铜/腺嘌呤金属有机框架的制备并用作药物载体性能的研究  

Preparation of Copper/Adenine Metal-Organic Framework and Its Performance as Drug Carrier

作　　者：李婉萌 赵亮 陈进 刘薇 Li Wanmeng;Zhao Liang;Chen Jin;Liu Wei(School of Pharmacy,Jinzhou Medical University,Jinzhou,Liaoning 121000,China)

机构地区：[1]锦州医科大学药学院,辽宁锦州121000

出　　处：《化学世界》2023年第4期249-256,共8页Chemical World

基　　金：辽宁省教育厅课题(No.JYTJCZR2020067)资助项目。

摘　　要：盐酸小檗碱(BRH)是一种异喹啉类生物碱,具有很强的生物和药理活性,但由于其水溶性差、半衰期短、生物利用度低,导致其在临床应用中受限。采用金属有机框架(Cu-MOF)作为载体材料负载BRH,以提高其生物利用度。Cu-MOF采用了安全简单、低成本的加热搅拌法合成,通过扫描电子显微镜(SEM)、X射线光电子能谱分析(XPS)、X射线衍射(XRD)、傅里叶变换红外光谱仪(FT IR)等对Cu-MOF材料进行表征,并对Cu-MOF材料进行载药以及体外释放实验。以巨噬细胞作为细胞模型,进行噻唑蓝(MTT)实验,结果显示Cu-MOF材料结构完整、大小均匀,Cu-MOF@BRH的载药量为(48±2.41)%,缓释作用明显,48 h累计释放率为53%,适合作为BRH的药物载体。细胞毒性实验结果显示,Cu-MOF材料中金属离子水平保持在生物用途允许的限度内且生物相容性良好。Cu-MOF材料安全可靠,作为药物载体使用,具有良好的发展前景。Berberine hydrochloride(BRH)is a kind of isoquinoline alkaloid with strong biological and pharmacological activity.However,due to its poor water solubility,short half-life and low bioavailability,its clinical application is limited.The purpose of this paper is to use the newly synthesized metal-organic framework(Cu-MOF)as carrier to load BRH for improving its bioavailability.Cu-MOF was synthesized using a safe,simple and low-cost heating/stirring method,and was characterized by scanning electron microscope(SEM),X-ray photoelectron spectroscopy(XPS),X-ray diffraction(XRD)and Fourier transform infrared spectroscopy(FT IR).Moreover,drug loading and in vitro release experiments on Cu-MOF were performed.Using macrophages as cell model,MTT assay experiments were conducted and the results showed that Cu-MOF possesses a well-defined structure and uniform size.The drug loading amount of Cu-MOF@BRH was(48±2.41)%with an obvious sustained release.The cumulative release rate at 48 h was~53%,which is suitable as drug carrier for BRH.The cytotoxicity results showed that the metal ion level in Cu-MOF remained within the allowable limit for biological use with good biocompatibility.Cu-MOF is safe and reliable so that it can be used as drug carrier with good prospect.

关 键 词：金属有机框架 盐酸小檗碱 药物载体 药物缓释 

分 类 号：R94[医药卫生—药剂学]