Cho Hyun-Jong, Park Ju-Hwan, Kim Dae-Duk, Yoon In-Soo
J Nanosci Nanotechnol. 2016 Feb;16(2):1433-6. doi: 10.1166/jnn.2016.11918.
Docetaxel (DCT) is one of anti-mitotic chemotherapeutic agents and has been used for the treatment of gastric cancer as well as head and neck cancer, breast cancer and prostate cancer. Poly(lactic- co-glycolic) acid (PLGA) is one of representative biocompatible and biodegradable polymers, and polyoxyl 15 hydroxystearate (Solutol HS15) is a nonionic solubilizer and emulsifying agent. In this investigation, PLGA/Solutol HS15-based nanoparticles (NPs) for DCT delivery were fabricated by a modified emulsification-solvent evaporation method. PLGA/Solutol HS15/DCT NPs with about 169 nm of mean diameter, narrow size distribution, negative zeta potential, and spherical morphology were prepared. The results of solid-state studies revealed the successful dispersion of DCT in PLGA matrix and its amorphization during the preparation process of NPs. According to the result of in vitro release test, emulsifying property of Solutol HS15 seemed to contribute to the enhanced drug release from NPs at physiological pH. All these findings imply that developed PLGA/Solutol HS15-based NP can be a promising local anticancer drug delivery system for cancer therapy.
多西他赛（DCT）是一种抗有丝分裂化疗药物，已被用于治疗胃癌以及头颈癌、乳腺癌和前列腺癌。聚乳酸-乙醇酸共聚物（PLGA）是一种具有代表性的生物相容性和可生物降解的聚合物，聚氧乙烯15羟基硬脂酸酯（Solutol HS15）是一种非离子增溶剂和乳化剂。在本研究中，通过改进的乳化-溶剂蒸发法制备了用于递送DCT的基于PLGA/Solutol HS15的纳米颗粒（NPs）。制备出了平均直径约为169 nm、粒径分布窄、ζ电位为负且呈球形形态的PLGA/Solutol HS15/DCT NPs。固态研究结果表明DCT在PLGA基质中成功分散且在NPs制备过程中发生了非晶化。根据体外释放试验结果，Solutol HS15的乳化性能似乎有助于在生理pH值下增强药物从NPs中的释放。所有这些发现表明，所开发的基于PLGA/Solutol HS15的NP可能是一种用于癌症治疗的有前景的局部抗癌药物递送系统。
