摘要
目的以聚乙二醇1000-维生素E琥珀酸酯(TPGS)为载体,制备姜黄素(Cur)胶束,从而改善Cur的水溶性和抗肿瘤活性。方法以粒径和载药量为指标,筛选Cur/TPGS胶束的制备方法;以胶束的粒径、Zeta电位等为评价指标,优化Cur/TPGS投料比;利用动态光散射技术和透射电镜技术,表征胶束的粒径、形态;利用MTT法测试Cur原料药和Cur/TPGS胶束的体外抗肿瘤活性。结果本文选择透析法制备Cur/TPGS胶束,Cur/TPGS的最佳投料比为1∶10,所得胶束呈球形,平均粒径约为54.4 nm,Zeta电位约为-12.1mV,载药量为7.35%,包封率为81.3%,稳定性良好。MTT法实验结果表明,Cur/TPGS胶束具有良好的体外抗肿瘤活性。结论本文采用透析法制备了一种稳定的Cur/TPGS胶束,改善了Cur的水溶性,明显提高了其抗肿瘤效果。
Objective To prepare curcumin(Cur)micelles with D-α-tocopherol polyethylene glycol 1000 succinate(TPGS)as carrier,so as to improve the water solubility and antitumor activity of curcumin. Methods The preparation method of Cur/TPGS micelles was investigated under the indication of particle size and drug loading of the micelles.The particle size of micelle and Zeta potential were used as evaluation indices to optimize the feed ratio of Cur/TPGS. The particle size and morphology of the micelles were characterized by the dynamic light scatter(DLS)method and transmission electron microscopy(TEM). The in vitro antitumor activity of Cur and Cur/TPGS micelles was evaluated by the MTT method. Results The Cur/TPGS micelle was manufactured by the dialysis method. The optimum feed ratio of Cur/TPGS was 1∶10. The Cur/TPGS micelles showed a spherical shape,with the average particle size and Zeta potential of 54.4 nm and-12.1 mV,respectively. The drug loading and the encapsulation efficiency were 7.35% and 81.3%,respectively. The Cur/TPGS micelles had a good stability and showed an in vitro antitumor activity better than Cur in the MTT test. Conclusion A stable Cur/TPGS micelle was prepared using the dialysis method in the present study,which greatly improved the water solubility and in vitro antitumor efficacy of Cur.
作者
韩宝来
李禄辉
刘伟芬
HAN Bao-lai;LI Lu-hui;LIU Wei-fen(Henan Vocational College of Applied Technology,Zhengzhou 450042,China)
出处
《国际药学研究杂志》
CAS
北大核心
2019年第8期606-613,共8页
Journal of International Pharmaceutical Research
基金
河南省科技攻关项目(182102310811)
