目的 探讨用β-谷甾醇替代胆固醇制备槲皮素脂质体的可行性，并筛选最佳制备工艺与处方。方法 以卵磷脂和β-谷甾醇为膜材制备不含胆固醇的槲皮素脂质体；以离心沉淀法测定脂质体的包封率；以包封率和载药量为评定指标，筛选该新型槲皮素脂质体的最佳制备方法；用正交设计优化该脂质体的制备工艺；用粒径、Zeta电位、AFM电镜、体外释放表征该新型槲皮素脂质体。结果 该新型脂质体的最佳制备方法为薄膜分散法，通过正交设计得最佳工艺为槲皮素与卵磷脂的质量比为1∶5，卵磷脂与β-谷甾醇的质量比为6∶1，PBS缓冲溶液pH值为6.0，水化时间为2 h。制备的槲皮素脂质体的包封率为（82.55±1.10）%，载药量为（11.40±1.14）%，粒径为（194.60±4.38）nm，Zeta电位为（?30.45±0.42）mV；AFM电镜验证表明该新型脂质体呈规则球形，粒径均一；新型脂质体体外释放与普通脂质体无差异。结论 用β-谷甾醇替代胆固醇制备槲皮素脂质体方法可行，采用最佳工艺制备的槲皮素脂质体包封率高，形态和粒径均较好，重现性好，可应用于工业化生产。

Objective To study the feasibility of preparing quercetin liposomes with β-sitosterol instead of cholesterol and optimize the prescription and preparation of quercetin liposomes. Methods Quercetin liposomes were prepared by film dispersion method with lecithin and β-sitosterol, encapsulation efficiency (EE) was determined by centrifugal precipitation method. EE and drug loading were adopted to evaluate and optimize preparation process as response in orthogonal design. Quercetin liposomes were characterized by particle size, potential, atomic force microscope (AFM) and in vitro release. Results Film dispersion method was the best method to prepare quercetin liposomes with lecithin and β-sitosterol. The optimum preparation process determined by orthogonal design was as follow: the ratio of quercetin to lecithin was 1∶5, the ratio of lecithin to β-sitosterol was 6∶1, pH value of PBS buffer solution was 6.0, the hydration time was 2 h, the EE was (82.55 ± 1.10)%, drug loading was (11.40 ± 1.14)%, particle size was (194.60 ± 4.38) nm, Zeta potential was (?30.45 ± 0.42) mV, and the prepared quercetin liposomes were verified by AFM with round shape and homogenious particle size. There was no difference between new type liposome and ordinary liposome. Conclusion Quercetin liposomes prepared with lecithin and β-sitosterol are practicable. The quercetin liposomes prepared by optimum preparation process have a high EE, good morphology, and reproducibility, and it can be used in industry.

国家自然科学基金资助项目（81102817）；江苏省滩涂生物资源与环境保护重点建设实验室项目（JLCBE09021）；盐城师范学院自然科学基金资助项目（09YCKL010）；盐城师范学院教研项目（13YCTCJY046）；盐城师范学院博士科研启动基金资助项目