靶向和酶响应纳米钻石载药体系的制备及细胞转运机制

发布时间：2018-04-10 14:27

本文选题：纳米钻石 + 甲氨蝶呤　；参考：《山西大学学报(自然科学版)》2017年03期

【摘要】：通过共价键合方法将叶酸配体和化疗药物甲氨蝶呤偶联于PEG化的纳米钻石载体上,获得纳米钻石-PEG-叶酸/甲氨蝶呤(ND-PEG-FA/GLY-MTX,NPFGM)药物输送体系。采用紫外-可见吸收光谱法测定了纳米钻石表面偶联甲氨蝶呤的量为(123±5.8)μg/mg。通过体外释药研究,表明NPFGM纳米颗粒在生理条件下具有良好的稳定性,而在微酸性溶菌酶存在下,酯键水解断裂导致药物甲氨蝶呤被催化释放。以乳腺癌细胞为模型,采用流式细胞技术表明细胞摄取纳米钻石药物体系主要通过小窝蛋白-决定、叶酸受体介导的靶向机制进入细胞。这些研究结果表明NPFGM是一个很有前途的药物递送平台,并为共价偶联药物提供新思路。
[Abstract]:The amount of coupling methotrexate on the surface of nanocrystalline diamond was determined by UV-Vis absorption spectrometry to be 123 卤5.8 渭 g / mg.The results of drug release in vitro showed that NPFGM nanoparticles had good stability under physiological conditions, but in the presence of micro-acid lysozyme, the hydrolysis of ester bond resulted in the catalytic release of methotrexate.Using breast cancer cells as a model, flow cytometry showed that the uptake of nanocrystalline drugs by cells was mainly mediated by fossa protein-dependent and folate receptor-mediated targeting mechanism.These results suggest that NPFGM is a promising drug delivery platform and provide new ideas for covalent coupling drugs.
【作者单位】：山西大学化学化工学院;
【基金】：国家自然科学基金(21071091) 山西省科技攻关计划(社会发展)(20130313021-1;201603D321025)
【分类号】：TB383.1;TQ460.1

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