目的 考察香茅醇（citronellol，CT）对人喉癌上皮细胞HEp-2和人乳腺癌细胞MCF-7增殖能力的影响，并制备CT自乳化递送系统（self-emulsified drug delivery system，SMs），对HEp-2体外抗肿瘤活性和细胞摄取能力进行评价。方法 采用MTT法考察CT对HEp-2和MCF-7细胞增殖能力的影响；通过伪三元相图法优化香茅醇自乳化递送系统（CT-SMs）处方，进行外观形态、粒径和Zeta电位表征。采用MTT法检测CT-SMs对HEp-2细胞增殖能力的影响；荧光倒置显微镜定性和流式细胞仪定量考察HEp-2细胞对CT-SMs的摄取情况。结果 经一定质量浓度CT处理后，MCF-7细胞增殖未受影响，差异无统计学意义（与对照组相比，P>0.05），而HEp-2细胞的增殖能力受到明显抑制（与对照组相比，P<0.05），呈剂量-时间依赖性；CT-SMs最佳处方是K_m（乳化剂与助乳化剂比例）为Kolliphor^® HS15-无水乙醇7：3，CT-K_m为3：7。制备的微乳平均粒径为（354.0±9.5）nm，外观圆整呈类球形，分布均匀，Zeta电位为（-13.4±0.3）mV。细胞摄取实验结果表明，相同质量浓度的CT-SMs和CT处理HEp-2细胞后，CT-SMs较CT摄取量更多，分别为545.70±11.56、230.00±17.76。结论 采用滴加水法成功制备了CT-SMs，其处方工艺可行，制得的自微乳质量稳定可控。CT-SMs可明显抑制HEp-2细胞的增殖。

Objective To investigate the effect of citronellol (citronellol, CT) on the proliferation of HEp-2 and MCF-7 cells, and prepare CT self-emulsifying drug delivery system (CT-SMs). Its antitumor activity and cell uptake ability of HEp-2 cells in vitro was evaluated. Methods The effect of CT on the cell proliferation of HEp-2 and MCF-7 were investigated by MTT assay. The pseudo-ternary phase diagram method was used to optimize the formulation of CT-SMs, and the appearance morphology, mean particle size, and Zeta potential were characterized. The effect of CT-SMs on the proliferation of HEp-2 cells was detected by MTT assay and cellular uptake was determined by fluorescence inversion microscopy and flow cytometry. Results After a certain concentration of CT treatment, MCF-7 cells proliferation was not affected, and the difference was not statistically significant (P>0.05 compared with the control group), while the proliferative capacity of HEp-2 cells was significantly inhibited (P<0.05 compared with the control group) in a dose-time dependent manner. The best prescription for CT-SMs was as following:K_m (emulsifier:co-emulsifier) was Kolliphor^® HS 15:absolute ethanol=7:3, CT:K_m=3:7, the mean particle size was (354.0±9.5) nm, the appearance was round and spherical with uniform distribution, and the Zeta potential was (-13.4±0.3) mV. The results of cellular uptake experiments showed that the intake of CT-SMs (545.70±11.56) was higher than that of CT (230.00±17.76) in HEp-2 cells treating the same concentration of CT-SMs and CT. Conclusion CT-SMs could significantly inhibit the proliferation of HEp-2 cells. In this study, CT-SMs were successfully prepared by dropping water method and the quality of CT-SMs was stable and controllable.

R283.6

贵阳市科技计划项目（筑科合同[2017]30-25号）；贵州省科技创新团队项目（黔科合人才团队[2015]4025号）；贵州省高层次创新型人才百层次人才项目（贵州省科技厅黔科合人才[2015]4029号；贵州医科大学药学国际科技合作基地（黔科合平台人才[2017]5802）