论文摘要
目的：制备聚乙二醇-聚乳酸-乙醇酸载硫酸长春新碱纳米粒（PEG-PLGA-VCR-NPs）并对其质量进行评价,研究其对肝癌细胞HepG2的体外抗肿瘤活性。方法：采用复乳-溶剂挥发法制备PEG-PLGA-VCR-NPs,在单因素试验的基础上通过正交试验优选其最佳制备工艺条件；质量评价包括外观及再分散性、形态、粒径大小及分布、zeta电位、载药率、包封率、稳定性、体外药物释放；MTT法考察其对HepG2细胞生长的抑制作用。结果：正交试验优选的最佳制备工艺条件为：PEG-PLGA浓度为20mg/mL,内水相/油相体积比为4/10,外水相/油相体积比为6/1,超声时间为1.5min；样品冻干粉为白色、疏松粉末,再分散性好,纳米粒子形态为类球形,粒径为159.6士%2.1nm,电位为-28.8士3.0%mv,载药量6.54士1.3%,包封率为70.5士1.5%,4℃保存6个月稳定性良好,体外释放结果表明PEG-PLGA-VCR-NPs可持续释放14d,累积释放量达到93.3%,其释放符合Higuchi方程；MTT结果表明随着时间的延长,其抗肿瘤作用显著增强。结论：采用复乳-溶剂挥发法制备的PEG-PLGA-VCR-NPs具有较合适的粒径,较高的载药量和包封率,较好的稳定性,显著的缓释效果和更强的抗肿瘤活性。
论文目录
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