OBJECTIVE: To optimize preparation technology of Oleanolic acid-loaded PCL-PLA-TPGS nanoparticles (OA-PCL-PLA-TPGS-NPs, namely OPPTN) , and to study inhibiting ratio on tumor cell (Hca-F) cultivated in vitro. METHODS: OPPTN were prepared by ultrasonication emulsion/solvent evaporation technique using self-made PCL-PLA-TPGS as carrier. The preparation conditions were selected by single factor method using their mean particle size, drug loading and encapsulation efficiency as evaluated index, such as proportion of OA to PCL-PLA-TPGS, the concentration of TPGS, ultrasonic power and stirring time. Inhibiting ratio of OPPTN on tumor cell (Hca-F) cultivated in vitro in 24, 38, 72 h was assessed by MTT assay method with OA concentrations of 2.5, 10, 20 μg·mL-1. RESULTS: Optimal preparation conditions were as follows: the ratio of OA to PCL-PLA-TPGS 4 :10, 0.03% of TPGS concentration, 400 W of ultrasonic power, 12 h of stirring time. The mean particle size was (214.2 ± 1.6) nm, Zeta potential was ( -23.7 ± 1.1) mV, drug-loading amount was (26.97 ± 2.13)% and encapsulation efficiency was (89.36 ± 2.06)%. Inhibiting ratio of OPPTN on tumor cell (Hca-F) cultivated in vitro in 24, 48, 72 h were 30.6% , 44.8% , 51.2% respectively with OA concentration of 2.5 μg·mL-1, increasing to 66.1% , 79.6% , 89.7% with OA concentration of 20 μg·mL-1. CONCLUSION: Preparation technology of OPPTN is reasonable and feasible, and prepared OPPTN show obvious sustained-release effect and anticancer activity.%目的:优化制备齐墩果酸(OA)聚己内酯-聚乳酸-水溶性维生素E纳米粒(OA-PCL-PLA-TPGS-NPs,简称OPPTN)的工艺条件,并研究其对小鼠腹水型肝癌高淋巴道转移细胞株(HCa-F)的体外细胞生长抑制率(IR).方法:用自制的PCL-PLA-TPGS为载体材料,采用超声乳化-溶剂挥发法制备OPPTN,以平均粒径、载药量和包封率为评价指标,通过单因素考察优化制备OPPTN时OA与载体的质量比、TPGS浓度、超声功率、搅拌时间;采用MTT法测定OA浓度为2.5、10、20 μg· mL-1时OPPTN对HCa-F细胞作用24、48、72h的IR.结果:较佳工艺为OA与载体质量比为4:10、TPGS浓度为0.03％、超声功率为400W、搅拌时间为12h;按此条件制备的OPPTN的平均粒径、Zeta电位、载药量和包封率分别为(214.2±1.6) nm、(-23.7±1.1)mV、(26.97±2.13)％和(89.36±2.06)％;OA浓度为2.5 μg·mL-1时OPPTN在24、48、72 h时对HCa-F的IR分别为30.6％、44.8％、51.2％,OA浓度为20μg· mL-1时IR分别为66.1％、79.6％、89.7％.结论:OPPTN的制备工艺合理可行,体外细胞试验显示其具有良好的缓释作用、生物可降解性及较强的抗肝癌活性.
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