叶酸修饰的聚(N-羟丙基甲基丙烯酰胺)-巯基嘌呤纳米粒子的制备和细胞毒性研究  

Preparation and cytotoxicity study of folic acid-modified poly(N-hydroxypropylmethacrylamide)-mercaptopurine nanoparticles

作　　者：狄钰馨 张加 赵敏智 龙海涛[1] 许卫兵 DI Yuxin;ZHANG Jia;ZHAO Minzhi;LONG Haitao;XU Weibing(College of Science,Gansu Agricultural University,Lanzhou 730070,China)

机构地区：[1]甘肃农业大学理学院,甘肃兰州730070

出　　处：《甘肃农业大学学报》2022年第6期33-42,共10页Journal of Gansu Agricultural University

基　　金：甘肃省自然科学基金项目(20JR10RA511);甘肃省高等学校创新能力提升项目(2019B-084)。

摘　　要：【目的】制备高效的聚合物抗癌药物输送系统,探究其对细胞活性的影响。抗癌药物6-巯基嘌呤(6MP)通过对谷胱甘肽敏感的前药(PTA)连接物共价结合到聚N-2-羟丙基甲基丙烯酰胺(HPMA)的-OH基团上,选择叶酸(FA)作为癌细胞靶向基团制备了聚(HPMA)-PTA、聚(HPMA)-FA-PTA两种聚合物。【方法】利用傅立叶变换红外光谱分析、热重分析、紫外分析、扫描电镜等对其化学组成进行了表征。【结果】两种复合物呈直径约为100~150 nm的球形粒子,采用MTT法和流式细胞仪对所制备的聚合物进行细胞毒性分析,证实产物具有良好的抗癌作用。【结论】聚(HPMA)-PTA、聚(HPMA)-FA-PTA聚合物具有明显的靶向性和抗肿瘤作用,表现出良好的生物应用前景。【Objective】The aim of this study was to prepare an efficient polymeric anticancer drug delivery system and to investigate its effect on cell activity.The anticancer drug 6-MP was covalently bonded to the-OH group of poly-HPMA through the carbonyl sulfide vinyl linker of glutathione reaction,and two polymers HPMA-PTA and polymers HPMA-FA-PTA were prepared.【Method】The structures of the two complexes were characterised by Fourier transform infrared spectroscopy,thermogravimetric analysis,UV analysis and scanning electron microscopy.【Result】The two complexes were spherical particles with a diameter of about 100~150 nm.The cytotoxicity analysis of the prepared polymers was performed by MTT method and flow cytometry,which confirmed the good anticancer effects of the products.【Conclusion】Poly(HPMA)-PTA and poly(HPMA)-FA-PTA polymers have obvious targeting and antitumour effects.It shows a good prospect of biological application.

关 键 词：抗癌药物 聚(HPMA)-PTA 聚(HPMA)-FA-PTA 细胞毒性 

分 类 号：TQ464.2[化学工程—制药化工]