目的 考察香茅醇（citronellol，CT）對(duì)人喉癌上皮細(xì)胞HEp-2和人乳腺癌細(xì)胞MCF-7增殖能力的影響，并制備CT自乳化遞送系統(tǒng)（self-emulsified drug delivery system，SMs），對(duì)HEp-2體外抗腫瘤活性和細(xì)胞攝取能力進(jìn)行評(píng)價(jià)。方法 采用MTT法考察CT對(duì)HEp-2和MCF-7細(xì)胞增殖能力的影響；通過偽三元相圖法優(yōu)化香茅醇自乳化遞送系統(tǒng)（CT-SMs）處方，進(jìn)行外觀形態(tài)、粒徑和Zeta電位表征。采用MTT法檢測(cè)CT-SMs對(duì)HEp-2細(xì)胞增殖能力的影響；熒光倒置顯微鏡定性和流式細(xì)胞儀定量考察HEp-2細(xì)胞對(duì)CT-SMs的攝取情況。結(jié)果 經(jīng)一定質(zhì)量濃度CT處理后，MCF-7細(xì)胞增殖未受影響，差異無統(tǒng)計(jì)學(xué)意義（與對(duì)照組相比，P>0.05），而HEp-2細(xì)胞的增殖能力受到明顯抑制（與對(duì)照組相比，P<0.05），呈劑量-時(shí)間依賴性；CT-SMs最佳處方是K_m（乳化劑與助乳化劑比例）為Kolliphor^® HS15-無水乙醇7：3，CT-K_m為3：7。制備的微乳平均粒徑為（354.0±9.5）nm，外觀圓整呈類球形，分布均勻，Zeta電位為（-13.4±0.3）mV。細(xì)胞攝取實(shí)驗(yàn)結(jié)果表明，相同質(zhì)量濃度的CT-SMs和CT處理HEp-2細(xì)胞后，CT-SMs較CT攝取量更多，分別為545.70±11.56、230.00±17.76。結(jié)論 采用滴加水法成功制備了CT-SMs，其處方工藝可行，制得的自微乳質(zhì)量穩(wěn)定可控。CT-SMs可明顯抑制HEp-2細(xì)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

貴陽市科技計(jì)劃項(xiàng)目（筑科合同[2017]30-25號(hào)）；貴州省科技創(chuàng)新團(tuán)隊(duì)項(xiàng)目（黔科合人才團(tuán)隊(duì)[2015]4025號(hào)）；貴州省高層次創(chuàng)新型人才百層次人才項(xiàng)目（貴州省科技廳黔科合人才[2015]4029號(hào)；貴州醫(yī)科大學(xué)藥學(xué)國(guó)際科技合作基地（黔科合平臺(tái)人才[2017]5802）