蛇葡萄素混合纳米胶束的制备及体外评价

Preparation and in vitro evaluation of ampelopsin-loaded nanomicelles

为了提高蛇葡萄素的溶解性和抗肿瘤活性,以普朗尼克F127和D-α-维生素E聚乙二醇1000琥珀酸酯为复合载体材料,采用薄膜水化法制备蛇葡萄素纳米胶束,考察蛇葡萄素纳米胶束的最佳工艺条件和理化参数。采用MTT法,比较原料及纳米胶束制剂对MCF-7细胞增殖的抑制作用。结果表明,蛇葡萄素纳米胶束平均粒径为(22.6±0.5)nm,包封率为(80.42±1.13)%,载药量为(4.41±0.26)%。所制得的蛇葡萄素混合纳米胶束比蛇葡萄素原料的溶解度增加16倍,且在不同释放介质中8 h可累积释放药物90%以上,并能够显著抑制MCF-7细胞的增殖(P<0.01)。该混合纳米胶束可作为蛇葡萄素新的药物传递系统。

To improve the solubility and antitumor activity of ampelopsin,ampelopsin-loaded nanomicelles from the mixture of pluronic F127 and D-α-tocopheryl polyethylene glycol 1000 succinate（ TPGS1000） were prepared by film-thin hydration method,in order to optimize the process conditions and physicochemical properties. The antitumor activities against MCF-7 cells between ampelopsin and nanomicelles were compared by MTT method,respectively. The results showed that the optimal nanomicelles were round with the nanometric size of（ 22. 6 ± 0. 5） nm,encapsulation efficiency rate of（ 80. 42 ± 1. 13） %,and drug-loading rate of（ 4. 41 ± 0. 26） %. The solubility of ampelopsin in mixed nanomicelles significantly increased by 16 times. In different release media,the mixed nanomicelles could release more than 90% of drug in 8 h,and showed stronger cytotoxicity and inhibition against MCF-7 cells（ P 0. 01）. The mixed nanomicelles can be used as new drug delivery system of ampelopsin.