目的 优化蛇葡萄素纳米结构脂质载体（ampelopsin loaded nanostructured lipid carriers，AMP-NLC）处方并对其进行质量表征，研究其对SMMC-7721细胞抑制作用和摄取情况。方法 采用有机溶剂蒸发法制备AMP-NLC，在单因素实验基础上结合Box-Behnken响应面优化AMP-NLC处方并对其进行质量表征。用MTT法测定SMMC-7721细胞的半数抑制浓度（inhibitory concentration of 50%，IC₅₀），并用罗丹明B染料观察其摄取情况。结果 最优处方为山嵛酸甘油酯与中链三酰甘油的比例为1∶11.5、药脂比为1∶10.5、蛋黄卵磷脂用量为21 mg和P188的用量为2%，所制AMP-NLC的平均包封率为（81.71±1.76）%、平均载药量为（3.86±0.22）%、平均粒径为（156.50±7.11）nm和平均ζ电位为（−11.00±0.95）mV，体外释药过程符合一级释放模型Q＝47.93(1－e^{−0.625 2 t})，蛇葡萄素和AMP-NLC对SMMC-7721细胞的IC₅₀分别为44.51、41.51μg/mL，且相对蛇葡萄素原料药，SMMC-7721细胞对AMP-NLC有较好摄取。结论 Box-Behnken响应面法所建立的模型可用于AMP-NLC处方优化，AMP-NLC能有效提高蛇葡萄素在SMMC-7721细胞的相对摄取。

Objective To optimize the formulation of ampelopsin nanostructured lipid carriers (AMP-NLC) and to characterize its quality, and to study its inhibitory effect on SMMC-7721 cells and its uptake. Methods AMP-NLC was prepared by organic solvent evaporation, and based on the single factor test combined with Box-Behnken response surface, the AMP-NLC prescription was optimized and its quality was characterized. The IC₅₀ of SMMC-7721 was measured by MTT method, and the uptake of SMMC-7721 cells was observed by rhodamine B dye.Results The optimal formula was that the ratio of glyceryl behenate to medium chain triglyceride was 1:11.5, the ratio of drug to lipid was 1:10.5, the dosage of egg yolk lecithin was 21 mg and the dosage of P188 was 2%, respectively. The average encapsulation efficiency of AMP-NLC was (81.71 ±1.76)%, the average drug loading was (3.86 ±0.22)%, the average particle size was (156.50 ±7.11) nm and the zeta potential was (−11.00 ±0.95) mV. The in vitro drug release process conformed to the primary release model Q=47.93(1-e^{−0.625 2 t}). The IC₅₀ of ampelopsin and AMP-NLC for SMMC-7721 cells were 44.51 and 41.51 μg/mL, and compared with ampelopsin, SMMC-7721 cells had a better uptake to AMP-NLC. Conclusion The model established by Box-Behnken design-response surface could be employed to optimize the formulation of AMP-NLC, and AMP-NLC could effectively improve the relative uptake of ampelopsin in SMMC-7721 cells.

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国家自然科学基金资助项目（81960756）；广西自然科学基金资助项目（2022GXNSFDA035063）；广西自然科学基金资助项目（2018GXNSFAA050078）；广西高校中青年教师科研基础能力提升基金资助项目（2019KY0148）；广西高校中青年教师科研基础能力提升基金资助项目（2019KY0315）