Kumar Sathish Sundar Dhilip, Surianarayanan Mahadevan, Vijayaraghavan R, Mandal Asit Baran, MacFarlane D R
Thermo Chemical Lab, Chemical Engineering Department, Central Leather Research Institute, Chennai 600 020, India.
Eur J Pharm Sci. 2014 Jan 23;51:34-44. doi: 10.1016/j.ejps.2013.08.036. Epub 2013 Sep 5.
The main focus of this study is to encapsulate hydrophobic drug curcumin in hydrophilic polymeric core such as poly(2-hydroxyethyl methacrylate) [PHEMA] nanoparticles from gelled ionic liquid (IL) to improve its efficacy. We have achieved 26.4% drug loading in a biocompatible hydrophilic polymer. Curcumin loaded PHEMA nanoparticles (C-PHEMA-NPs) were prepared by nano-precipitation method. Scanning electron microscopy (SEM) and atomic force microscopy (AFM) analysis showed that the prepared nanoparticles were spherical in shape and free from aggregation. The size and zeta potential of prepared C-PHEMA-NPs were about 300 nm and -33.4 mV respectively. C-PHEMA-NPs were further characterized by FT-IR spectroscopy which confirmed the existence of curcumin in the nanoparticles. X-ray diffraction and differential scanning calorimetry studies revealed that curcumin present in the PHEMA nanoparticles were found to be amorphous in nature. The anticancer activity of C-PHEMA-NPs was measured in ovarian cancer cells (SKOV-3) in vitro, and the results revealed that the C-PHEMA-NPs had better tumor cells regression activity than free curcumin. Flow cytometry showed the significant reduction in G0/G1 cells after treatment with C-PHEMA-NPs and molecular level of apoptosis were also studied using western blotting. Toxicity of PHEMA nanoparticles were studied in zebrafish embryo model and results revealed the material to be highly biocompatible. The present study demonstrates the curcumin loaded PHEMA nanoparticles have potential therapeutic values in the treatment of cancer.
本研究的主要重点是将疏水性药物姜黄素包裹在亲水性聚合物核中,例如由凝胶离子液体(IL)制备的聚甲基丙烯酸2-羟乙酯[PHEMA]纳米颗粒,以提高其疗效。我们在一种生物相容性亲水性聚合物中实现了26.4%的药物负载量。通过纳米沉淀法制备了负载姜黄素的PHEMA纳米颗粒(C-PHEMA-NPs)。扫描电子显微镜(SEM)和原子力显微镜(AFM)分析表明,所制备的纳米颗粒呈球形且无聚集。所制备的C-PHEMA-NPs的尺寸和zeta电位分别约为300 nm和-33.4 mV。通过傅里叶变换红外光谱(FT-IR)对C-PHEMA-NPs进行了进一步表征,证实了纳米颗粒中存在姜黄素。X射线衍射和差示扫描量热法研究表明,PHEMA纳米颗粒中的姜黄素呈无定形。在体外对卵巢癌细胞(SKOV-3)测定了C-PHEMA-NPs的抗癌活性,结果表明C-PHEMA-NPs比游离姜黄素具有更好的肿瘤细胞消退活性。流式细胞术显示用C-PHEMA-NPs处理后G0/G1期细胞显著减少,并且还使用蛋白质印迹法研究了凋亡的分子水平。在斑马鱼胚胎模型中研究了PHEMA纳米颗粒的毒性,结果表明该材料具有高度生物相容性。本研究表明负载姜黄素的PHEMA纳米颗粒在癌症治疗中具有潜在的治疗价值。