Nanomedicine and Nanobiology Research Center, Shiraz University of Medical Sciences, Shiraz, Iran.
Arasto Pharmaceutical Chemicals Inc., Yousefabad, Jahanarar Avenue, Tehran, Iran.
Biomed Pharmacother. 2019 Jan;109:2427-2433. doi: 10.1016/j.biopha.2018.11.110. Epub 2018 Nov 30.
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.
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。
