pH响应性羧甲基化纤维素微球原位生长UiO-66及用于双氯芬酸钠的控释OA
In situ growth of UiO-66 on pH-responsive carboxymethylated cellulose microspheres for controlled release of diclofenac sodium
首先通过氯乙酸钠与纤维素微球(CM)进行醚化反应制备羧甲基化纤维素微球(CMC-M),然后以CMC-M为生物聚合物骨架原位生长锆基金属有机骨架(UiO-66),成功制备了锆基金属有机框架/羧甲基化纤维素复合微球(UiO-66@CMC-M),并以双氯芬酸钠(DCF)为模型药物研究了其药物负载和控释能力.通过扫描电子显微镜、能量色散X射线光谱、傅里叶变换红外光谱、X射线衍射和热重分析等表征证实了UiO-66晶体围绕CMC-M骨架的成功复合,且CMC-M上的羧基可能与UiO-66的Zr4+节点发生配位键合.药物负载实验表明DCF的负载主要受物理和化学吸附共同控制,且为单层吸附.体外释放研究证实了 DCF@UiO-66@CMC-M的 pH响应性控释能力.在模拟胃酸条件(pH=1.2)下,DCF在 70 h累计释放约24%,而在模拟肠道条件(pH=7.4)下,70 h 累计释放约 80%.释放动力学拟合结果显示,药物释放遵循Korsmeyer-Peppas模型,且释放机制符合Fickian扩散.细胞毒性实验进一步证实了UiO-66@CMC-M具有良好的生物相容性和极低的细胞毒性.本研究为设计一种DCF的新型控释载体提供了理论依据.
Carboxymethylated cellulose microspheres(CMC-M)were first synthesized via etherification of cellulose microspheres(CM)with sodium chloroacetate.Subsequently,zirconium-based metal-organic framework UiO-66 was grown in situ onto the CMC-M biopolymer backbone to successfully fabricate UiO-66@CMC-M composite microspheres.The drug loading and controlled release performance of the composite were then evaluated using diclofenac sodium(DCF)as a model drug.Characterization results from scanning electron microscopy,energy-dispersive X-ray spectroscopy,Fourier-transform infrared spectroscopy,X-ray diffraction,and thermogravimetric analysis confirmed the successful integration of UiO-66 crystals on the CMC-M framework,suggesting potential coordination bonding between the carboxyl groups on CMC-M and the Zr4+nodes of UiO-66.Drug loading experiments indicated that DCF loading was governed by a combination of physical and chemical interactions,leading to monolayer adsorption.In vitro release studies demonstrated pH-responsive controlled release behavior of DCF@UiO-66@CMC-M.Under simulated gastric fluid(pH=1.2),the cumulative release of DCF was approximately 24%over 70 h,whereas it reached approximately 80%under simulated intestinal fluid(pH=7.4).Kinetic fitting revealed that the drug release profile followed the Korsmeyer-Peppas model,with the mechanism consistent with Fickian diffusion.Cytotoxicity assays further confirmed that UiO-66@CMC-M possesses excellent biocompatibility and negligible cytotoxicity.This study provides a theoretical foundation for the design of novel controlled-release carriers for DCF.
彭晨俊男;罗晓刚
武汉工程大学化工与制药学院,绿色化工过程教育部重点实验室(武汉工程大学),湖北 武汉 430205武汉工程大学化工与制药学院,绿色化工过程教育部重点实验室(武汉工程大学),湖北 武汉 430205
资源环境
羧甲基化纤维素微球UiO-66原位合成双氯芬酸钠控释载体
carboxymethyl-modified cellulose microsphereUiO-66in situ synthesisdiclofenac sodiumcontrolled release carrier
《武汉工程大学学报》 2026 (2)
149-158,10
湖北省重点研发计划项目(2022BAB109,2024BEB002)
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