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功能化石墨烯负载毛萼乙素抗肿瘤制剂的研究
Functionalized Graphene Oxide as a Nanocarrier for Loading and Delivering of Eriocalyxin B
【摘要】 首先通过改进的Hummers法制备了氧化石墨烯(GO),然后通过酰胺化反应将端基为氨基的六臂聚乙二醇(PEG)连接到氧化石墨烯的表面,以改善其水溶性和生物相容性.原子力显微镜(AFM)数据表明所制备的GO-PEG的尺寸小于250 nm,稳定性试验证明GO-PEG在水和PBS缓冲液中可以很好地分散.利用制备的GO-PEG作为药物载体,通过物理共混的方法负载了疏水性抗肿瘤药物——毛萼乙素.紫外光谱法测得载药率为18.8%.选择肺癌细胞A549和乳腺癌细胞MCF-7对载药体系的细胞毒性进行了研究,结果表明即使在高达100 mg/L的浓度下培养48 h,GO-PEG载体对两种细胞仍然具有很小的毒性(相对细胞存活率>85%),而通过载体负载毛萼乙素后的疗效有所增强,对癌细胞具有更大的杀伤作用.
【Abstract】 Graphene oxide(GO) was firstly prepared by modified Hummers method. In order to improve its water solubility and biocompatibility, 6-arm PEG was grafted to GO via a facile amidation reaction. The size of obtained GO-PEG was less than 250 nm. Stability test indicated the good dispersibility of GO-PEG in water and PBS buffer. Furthermore, eriocalyxin B, a widely used cancer chemotherapy drug, is adsorbed onto GO-PEG via physical blending with a drug loading ratio of 18.8% obtained by UV spectrum. Lung cancer cell A549 and breast cancer cell MCF-7 were selected to study the cytotoxicity of GO-PEG/eriocalyxin B, GO-PEG, and free eriocalyxin B. The results demonstrated that GO-PEG nano-carrier possessed low toxicity(relative cell viability>85%), even cultivated for 48 h at a relatively high concentration of 100 mg/L. Compared to pure drug, GO-PEG/eriocalyxin B nanocarrier shows higher cytotoxicity in A549 and MCF-7 cells.
【Key words】 graphene oxide; eriocalyxin B; drug delivery; cell viability;
- 【文献出处】 有机化学 ,Chinese Journal of Organic Chemistry , 编辑部邮箱 ,2013年10期
- 【分类号】TQ463
- 【被引频次】17
- 【下载频次】291