Huang Ren-Jie, Yan Xue-Li, Chen Hu-Biao
Department of Pharmacy, Fujian Health College, Fuzhou 350101, China.
School of Chinese Medicine, Hong Kong Baptist University, Hong Kong, China.
Zhongguo Zhong Yao Za Zhi. 2016 Mar;41(6):1054-1058. doi: 10.4268/cjcmm20160613.
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.
为提高蛇葡萄素的溶解度和抗肿瘤活性，采用薄膜水化法，以泊洛沙姆F127和聚乙二醇1000维生素E琥珀酸酯（TPGS1000）的混合物制备了载蛇葡萄素纳米胶束，以优化工艺条件和理化性质。分别采用MTT法比较蛇葡萄素和纳米胶束对MCF-7细胞的抗肿瘤活性。结果表明，最佳纳米胶束呈圆形，纳米尺寸为（22.6±0.5）nm，包封率为（80.42±1.13）%，载药率为（4.41±0.26）%。蛇葡萄素在混合纳米胶束中的溶解度显著提高了16倍。在不同释放介质中，混合纳米胶束在8小时内可释放90%以上的药物，并对MCF-7细胞表现出更强的细胞毒性和抑制作用（P<0.01）。混合纳米胶束可作为蛇葡萄素的新型药物递送系统。
