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评价一种自微乳释药物传递系统的紫杉醇。

Evaluation of a self-nanoemulsifying docetaxel delivery system.

机构信息

Nanomedicine and Nanobiology Research Center, Shiraz University of Medical Sciences, Shiraz, Iran.

Arasto Pharmaceutical Chemicals Inc., Yousefabad, Jahanarar Avenue, Tehran, Iran.

出版信息

Biomed Pharmacother. 2019 Jan;109:2427-2433. doi: 10.1016/j.biopha.2018.11.110. Epub 2018 Nov 30.

Abstract

A self-nanoemulsifying drug delivery system (SNEDDS) was developed as a novel route to enhance the efficacy of docetaxel lipophilic drug. SNEDDS comprised ethyl oleate, Tween 80 and poly(ethylene glycol) 600, as oil, surfactant and co-surfactant, and formed stabilized monodispersed oil nanodroplets upon dilution in water. SNEDDS represented encapsulation efficiency and loading capacity of 21.4 and 52.7%, respectively. The docetaxel release profile from the drug-loaded SNEDDS was recorded, its effectiveness against MCF-7 cell line was investigated, and an IC value of 0.98 ± 0.05 μg mL was attained. The drug-loaded SNEDDS was administrated in rats, and the pharmacokinetic parameters of maximum concentration of 22.2 ± 0.8 μg mL, time to attain this maximum concentration of 230 min, and area under the curve of 1.71 ± 0.18 μg min mL were obtained. The developed SNEDDS formulation can be represented as an alternative to docetaxel administration.

摘要

自微乳药物传递系统(SNEDDS)被开发为一种增强疏水性药物多西紫杉醇疗效的新途径。SNEDDS 由油酸乙酯、吐温 80 和聚乙二醇 600 组成,分别作为油相、表面活性剂和助表面活性剂,在水中稀释后形成稳定的单分散油纳米液滴。SNEDDS 的包封效率和载药量分别为 21.4%和 52.7%。记录了载药 SNEDDS 的多西紫杉醇释放曲线,研究了其对 MCF-7 细胞系的作用,得到 IC 值为 0.98±0.05μg mL。将载药 SNEDDS 给大鼠给药,得到最大浓度为 22.2±0.8μg mL 的药代动力学参数,达到最大浓度的时间为 230 分钟,曲线下面积为 1.71±0.18μg min mL。所开发的 SNEDDS 制剂可作为多西紫杉醇给药的替代方案。

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