目的 制备聚乙二醇1000维生素E琥珀酸酯（D-α-tocopherol polyethylene glycol 1000 succinate，TPGS）修饰的地榆皂苷I长循环脂质体，并对其进行质量评价。方法 采用薄膜分散法制备TPGS包衣脂质体，在单因素实验基础上，通过Box-Behnken响应面分析法对处方进行优化，采用超滤离心法测定药物包封率，透射电镜（TEM）观察脂质体微观形态，激光粒度仪测定脂质体的粒径、多分散性和Zeta电位，并对其稳定性和体外释放情况进行考察。结果 所制得的TPGS包衣脂质体微观形态呈球形或类球形双层结构、外观带淡蓝色乳光，粒径为（95.79±0.81）nm，多分散系数（PDI）为0.048±0.007，Zeta电位为（-38.60±0.97）mV，包封率为79.89%，载药量为10.48%。体外释放研究表明，与游离地榆皂苷I溶液相比，TPGS包衣脂质体具有明显的缓释效果。结论 通过优化后的处方和制备工艺，制备了外观均一稳定、包封率较高的TPGS修饰的地榆皂苷I长循环脂质体，可用于进一步的研究。

Objective To prepare D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) modified ziyuglycoside I long- circulating liposomes and evaluate the quality. Methods TPGS coated liposomes were prepared by the film dispersion method. On the basis of the single factor experiment, the prescription was optimized by Box-Behnken response surface analysis. The drug entrapment efficiency (EE) was determined by ultrafiltration centrifugation, and the microscopic morphology of liposomes were observed under the transmission electron microscope (TEM). The particle size, polydispersity, and Zeta potential were determined by laser particle size analyzer, and investigating the stability and in vitro release of liposomes. Results The microscopic morphology of TPGS coated liposomes were spherical or quasi-spherical bilayer structure with light blue opalescence in appearance, the particle size was (95.79 ±0.81) nm, polydispersity index was 0.048 ±0.007, Zeta potential value was (-38.60 ±0.97) mV, the entrapment efficiency was 79.89%, and the drug load was 10.48%. The in vitro release studies showed that TPGS coated liposomes had an obvious slow-release effect compared with the free ziyuglycoside I solution. Conclusion TPGS-modified ziyuglycoside I long-circulating liposomes with uniform stability and high encapsulation efficiency were prepared through optimized prescription and formulation process, which can be used for further research.

R283.6

贵州省科技厅基础研究计划（黔科合基础［2018］1426）；江西中医药大学现代中药制剂教育部重点实验室开放基金（TCM-202007）