目的 制备水飞蓟宾（silybin，SLB）前体脂质体并对其进行质量评价。方法 采用冷冻干燥法制备SLB前体脂质体，以包封率和载药量为评价指标，采用单因素考察和正交试验法，优化SLB前体脂质体处方及制备工艺，筛选最优冻干保护剂并考察SLB前体脂质体的形态、粒径分布、包封率及稳定性。结果 SLB前体脂质体的最优处方及制备工艺为药脂比1∶12，磷脂胆固醇比4∶1，水合介质pH值为7.4，制备温度为45 ℃；最优冻干保护剂为甘露醇；所形成的前体脂质体外观饱满、致密，复水水合后粒径为（251.40±2.14）nm，Zeta电位值为（−30.80±0.89）mV，包封率为（88.92±5.86）%，贮存期间（30 d）稳定性较好。结论 制备的SLB前体脂质体工艺简单、包封率高、稳定性好，值得进一步研究。

Objective To prepare silybin (SLB) proliposomes and evaluate its quality. Methods SLB proliposomes were prepared by freeze-drying method, and the formulation and process were optimized by single factor investigation and orthogonal design with the encapsulation efficiency and drug loading as indexes. The optimal cryoprotetant was selected and the morphology, particle size, encapsulation efficiency, and stability of SLB proliposomes were investigated. Results The optimized preparation process was as follows:The ratio of drug to total lipid was 1:12, the ratio of phospholipid to cholesterol was 4:1, the pH of hydration medium was 7.4 and the temperature was 45℃. Mannitol was the optimal cryprotectant to prepare SLB proliposomes, and the formation of SLB proliposomes looked plumpy and compact. The size of preliposome was around (251.40±2.14) nm, the Zeta potential was around (-30.80±0.89) mV, encapsulation efficiency was (88.92±5.86)%, and it had good stability during storage. Conclusion The preparation process of SLB proliposomes is simple, and it has high encapsulation efficiency and good stability, therefore, it is deserved to be further studied.

国家自然科学基金资助项目（81303231）；陕西省科技厅项目（2015JM8449）；陕西省优势学科资助项目（1007）；西安医学院校级科研青年基金项目（2015QN05）；西安医学院校级大学生创新基金项目（2015DXS1-11）