Cerqueira Brenda Brenner S, Lasham Annette, Shelling Andrew N, Al-Kassas Raida
School of Pharmacy, Faculty of Medical and Health Sciences, University of Auckland, Auckland, New Zealand.
Department of Molecular Medicine and Pathology, Faculty of Medical and Health Sciences, University of Auckland, Auckland, New Zealand.
Mater Sci Eng C Mater Biol Appl. 2017 Jul 1;76:593-600. doi: 10.1016/j.msec.2017.03.121. Epub 2017 Mar 18.
This study aimed at development of poly (lactic-co-glycolic acid) (PLGA) nanoparticles embedded with paclitaxel and coated with hyaluronic acid (HA-PTX-PLGA) to actively target the drug to a triple negative breast cancer cells. Nanoparticles were successfully fabricated using a modified oil-in-water emulsion method. The effect of various formulations parameters on the physicochemical properties of the nanoparticles was investigated. SEM imaging confirmed the spherical shape and nano-scale size of the nanoparticles. A sustained drug release profile was obtained and enhanced PTX cytotoxicity was observed when MDA-MB-231 cells were incubated with the HA-PTX-PLGA formulation compared to cells incubated with the non-HA coated nanoparticles. Moreover, HA-PLGA nanoparticles exhibited improved cellular uptake, based on a possible receptor mediated endocytosis due to interaction of HA with CD44 receptors when compared to non-coated PLGA nanoparticles. The non-haemolytic potential of the nanoparticles indicated the suitability of the developed formulation for intravenous administration.
本研究旨在开发包载紫杉醇并涂覆透明质酸的聚（乳酸-乙醇酸）共聚物纳米粒（HA-PTX-PLGA），以将药物主动靶向三阴性乳腺癌细胞。采用改良的水包油乳液法成功制备了纳米粒。研究了各种制剂参数对纳米粒理化性质的影响。扫描电子显微镜成像证实了纳米粒的球形和纳米级尺寸。与用未涂覆透明质酸的纳米粒孵育的细胞相比，当MDA-MB-231细胞与HA-PTX-PLGA制剂孵育时，获得了持续的药物释放曲线，并观察到增强的紫杉醇细胞毒性。此外，与未涂覆的PLGA纳米粒相比，由于透明质酸与CD44受体的相互作用，基于可能的受体介导的内吞作用，HA-PLGA纳米粒表现出改善的细胞摄取。纳米粒的非溶血潜力表明所开发的制剂适用于静脉给药。
