| 李东昱,肖圆媛,刘礼煌,蒋福匀,邵佳慧,李丽,刘宇.化学通报,2025,88(11):1208-1213,1220. |
| ZIF-8载双氯芬酸钾pH响应递药系统研究 |
| Study on pH - Responsive Drug - Delivery System of ZIF - 8 Loaded with Potassium Diclofenac |
| 投稿时间：2025-06-17 修订日期：2025-07-12 |
| DOI： |
| 中文关键词: 双氯芬酸钾 金属有机 ZIF-8 MOF 计算机辅助药物设计 |
| 英文关键词:diclofenac potassium, Metal-organic framework, ZIF-8, MOF, Computer aided drug design |
| 基金项目:第十三届大学生创新创业大赛项目研究支持 |
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| 中文摘要: |
| 本文旨在探索沸石咪唑酯骨架-8(ZIF-8)包裹双氯芬酸钾的制备方法及其性能，并通过计算机辅助设计阐明药物与载体之间的相互作用机制，以开发一种新型的pH响应性药物系统。通过溶剂热法合成了ZIF-8，测得合成的ZIF-8的粒径为153.5±4.19nm及Zeta电位27.5±3.31mv。利用上述ZIF-8进行初步载药实验，通过红外光谱证实了双氯芬酸钾成功负载于ZIF-8中，随后采用星点设计-效应面法优化载药条件，结果表明，当双氯芬酸钾与ZIF-8的质量比为1:1、反应温度为35℃、反应时间为3h，载药率达到最大值24.92%。体外释放实验显示，DCFP@ZIF-8在人工胃液中，12h就释放了接近85%的药物，24h达到释放平衡；在人工肠液中，48h释放了接近80%的药物；在生理盐水中48h释放接近75%。通过计算机辅助设计验证双氯芬酸钾与ZIF-8之间C-H···O、Cl···H、K···H等一系列价键之间强相互作用使其在ZIF-8中稳定负载，并在不同pH环境下表现出差异化的释放行为，ZIF-8在中性和碱性环境中稳定，抑制药物释放，而在酸性胃液中则加速释放。本研究为开发具有pH响应性的药物系统提供了实验依据，并为双氯芬酸钾的临床应用提供了新的思路。 |
| 英文摘要: |
| This study explores preparing potassium diclofenac encapsulated in ZIF-8 and its properties, elucidating the drug-carrier interaction mechanism via computer-aided design to develop a novel pH-responsive drug delivery system. ZIF-8 was synthesized solvothermally, exhibiting a particle size of 153.5±4.19nm and Zeta potential of 27.5±3.31mv. Preliminary loading confirmed encapsulation via infrared spectroscopy. Drug loading was optimized using central composite design-response surface methodology, revealing maximum loading efficiency of 24.92% at a 1:1 mass ratio (drug:ZIF-8), 35°C, and 3 hours. In vitro release showed DCFP@ZIF-8 released nearly 85% within 12h in simulated gastric fluid, equilibrating at 24h; released nearly 80% within 48h in simulated intestinal fluid; and released nearly 75% within 48h in saline. Computer-aided design verified strong interactions (C-H··O, Cl··H, K··H bonds) ensure stable loading and differential pH-dependent release. ZIF-8 remains stable in neutral/alkaline environments, inhibiting release, but accelerates in acidic gastric fluid. This research provides evidence for pH-responsive systems and offers new insights for diclofenac potassium"s clinical application. |
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