基于PEG-PLGA和CMCS载体制备白藜芦醇纳米粒在结肠癌治疗中的应用＊

目的 为了提高白藜芦醇（Resveratrol,RES）的生物利用度,将其制备成纳米粒子,并研究其体外抗结肠癌的作用。方法 分别以聚乙丙交酯聚乙二醇共聚物（PEG-PLGA）和羧甲基壳聚糖（Carboxymethyl chitosan,CMCS）作为药物载体,采用纳米沉淀法和乳化交联法分别制备了PEG-PLGA共载白藜芦醇纳米粒（RES-PEG-PLGA NPs）和CMCS共载白藜芦醇纳米粒（RES-CMCS NPs）,利用紫外分光光度计、激光粒度分析仪和透射电子显微镜等仪器对纳米粒的理化性质进行表征;采用CCK-8检测法测定纳米粒对人结肠癌细胞（SW480）的抗增殖活性,并通过荧光显微镜考察了纳米粒在SW480细胞中的摄取。结果 RES-PEG-PLGA NPs粒径为78.67 ± 1.0 nm,包封率为87%;RES-CMCS NPs粒径为231 ± 1.6 nm,包封率为60%。结论 两种纳米粒在模拟肿瘤微环境下均能实现白藜芦醇的缓释,都可以有效地被SW480细胞摄取,并且对SW480细胞表现出较高的抑制作用。

Resveratrol-loaded Nanoparticles Based on PEG-PLGA and CMCS for the Treatment of Colorectal Cancer

Objective To improve the bioavailability of resveratrol (RES), resveratrol nanoparticles were prepared to study their anti-colon cancer effects in vitro.Methods PEG-PLGA co-loaded RES nanoparticles (RES-PEG-PLGA NPs) and CMCS co-loaded RES nanoparticles (RES-CMCS NPs) were prepared by nano-precipitation method and emulsification cross-linking method using polyethylene glycol copolymer (PEG-PLGA) and carboxymethyl chitosan (CMCS) as drug carriers, respectively. The physical and chemical properties of nanoparticles were characterized by ultraviolet spectrophotometer, laser particle size analyzer and transmission electron microscopy. The antiproliferative activity of nanoparticles against human colon cancer cells (SW480 cells) was determined by CCK-8 assay. The cell uptake of nanoparticles in SW480 cells was investigated by fluorescence microscopy.Results The particle size of RES-PEG-PLGA NPs was 78.67 ± 1.0 nm and the encapsulation efficiency was 87%. The particle size of RES-CMCS NPs was 231 ± 1.6 nm and the encapsulation efficiency was 60%.Conclusion Both nanoparticles achieved the sustained release of the RES under simulated tumor environment and had a high inhibition rate on SW480 cells with an effective uptaking by SW480 cells.