热碱解改性UiO-66材料对槲皮素的装载、释放及抗氧化作用研究  

Study on release and antioxidant activity of quercetin after loaded by hot alkali hydrolysis modified UiO-66 material

作　　者：畅瑞苗[1,2,3] 张艳洋 康安娟 张广彬 余彦平[1] 任俊照 陈安家 李勇[2,3] CHANG Rui-miao;ZHANG Yan-yang;KANG An-juan;ZHANG Guang-bin;YU Yan-ping;REN Jun-zhao;CHEN An-jia;LI Yong(School of Pharmacy,Shanxi Medical University,Taiyuan 030001,China;Shanxi Bethune Hospital(Shanxi Academy of Medical Sciences,Tongji Shanxi Hospital),Third Hospital of Shanxi Medical University,Taiyuan 030032,China;Tongji Hospital,Tongji Medical College,Huazhong University of Science and Technology,Wuhan 430030,China;Shanxi Liye Pharmaceutical Co.,Ltd.,Taiyuan 030021,China)

机构地区：[1]山西医科大学药学院,山西太原030001 [2]山西白求恩医院(山西医学科学院同济山西医院),山西医科大学第三医院,山西太原030032 [3]华中科技大学同济医学院附属同济医院,湖北武汉430030 [4]山西立业制药有限公司,山西太原030021

出　　处：《药学学报》2023年第9期2802-2810,共9页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(32200323);山西省基础研究计划(20210302124190)。

摘　　要：UiO-66(University of Oslo 66)可以提高难溶性中药活性成分的释放率和生物利用度,是一种具有临床应用前景的金属有机骨架材料。然而原型UiO-66对槲皮素的装载不理想。将UiO-66置于碱性溶液中加热后获得了“热”碱解改性材料UiO-66-BH(UiO-66-blend-heating)。UiO-66-BH维持着UiO-66八面体结构的轮廓,但表面出现明显粗糙不平的孔隙。UiO-66-BH对槲皮素的饱和吸附量为138.92 mg·g^(-1),对槲皮素的吸附属于单分子层吸附,吸附过程受控于化学吸附作用。UiO-66-BH可控制槲皮素在模拟胃肠液中的释放,并在长时间释放后模拟肠液中药物浓度明显高于原料药(36%vs 9%)。与槲皮素相比,载有槲皮素的UiO-66-BH@槲皮素载药系统对2,2′-联氮双(3-乙基苯并噻唑啉-6-磺酸)二铵盐(2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic acid)ammonium salt,ABTS)自由基的清除能力有所下降,而对1,1-二苯基-2-苦味基肼(1,1-diphenyl-2-picrylhydrazyl,DPPH)自由基的清除能力几乎不变,显示了载药系统类似槲皮素的抗氧化作用。研究表明,本文合成的UiO-66-BH可控制槲皮素在模拟胃肠液中的释放,有望改善槲皮素的生物利用度。UiO-66(University of Oslo 66)is a kind of promising material that can improve the release and bioavailability of poorly water-soluble bioactive compounds of traditional Chinese medicine.However,the loading of quercetin in raw UiO-66 was not ideal.In this study,UiO-66-BH(UiO-66-blend-heating)was obtained by heating UiO-66 and KOH solution following blended them.UiO-66-BH maintained the outline of octahedral structure of UiO-66 but with obvious rough and uneven pores on the surface.UiO-66-BH had good adsorption of quercetin with saturation adsorption was 138.92 mg·g^(-1),the adsorption process belonged to single molecular layer adsorption and was controlled by chemisorption.UiO-66-BH can control the release of quercetin in simulated gastrointestinal fluid,and the drug concentration was significantly higher than that of free quercetin after long-term release(36%vs 9%).Compared with quercetin,the ABTS(2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic acid)ammonium salt)radical scavenging activity of UiO-66-BH@quercetin drug delivery system decreased,while the DPPH(1,1-diphenyl-2-picrylhydrazyl)radical scavenging activity remained almost unchanged.The drug delivery system showed a strong antioxidant effect similar to quercetin.The findings indicated that UiO-66-BH could control release of quercetin and was expected to be used as a drug carrier material for some insoluble active components of traditional Chinese medicine such as quercetin.

关 键 词：槲皮素 UiO-66 热碱解技术 吸附行为 抗氧化活性 体外释放 

分 类 号：R944[医药卫生—药剂学]