【摘要】 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、20μg·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2.5μg·mL-1时OPPTN在24、48、72h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。更多还原

【Abstract】 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 toPCL-PLA-TPGS 4 ∶10,0.03% of TPGS concentration,400 W of ultrasonic power,12 h of stirring time. The mean particle sizewas(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.更多还原