目的 合成靶向修饰型介孔硅纳米粒用作抗肿瘤药物传递载体,提高对肿瘤细胞的杀伤效力。方法 采用模板-水热法合成介孔硅,以氨基基团(NH2)、聚乙烯亚胺(PEI)进行结构修饰,包载药物盐酸多柔比星(DOX),考察新型纳米粒形态、粒度、红外吸收特征等,并以人乳腺癌MCF-7细胞为模型,对纳米载体的释药性能、细胞摄取、体外抗肿瘤活性进行评价。结果 未修饰型介孔硅(MSNs)与2种修饰型纳米粒(MSNs-NH2、MSNs-PEI)为类球形颗粒,粒径分别为(65±19)、(86±27)和(107±34) nm,红外光谱、差热分析(DSC)等结果证实MSNs表面被功能化基团成功修饰。MSNs-NH2与MSNs-PEI的释药速度比未修饰型MSNs明显降低,3种纳米粒(MSNs、MSNs-NH2和MSNs-PEI)的细胞摄取效率分别为DOX溶液的2.05,2.89和2.63倍,对MCF-7细胞的杀伤力分别为1.77、2.21和2.19倍。结论 使用该方法可成功制得介孔硅纳米载体,修饰型MSNs具有更优良的的载体性能与抗肿瘤活性。
Abstract
OBJECTIVE To prepare mesoporous silica nanoparticles (MSNs) modified by targeted ingredients to improve the tumor cell lethality of antitumor drugs. METHODS MSNs were prepared by template-hot water method, and modified with amino group and polyethyleneimine. The nano-carriers were characterized by their morphology, particle size and infrared absorption. Meanwhile, the intracellular uptake and in vitro antitumor activity of MSNs were evaluated on human breast carcinoma cell line (MCF-7). RESUTLS Three kinds of nanoparticles, MSNs, MSNs-NH2 and MSNs-PEI were all spherical, with mean diameters of (65±19), (77±17) and (117±21) nm, respectively. Infrared spectrum and differential thermal analysis results indicated that the functional groups were linked onto the surface of MSNs, and slower drug release was observed for MSNs-NH2 and MSNs-PEI. Moreover, the cellular uptake of three nanoparticles were 2.05, 2.89, and 2.63 times higher than free doxorubicin, and the cytotoxicity activity against MCF-7 cells were 1.77, 2.21, and 2.19 times, respectively. CONCLUSION The preparation method can be used to prepare MSNs nano-carriers. MSNs-NH2 and MSNs-PEI have improved carrier property and antitumor activity.
关键词
介孔硅 /
纳米载体 /
靶向修饰 /
盐酸多柔比星 /
抗肿瘤
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Key words
mesoporous silica nanoparticle /
nano-carriers /
targeting modification /
doxorubicin /
antitumor
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中图分类号：
R944
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参考文献
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脚注
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基金
河南省科技厅科技攻关项目资助(172102310430)
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