姜黄素聚合物胶束的制备及抗肿瘤活性评价  

Preparation and evaluation of antitumor acticity of curcumin polymer micelles

作　　者：杜艳[1] 杜丽 DU Yan;DU Li(School of Pharmacy,Shanxi Medical University,Shanxi Taiyuan 030001,China;Department of Pharmacy,Shanxi Province Cancer Hospital/Shanxi Hospital Affiliated to Cancer Hospital,Chinese Academy of Medical Sciences/Cancer Hospital Affiliated to Shanxi Medical University,Shanxi Taiyuan 030013,China)

机构地区：[1]山西医科大学药学院,山西太原030001 [2]山西省肿瘤医院/中国医学科学院肿瘤医院山西医院/山西医科大学附属肿瘤医院药学部,山西太原030013

出　　处：《中国医院药学杂志》2023年第2期181-185,共5页Chinese Journal of Hospital Pharmacy

摘　　要：目的:制备姜黄素的维生素E聚乙二醇琥珀酸酯(TPGS)聚合物胶束,从而改善姜黄素的水溶性和抗肿瘤活性。方法:以TPGS为载体材料,采用薄膜水化法制备姜黄素胶束;以包封率和粒径为指标,考察水化温度、水化时间、药载比和水化体积的影响;以包封率、粒径、载药量为指标,经四因素三水平正交试验,确定姜黄素/TPGS胶束的最佳制备工艺;考察姜黄素/TPGS胶束的体外释放度;利用MTT法测试姜黄素/TPGS的体外抗肿瘤活性。结果:姜黄素/TPGS胶束的最佳药载比为1∶40,水化温度为60℃,水化时间为30 min,水化体积为6 mL;所得胶束平均粒径为11.02 nm, Zeta电位为-11.31,载药量为2.65%,包封率为96.20%;姜黄素/TPGS 48 h体外累积释放率为78%,具有一定的缓释性;MTT法表明,姜黄素/TPGS具有良好的抗肿瘤活性。结论:该文采用薄膜水化法制备了一种稳定的姜黄素/TPGS胶束,改善了姜黄素的水溶性,明显提高了其抗肿瘤效果。OBJECTIVE To prepare vitamin E polyglycolsuccinyl ester(TPGS)micelles of curcumin(CUR),thus improving the water solubility and antitumor activity of CUR.METHODS Using TPGS as carrier material, CUR micelles were prepared by film dispersionmethod.The effects of hydration temperature, hydration time, drug loading ratio and hydration volume were investigated by using encapsulation ratio and particle size as indexes.The optimum preparation process of CUR/TPGS micelles was determined by orthogonal test of four factors and three levels with encapsulation rate, particle size and drug loading as indexes.The in vitro release of CUR/TPGS micelles was investigated.The in vitroantitumor activity of CUR/TPGS was measured by MTT assay.RESULTS The optimal drug loading ratio of CUR/TPGS micelles was 1∶40,hydration temperature was 60 ℃,hydration time was 30 min and hydration volume was 6 mL.The average particle size of the micelles was 11.02 nm, the Zeta potential was-11.31,the drug loading was 2.65%,and the encapsulation rate was 96.2%.The cumulative release rate of CUR/TPGS 48 h in vitro was 78%,indicating sustained release.MTT assay showed that CUR/TPGS had good antitumor activity.CONCLUSION In this paper, a stable micelle of CUR/TPGS was prepared by thin film hydration method.The water solubility of CUR was improved and its antitumor effect was obviously improved.

关 键 词：姜黄素 胶束 薄膜分散法 体外释放 抗肿瘤活性 

分 类 号：R283.6[医药卫生—中药学]