多孔材料ZIF-8的制备及其对布洛芬的载药性能  

Preparation of the porous ZIF-8 and the behaviors of loading ibuprofen

作　　者：孙瑞华 杨卓凡 张芮博 江奇[3] 卢晓英[2] 廖海[1] SUN Ruihua;YANG Zhuofan;ZHANG Ruibo;JIANG Qi;LU Xiaoying;LIAO Hai(School of Life Science and Engineering,Southwest Jiaotong University,Chengdu 610031,China;School of Medicine(Institute of Biomedical Engineering),Southwest Jiaotong University,Chengdu 610031,China;Key Laboratory of Magnetic Suspension Technology and Maglev Vehicle(Ministry of Education),Chengdu 610031,China)

机构地区：[1]西南交通大学生命科学与工程学院,成都610031 [2]西南交通大学医学院(生物医学工程研究院),成都610031 [3]磁浮技术与磁浮列车教育部重点实验室,成都610031

出　　处：《复合材料学报》2024年第12期6757-6764,共8页Acta Materiae Compositae Sinica

基　　金：国家自然科学基金(51602266);四川省重点研发项目(2021YFG2016);中央引导地方科技发展资金面上项目(2021ZYD0066);成都市技术创新研发项目(2022-YF05-00320-SN);大学生创新创业训练计划(SRTP2023187)。

摘　　要：难溶性药物的低溶解度,严重限制了其口服生物利用度。对此,结合金属-有机框架(MOFs)材料具有疏水性和高比表面积的特点,以溶液共沉淀法制备了MOF多孔材料ZIF-8作为载药基底。通过改变Zn^(2+)与2-甲基咪唑(2-methylimidazole)的摩尔比,进而对ZIF-8的比表面积及孔径分布进行调控,然后对难溶性药物布洛芬(IBP)的负载性能进行研究。研究结果表明:当Zn^(2+)与2-甲基咪唑的摩尔比为1:8时,材料ZIF-8(8)具有最大的比表面积和孔体积,分别为1187 m^(2)/g和1.183 cm^(3)/g,其对难溶性药物布洛芬的负载量高达21.8%。且药物载体复合材料IBP-ZIF-8(8)表现出良好的体外溶出度,在pH为2.5和7.4的磷酸缓冲溶液中,其累积溶出度均为98%左右。ZIF-8(8)处理的小鼠单核巨噬细胞白血病细胞(Mouse mononuclear macrophages cells,RAW246.7)存活率均高达94%以上,表现出良好的生物安全性。Oral bio avail ability of poorly soluble drugs is severely limited due to their low solubility.In recent years,metal-organic frameworks(MOFs)materials have attracted much attention because of their hydrophobicity and high specific surface area.In this paper,the porous ZIF-8,one of MOF family materials,were prepared by solution co-precipitation method.The specific surface area and pore size distribution of ZIF-8 were optimized by changing the molar ratio of Zn^(2+)to 2-methylimidazole.In addition,ZIF-8 were used as the carrier for ibuprofen(IBP),a poorly soluble drug,and its loading performance was studied in detail.The results showed that when the molar ratio of Zn^(2+)to 2-methylimidazole was 1:8,ZIF-8(8)had the largest specific surface area(1187 m^(2)/g)and pore volume(1.183 cm^(3)/g).And the loading capacity of ZIF-8(8)on IBP was as high as 21.8%.The drug carrier composite(IBPZIF-8(8))showed a well dissolution rate in vitro,and its cumulative dissolution rate was about 98%in phosphate buffer solution with pH of 2.5 and 7.4.The survival rate of RAW246.7 cells treated with IBP-ZIF-8(8)was over 94%,demonstrating satisfied biosafety.ZIF-8(8)with excellent specific surface area,pore volume,good loaded-IBP performance and biosafety has great potential applications in drug controlled-release system.

关 键 词：有机-金属框架物 ZIF-8 布洛芬 难溶性药物 口服生物利用度 

分 类 号：R318.08[医药卫生—生物医学工程] TB332[医药卫生—基础医学]