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
-
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。Abstract: 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.
下载: