齐墩果酸PCL-PLA-TPGS纳米粒的工艺优化及体外细胞抑制试验研究  

Optimization of Preparation Technology of Oleanolic Acid-loaded PCL-PLA-TPGS Nanoparticles and in Vitro Cell Inhibitory Test

作　　者：顾晓华[1] 秋泽文[2] 徐红[2] 鲍旭[2] 高萌[2] 梅林[2] 田燕[2] 

机构地区：[1]大连医科大学附属第一医院,辽宁大连116011 [2]大连医科大学,辽宁大连116044

出　　处：《中国药房》2012年第37期3497-3499,共3页China Pharmacy

基　　金：辽宁省教育厅2010年度资助课题(L2010129)

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。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 efficien- cy 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 effi- ciency 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.

关 键 词：齐墩果酸 聚己内酯-聚乳酸-水溶性维生素E 纳米粒 制备 体外试验 细胞生长抑制率 

分 类 号：R944.9[医药卫生—药剂学] R979.19[医药卫生—药学]