目的 制备黄芩苷(baicalin,BCN)聚乙二醇维生素E琥珀酸酯(TPGS)纳米胶束(BCN-TPGS-PMs)以改善其溶解性和体外抗肿瘤效果.方法 采用薄膜水化法制备BCN-TPGS-PMs;透射电子显微镜观察纳米胶束形态;粒度测定仪考察其粒径和Zeta电位;超速离心法考察制剂的包封率及载药量;动态膜透析法考察体外释药特性;四甲基偶氮唑盐(MTT)法考察其对人乳腺癌细胞(MCF-7)的抑制作用.结果 所制备的BCN-TPGS-PMs平均粒径为(11.91±0.14)nm;载药量和包封率分别为(5.42±0.04)%和(95.83±7.34)%;在体外pH 7.4、6.5的磷酸盐缓冲液(PBS)中24 h内分别释放28.53%和35.06%;表明所制备胶束粒径较小且均一,体外释放具有一定缓释性.同时体外细胞毒性实验表明BCN-TPGS-PMs较BCN能够显著地抑制MCF-7细胞的增殖(P<0.05).结论 所制备的BCN-TPGS-PMs粒径小,载药量高,稳定性好,能显著提高BCN的体外抗肿瘤效果.

Objective To prepare baicalin-loaded TPGS nanomicells (BCN-TPGS-PMs) and to evaluate its physicochemical properties, in vitro release behavior, and antitumor activity against MCF-7 cells. Methods BCN-TPGS-PMs were prepared by film-thin hydration method. The preparation methods and formulations were optimized and screened based on particle size and encapsulation efficiency (EE) of micelles. The transmission electron microscope (TEM) was used to observe the particle appearance, zetasizer instrument was used to detect the diameter and Zeta potential, and ultracentrifugation was utilized to determine the EE and drug-loading rate. Dynamic dialysis method was used to study the in vitro release behavior of BCN-TPGS-PMs, and the antitumor activity against MCF-7 cells was determined by MTT method. Results The optimal BCN-TPGS-PMs were round with the nanometric size of (11.91 ± 0.14) nm, high EE rate of (95.83 ± 7.34)%, and drug-loading rate of (5.42 ± 0.04)%. The in vitro release behavior showed that BCN-TPGS-PMs had a slow release. Compared with free BCN, BCN-TPGS-PMs showed stronger cytotoxicity and inhibition against MCF-7 cells (P < 0.05). Conclusion The prepared BCN-TPGS-PMs have small particle size, high drug-loading rate, and good stability, and could obviously increase the in vitro inhibitory effect of BCN.

高等学校博士学科点专项科研基金(20130013120008)