膜超声法制备大黄素传递体,以包封率为考察指标,通过单因素考察和正交实验设计优选最佳处方和工艺；采用Zetasizer电位及纳米粒度分析仪测定其Zeta电位并分析其大小,用紫外分光光度法测定药物的包封率等.结果 大黄素传递体最佳制备配方为去氧胆酸钠与磷脂比为1∶8,胆固醇与磷脂比为1∶3,维生素E与磷脂比为1∶20,大黄素与磷脂比为1∶6.所得大黄素传递体Zeta电位-15.11 mV,平均粒径为292.2 nm,球形圆整,大小均匀.在检测波长为435 nm处的吸光度（A）与药物浓度[C,（g/L）]的标准曲线方程为A=50.485C -0.0913（R2=0.9991）,测得平均包封率为（69.35 ±0.25）％.结论 该传递体制备处方精确合理、工艺简单可行,所得传递体带负电,粒径较小且分布均匀,包封率高且稳定性好.

Objective To prepare the emodin transfersome and to evaluate its quality. Methods Emodin transfersome was prepared by film-ultrasonic dispersion method. The effects of the ratio of different components in the transfersome products on encapsulation efficiency were investigated. The rates of envelopment of emodin transfersome were determined by ultraviolet spectrophotometry（UV）. The particle size and Zeta potential of emodin transfersome were evaluated by Zetasizer analyzer. Results The appropriate formulation was cholesterol vs phospholipids 1 ： 3, deoxycholic acid sodium salt vs phospholipids 1：6, emodin vs phospholipids 1： 10, vitamin E vs phospholipids 1：20. Zeta potential was-15.11 mV and the particle size was 292.2 nm. The mean encapsulation eitieieney was （65.35 ± 0.25） %. Conclusion The preparation method is simple and reasonable, showing high encapsulation efficiency and stability.