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目的制备TPGS/VE-hyd-DOX酸敏感聚合物胶束,延长阿霉素在体内的循环时间,并降低阿霉素的不良反应。方法将盐酸阿霉素(DOX·HCl)上的氨基与D-α生育酚琥珀酸酯(VE)上的羟基连接,用薄膜溶剂水化法制备TPGS/VE-hyd-DOX聚合物胶束,紫外分光光度法(UV)测定阿霉素的含量,计算包封率,粒度仪测定其粒径及电位,并对其体外释放药物特性进行了分析。结果 TPGS/VE-hyd-DOX聚合物胶束的平均粒径为(85.06±3.20)nm,Zeta电位为0.315 mV。平均包封率为(93.00±2.49)%,TPGS/VE-hyd-DOX聚合物胶束较TPGS/VE-amid-DOX聚合物胶束具有明显的pH敏感性。结论该聚合物胶束具有良好的物理特性和缓释效果,作为抗肿瘤药物的靶向传递系统具有良好的应用前景。
OBJECTIVE To prepare TPGS / VE-hyd-DOX acid-sensitive polymer micelles to prolong the circulating time of doxorubicin in vivo and to reduce the adverse reaction of doxorubicin. Methods The amino groups on doxorubicin hydrochloride (DOX · HCl) were linked to hydroxyl groups on D-α-tocopheryl succinate (VE). The TPGS / VE-hyd-DOX polymer micelles were prepared by thin- The content of doxorubicin was determined by UV spectrophotometry. The entrapment efficiency was calculated. The particle size and potential were measured by particle size analyzer. The drug release characteristics in vitro were analyzed. Results The average size of TPGS / VE-hyd-DOX micelles was (85.06 ± 3.20) nm and the zeta potential was 0.315 mV. The average entrapment efficiency of TPGS / VE-hyd-DOX polymer micelles was (93.00 ± 2.49)%, which was significantly higher than that of TPGS / VE-amid-DOX polymer micelles. Conclusion The polymer micelles have good physical properties and sustained release effect, which has good application prospects as a targeted delivery system of antitumor drugs.