摘要
目的以金属-有机框架化合物UiO-66-NH_(2)为药物载体,负载甲硝唑(MTZ),探究UiO-66-NH_(2)负载甲硝唑的体外缓释的能力。方法采用核磁(1H-NMR)、红外光谱(IR)、差示扫描量热法(DSC)、氮气物理吸附-脱附(BET)、X射线衍射(XRD)对UiO-66-NH_(2)、MTZ@UiO-66-NH_(2)、R-MTZ@UiO-66-NH_(2)等MOFs材料进行表征。利用紫外-可见分光光度法(UV-vis)检测载药及缓释效率。结果1H-NMR结果证实用溶剂热法制备出药物载体UiO-66-NH_(2)。红外光谱、差示扫描量热法、氮气物理吸附-脱附表征结果表明,利用浸渍法成功将甲硝唑负载到UiO-66-NH_(2)孔道内。X射线衍射表征结果确定UiO-66-NH_(2)经过负载和缓释过程,晶体结构保持不变,骨架完整。紫外-可见分光光度法确定UiO-66-NH_(2)载药率为44.4%,在pH=7.4 PBS缓冲液(模拟人体血液pH环境)为体外缓释介质中,体外缓释时间长达83.5 h,缓释率为83.2%。结论实验结果证实,经UiO-66-NH_(2)负载后的甲硝唑体外缓释能力较纯甲硝唑体外缓释能力更强。UiO-66-NH_(2)可有效延长甲硝唑体外缓释时间,提高缓释效率,是一种具有潜在价值的药物载体。
Objective To explore loading ability of metal-organic framework UiO-66-NH_(2) as a drug carrier for metronidazole(MTZ)and its sustained release in vitro.Methods The MOFs(Metal-Organic Frameworks,MOFs)materials including UiO-66-NH_(2),MTZ@UiO-66-NH_(2),R-MTZ@UiO-66-NH_(2),etc.were characterized by 1H-Nuclear magnetic resonance(1H-NMR),infrared spectroscopy(IR),differential scanning calorimetry(DSC),nitrogen physical adsorption-desorption(BET)and X-ray diffraction(XRD).The drug loading and sustained-release efficiency of the carrier were detected by ultraviolet and visible spectrophotometry(UV-Vis).Results The 1H-NMR results confirmed that the drug carrier UiO-66-NH_(2) was prepared by solvothermal method.Infrared spectroscopy,differential scanning calorimetry,and nitrogen physical adsorption-desorption characterization results showed that metronidazole was successfully loaded into UiO-66-NH_(2) pores by impregnation method.The results of X-ray diffraction characterization confirmed that UiO-66-NH_(2) had the same crystal structure and complete skeleton after loading and slow-release process.The drug loading rate of UiO-66-NH_(2) was determined to be 44.4%.The release of MTZ from the carrier into the PBS buffer with pH of 7.4 as release medium can be sustainedas long as 83.5 hours with a drug release rate of 83.2%.Conclusion UiO-66-NH_(2) can effectively achieve the in vitro sustained-release of metronidazole and can be developed as a potentially valuable drug carrier.
作者
王萍萍
田鑫
茹丹丹
张建永
Wang Pingping;Tian Xin;Ru Dandan;Zhang Jianyong(School of Pharmacy,Zunyi Medical University,Zunyi Guizhou 563099,China;School of Pharmacy,Zunyi Medical University Key Laboratory of Basic Pharmacology of Ministry of Education,Zunyi Medical University,Zunyi Guizhou 563099,China)
出处
《遵义医科大学学报》
2023年第3期312-318,共7页
Journal of Zunyi Medical University
基金
贵州省教育厅青年科技人才成长项目,NO:黔教合KY字[2018]227
遵义市科技计划项目,NO:遵市科合HZ字(2021)288号
遵义医科大学2020年度学术新苗培养及创新探索专项项目,NO:黔科平台人才[2020]-014。
