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目的制备并表征装载依托泊苷(VP-16)的D-?-生育酚-聚乙二醇琥珀酸酯(TPGS)胶束(VP-16/TPGS)。方法采用薄膜水化法制备VP-16/TPGS,测定其粒径、Zeta电位,研究其体外药物释放行为,考察其细胞摄取和细胞毒性,评价其血液相容性。结果所制得的VP-16/TPGS胶束具有较小的粒径;具有较高的载药量和包封率;体外呈现良好的缓控释效果;可增强H446细胞对其的摄取,进而提高抗肿瘤活性;具有较高的血液相容性。结论 VP-16/TPGS胶束是一种安全、有效的VP-16递送系统。
Objective To prepare and characterize D -? - tocopherol - polyethylene glycol succinate (VPGS) micelles (VP-16 / TPGS) loaded with etoposide (VP-16) Methods The membrane hydration method was used to prepare VP-16 / TPGS. The particle size and Zeta potential of VP-16 / TPGS were measured. The in vitro drug release behavior was investigated. The cellular uptake and cytotoxicity were investigated to evaluate the blood compatibility. Results The obtained VP-16 / TPGS micelles showed a smaller particle size, higher drug loading and entrapment efficiency, good sustained and controlled release in vitro, increased uptake by H446 cells, Improve anti-tumor activity; with high blood compatibility. Conclusion VP-16 / TPGS micelles are a safe and effective VP-16 delivery system.