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[负载白藜芦醇的纳米胶束的制备及体外评价]

[Preparation and in vitro evaluation of ampelopsin-loaded nanomicelles].

作者信息

Huang Ren-Jie, Yan Xue-Li, Chen Hu-Biao

机构信息

Department of Pharmacy, Fujian Health College, Fuzhou 350101, China.

School of Chinese Medicine, Hong Kong Baptist University, Hong Kong, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2016 Mar;41(6):1054-1058. doi: 10.4268/cjcmm20160613.

Abstract

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.

摘要

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。

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