研究聚乙二醇修饰木犀草素脂质体的最佳制备工艺，以提高木犀草素的生物利用度。采用薄膜分散法制备聚乙二醇修饰木犀草素脂质体，以磷脂、胆固醇和磷脂酰乙醇胺-聚乙二醇2000作为载体，包封率为评价指标，采用Box-Behnken设计实验响应面优化法优化工艺参数，分析聚乙二醇修饰木犀草素脂质体的粒径、电位和形态等指标。结果表明聚乙二醇修饰木犀草素脂质体的最佳制备参数为：膜材比为10:1，脂药比为16:1，磷脂酰乙醇胺-聚乙二醇2000的质量分数为3%，超声时间15 min，水化温度40 ℃。Box-Behnken响应面法优化后的聚乙二醇修饰木犀草素脂质体平均包封率为86.3%，平均粒径为134.1 nm，电位为-14.07 mV，且在胃液、小肠液和结肠液中的累积释放率分别为39.08%、43.67%和71.71%。所制备的聚乙二醇修饰木犀草素脂质体包封率高，粒度均匀，缓释效果明显。

The optimal preparation process of polyethylene glycol-modified luteolin liposome was investigated to enhance the bioavailability of luteolin. Polyethylene glycol-modified luteolin liposomes were prepared by the thin-film dispersion method. Phospholipids, cholesterol and phosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG2000) were employed as carriers, and the encapsulation efficiency was used as the evaluation index. The Box-Behnken design experiment was used to optimize the process parameters by response surface optimization method. Then the size, zeta potential and morphology of the prepared liposomes were determined. Results showed that the optimal conditions were: ratio of membrane to material was 10:1, ratio of lipid to drug was 16:1, and mass fraction of DSPE-PEG2000 was 3%, ultrasonic treatment time was 15 min, and hydration temperature was 40 ℃. The average encapsulation efficiency of the modified luteolin liposomes was approximately 86.3%, with the mean particle size and potential being 134.1 nm and -14.07 mV, respectively. The cumulative release rates of luteolin from the liposomes in the simulated gastric juice, small intestinal juice and colon fluid were 39.08%, 43.67% and 71.71%, respectively. The prepared liposomes had a high encapsulation efficiency, uniform particle size and obvious sustained-release effect. The preparation method is simple and feasible.

西安市科技计划项目（2019216514GXRC001CG002-GXYD1.6）；西安市未央区科技计划项目（201926）