聚乙二醇修饰的超顺磁性氧化铁纳米粒的制备及体外评价  

Preparation and in vitro evaluation of PEG-coated superparamagnetic iron oxide nanoparticles

作　　者：周丽君[1,2] 刘建平[1] 熊非[2] 陈跃坚 黄蓉蓉[2] 顾宁[2] 

机构地区：[1]中国药科大学药剂学教研室,南京210009 [2]东南大学生物科学与医学工程学院,南京210009 [3]南京圣和药业有限公司,南京210018

出　　处：《中国药科大学学报》2013年第4期316-320,共5页Journal of China Pharmaceutical University

基　　金：国家重点基础研究发展计划("九七三"计划)资助项目(No.2011CB933503);国家"重大新药创制"科技重大专项资助项目(No.2009ZX09310-004)~~

摘　　要：采用透析法制备以聚乙二醇(PEG)为亲水端,油酸(OA)为亲脂端,赖氨酸(Lys)为连接段的mPEG-Lys-OA2(PLO)修饰的超顺磁性氧化铁纳米粒(PLO-SPIO NPs)。分别采用透射电镜、动态光散射法对制得的PLO-SPIO NPs的形态和粒径进行表征;通过邻二氮菲显色法测定制剂中铁浓度;用振动样品磁强计测定制剂的饱和磁化强度,并绘制磁滞回线;以二巯基丁二酸修饰的超顺磁性氧化铁纳米粒(DMSA-SPIO NPs)为对照,考察RAW264.7巨噬细胞对相同铁浓度的PLO-SPIO NPs的吞噬情况,通过四唑单钠盐(CCK-8)法检测细胞活力。结果表明,制得的PLO-SPIO NPs近似呈球形,平均粒径为(89.6±2.3)nm,多分散指数为0.107;铁浓度为(221.91±1.9)μg/mL;饱和磁化强度为58.94 emu/g,磁滞回线证明PLO-SPIO NPs具有良好的超顺磁性;细胞实验结果显示RAW264.7巨噬细胞对DMSA-SPIO NPs的摄入量显著高于PLO-SPIO NPs(P<0.05)。上述数据表明,制备的PLO-SPIO NPs能够有效地躲避网状内皮系统的吞噬,延长血液循环时间,具有良好的应用前景。Based on the mPEG-Lys-OA2 which consisted of hydrophilic methyl-polyethylene glycol,hydrophobic oleinic acid and lysine as connecting arm,mPEG-Lys-OA2-coated superparamagnetic iron oxide nanoparticles（PLO-SPIO NPs） were prepared by dialysis method and the mPEG-Lys-OA2 was synthesized by our research group.Transmission electron microscopy（TEM） and dynamic light scattering（DLS） were employed respectively to characterize the morphology and size of the PLO-SPIO NPs.The concentration of iron was determined by phenanthroline spectrophotometry.The saturation magnetization was measured by vibrating sample magnetometer（VSM）,and hysteresis loop was drawn.RAW264.7 macrophages were cultured in the presence of DMSA-SPIO NPs as control and PLO-SPIO NPs.CCK-8 assay was applied to detect the cell viability.The results showed that the PLO-SPIO NPs was quasi-spherical,and that the mean hydrodynamic size and polydispersity index（PDI） were（89.6±2.3） nm and 0.107,respectively.The concentration of iron was（221.91±1.9） μg/mL,and the superparamagnetism was conformed by the hysteresis loop with the saturation magnetization of 58.94 emu/g.It was also found that the iron amount swallowed by the RAW264.7 macrophages was significantly lower than the control（P0.05）.Consequently,the PLO-SPIO NPs prepared in this study could significantly reduce the uptake of the RES,prolong their circulation time and offer a potential promise for cancer therapy in future.

关 键 词：磁性纳米粒 油酸 赖氨酸 聚乙二醇 修饰 超顺磁性 制备 评价 

分 类 号：R944[医药卫生—药剂学]