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通过酰胺化反应在聚甲基丙烯酸环氧丙酯-g-聚乙二醇聚合物(PGMA-g-PEG)上修饰叶酸靶分子(FA).核磁共振(1H-NMR)和红外光谱(FTIR)测试表明成功合成了PGMA-g-(PEG)(FA)聚合物.利用该聚合物对量子点(QDs)进行配体交换形成水溶性量子点,再通过戊二醛及亚胺键键连的方式在水溶性量子点表面连接抗癌药物阿霉素(DOX)形成叶酸靶向的诊疗一体体系.紫外-可见光谱(UV-Vis)谱图显示该体系具有量子点和阿霉素的特征吸收峰,同时还出现了叶酸的特征吸收峰,由此说明了叶酸靶向的诊疗一体体系的成功制备.通过体外药物释放研究表明该体系具有较好的p H敏感性,在p H为5.0时具有较大的药物释放率,而在p H为7.4时较稳定,药物几乎得不到释放.通过He La细胞实验研究表明相比于诊疗体系,带有叶酸靶向的诊疗体系具有更大的细胞毒性,可以更好的被细胞所摄取,在细胞内形成较高浓度的量子点和阿霉素,可以更好的实现细胞的成像和肿瘤的治疗.
Folic acid target molecules (FA) were modified by amidation on poly (glycidyl methacrylate) -g-polyethylene glycol (PGMA-g-PEG) .The nuclear magnetic resonance (1H-NMR) and FTIR The results show that the PGMA-g- (PEG) (FA) polymer has been synthesized successfully, and the quantum dots (QDs) are exchanged with ligands to form water-soluble quantum dots by glutaraldehyde and imine linkages (DOX) on the surface of water-soluble quantum dots to form the therapeutic system of folic acid.Ultraviolet-Visible spectroscopy (UV-Vis) spectroscopy shows the system has the characteristics of quantum dots and doxorubicin Absorption peaks and the appearance of the characteristic absorption peak of folic acid.According to the successful preparation of the folate-targeted therapeutic system, the system has good p H sensitivity through in vitro drug release studies, Had a higher drug release rate and was more stable at pH 7.4 and almost no release of the drug.Experimental studies using HeLa cells showed that the treatment system with folate targeting was larger than the therapeutic system Cytotoxicity, can be better taken by the cells, the formation of a higher concentration of cells in the amount of Doxorubicin point and can achieve better imaging and therapy of tumor cells.