摘要
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 the eptoposide（VP-16）-loaded D-α tocopheryl polyethylene glycol succinate（TPGS） micelles. METHODS The VP-16/TPGS was prepared using thin-film hydration method. The particle size and Zeta potential were measured. The drug release behavior, cellular uptake and cytotoxicity were also studied. At last, the hemocompatibility was also evaluated. RESULTS The prepared VP-16/TPGS micelles had small sizes, high drug loading capacity and encapsulated efficiency. The VP-16/TPGS micelles also exhibited a sustained and controllable in vitro release behavior. The enhanced cellular uptake of the VP-16/TPGS micelles by H446 celles improved the cytotoxicity. Besides, the VP-16/TPGS micelles showed a good hemocompatibility. CONCLUSION VP-16/TPGS nanomicelle may be a safe and efficient drug delivery system for VP-16.
出处
《中国现代应用药学》
CAS
CSCD
2017年第7期992-996,共5页
Chinese Journal of Modern Applied Pharmacy
