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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p H 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 (BCN) polyethylene glycol vitamin E succinate (TPGS) nanomicelles (BCN-TPGS-PMs) to improve its solubility and antitumor effect in vitro. Methods BCN-TPGS-PMs were prepared by the membrane hydration method. The morphology of the nanomicelles was observed by transmission electron microscopy. The particle size and Zeta potential were measured by particle size analyzer. The entrapment efficiency and drug loading were determined by ultracentrifugation. Method to investigate the in vitro release characteristics; MTT assay of human breast cancer cells (MCF-7) inhibition. Results The average particle diameter of BCN-TPGS-PMs was (11.91 ± 0.14) nm. The drug loading and encapsulation efficiency were (5.42 ± 0.04)% and (95.83 ± 7.34)%, respectively. Phosphate buffered saline (PBS) released 28.53% and 35.06% respectively within 24 h. The results showed that the size of micelles prepared was small and uniform, and sustained release in vitro was observed. In vitro cytotoxicity experiments showed that BCN-TPGS-PMs significantly inhibited the proliferation of MCF-7 cells compared with BCN (P <0.05). Conclusion BCN-TPGS-PMs prepared with small particle size, high drug loading, good stability, can significantly enhance the anti-tumor effect of BCN in vitro.