目的 制备番荔枝总内酯纳米混悬剂，并对其体外抗肿瘤作用进行研究。方法 使用反溶剂沉淀法中的超声法制备番荔枝总内酯纳米混悬剂，考察其处方和制备工艺参数；动态光散射法测定其粒径和电位，透射电镜考察其粒径分布和形态；并对其人工胃肠液稳定性进行考察；采用MTT比色法比较番荔枝总内酯纳米混悬剂和溶液对HepG2细胞毒性差异。结果 制备方法为将10 mg番荔枝总内酯与1 mg PGDA共溶于1 mL有机溶剂中，超声（250 W）快速注入到5 mL水中，减压旋转蒸发除去有机溶剂，调整总体积至5 mL。番荔枝总内酯纳米混悬剂平均粒径为（146.0±2.4）nm，多分散指数（PDI）为0.184±0.02，Zeta电位（26.0±2.0）mV，纳米混悬剂几乎呈类球型，粒径分布接近于正态分布，分布比较均匀；人工胃肠液内4 h稳定存在，粒径基本不发生变化；对HepG2细胞增殖均有一定的抑制作用，番荔枝总内酯纳米混悬剂组的细胞增殖抑制效果均优于溶液组。结论 制备了以PGDA为载体的番荔枝总内酯纳米混悬剂，解决了药物的难溶和给药问题，为番荔枝总内酯的纳米剂型研究提供了参考。

Objective To prepare Annonaceous Acetogenins (ACGs) Naonosuspensions and study its anti-tumor activities in vitro. Methods ACGs Naonosuspensions were prepared with ultrasonic method in anti-solvent precipitation and its prescription and preparation process parameters were investigated. Dynamic light scattering method was used to measure particle size and transmission electron microscopy was used to observe the morphology. The stability of ACGs Nanosuspensions in different medium was also studied. MTT assay was used to assess their in vitro cytotoxicity against HepG2 cell line in contrast to free ACGs. Results The best preparation method was as following:10 mg ACGs and 1 mg PGDA co-dissolved in 1 mL organic solvents, and then were rapidly infused into 5 mL water by ultrasound (250 W), then decompressed and rotated evaporation to remove organic solvents, and were adjusted the total volume to 5 mL. The average particle size of ACGs Naonosuspensions was (146.0 ±2.4) nm, the polydispersity index (PDI) value was 0.184 ±0.02, the Zeta potential was (26.0 ±2.0) mV, and the particle size distribution was close to normal distribution. Naonosuspensions were nearly spherical, and the distribution was more uniform. They were quite stable in artificial gastric juice and intestinal juice for 4 h. ACGs Naonosuspensions had a certain inhibitory effect against proliferation of HepG2 cells, and the effect of naonosuspensions group was better than that of the solution group. Conclusion ACGs Naonosuspensions are successfully prepared taking PGDA as the carrier, and insolubility and drug delivery are solved, which provides reference for nano-formulation study of ACGs.

国家自然科学基金-广东联合基金资助项目（U1401223）