Department of Experimental Surgery, McGill University, Montreal, QC H3H1P3, Canada.
J Biomater Sci Polym Ed. 2013;24(5):574-88. doi: 10.1080/09205063.2012.700111. Epub 2012 Aug 13.
This study aims at modifying the synthesis method of preparing N-isopropylacrylamide (NIPAAM)/N-vinyl-2-pyrrolidone (VP)/Polyethylene glycol monoacrylate (PEG-A) polymeric nanoparticles encapsulating curcumin as a model drug. The optimal concentration of nanoparticle reagents was determined using Fourier Transform Infrared Spectroscopy. Curcumin nanoparticles mean hydrodynamic size was found to be 104 nm with zeta potential of 3 ± 13 mV. The release kinetic study of curcumin nanoparticles indicates that a maximum release of curcumin at 24 h positively correlates with increase in temperature; however, change in pH did not produce any substantial drug release. In vitro cell viability assay performed on cancer cells exposed to various concentrations of model compound displayed the IC50 ranging between 100 and 200 μg/mL for human prostate cancer cells (PC3 cells) and 50 and 200 μg/mL for epidermoid carcinoma (A431 cell line). The Hoechst staining and phase contrast micrographs for 48 h exposure of curcumin nanoparticles at a concentration of 400 μg/mL resulted in almost 92% of cells death in both cell lines. This study concludes that the physiochemical characteristics of NIPAAM/VP/PEG-A polymer with key features of water solubility, sustained drug release, small particle size make these nanoparticles a prominent drug delivery device.
本研究旨在改进制备载姜黄素的 N-异丙基丙烯酰胺（NIPAAM）/N-乙烯基-2-吡咯烷酮（VP）/聚乙二醇单丙烯酸酯（PEG-A）聚合物纳米粒子的合成方法。采用傅里叶变换红外光谱法确定纳米粒子试剂的最佳浓度。发现姜黄素纳米粒子的平均水动力粒径为 104nm，zeta 电位为 3±13mV。姜黄素纳米粒子的释放动力学研究表明，在 24 小时内，姜黄素的最大释放量与温度的升高呈正相关；然而，pH 值的变化并没有导致药物的实质性释放。对暴露于不同浓度模型化合物的癌细胞进行的体外细胞活力测定显示，人前列腺癌细胞（PC3 细胞）的 IC50 值在 100 至 200μg/ml 之间，表皮样癌细胞（A431 细胞系）的 IC50 值在 50 至 200μg/ml 之间。在浓度为 400μg/ml 时，姜黄素纳米粒子暴露 48 小时的 Hoechst 染色和相差显微镜照片显示，两种细胞系中几乎有 92%的细胞死亡。本研究得出结论，NIPAAM/VP/PEG-A 聚合物的物理化学特性具有水溶性、持续药物释放、粒径小等关键特征，使这些纳米粒子成为一种突出的药物递送装置。
