β-环糊精金属有机框架作为一种绿色载体,可提高叶黄素的溶解度、生物利用度和肝脏保护作用

IF 5.2 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Dan Yang , Min Zhao , Yihe Huang , Liwen Chen , Jiqin Fang , Jiaonan Liu , Miao Wang , Chunjie Zhao
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引用次数: 0

摘要

对乙酰氨基酚诱发肝损伤的发病率有所上升,但有效的预防方法却很有限。虽然木犀草素具有保肝活性,但其溶解度和生物利用度较低,限制了其应用。环糊精金属有机框架(CD-MOFs)具有三维网络结构和较大的内腔,是溶解性较差药物的优良载体。在这项研究中,我们使用 CD-MOFs 作为载体来提高叶黄素的溶解度,并评估了它们的抗氧化活性、生物利用度和保肝作用。我们将叶黄素载入了β-CD-MOF、γ-CD-MOF、β-CD 和 γ-CD,并通过粉末 X 射线衍射仪(PXRD)和热重分析(TGA)对其进行了表征。结果表明,木犀草素-β-CD-MOF 最为稳定。分子模拟确定的主要驱动力是氢键和范德华力。木犀草素-β-CD-MOF 的负载能力为 14.67 wt%。与未加工的木犀草素相比,木犀草素-β-CD-MOF 的溶解度提高了 4.50 倍,体外抗氧化活性也有所提高。在健康大鼠和对乙酰氨基酚引起的肝损伤大鼠体内,叶黄素-β-CD-MOF 使叶黄素的生物利用率分别提高了约 4.04 倍和 11.07 倍。生化分析表明,在对乙酰氨基酚诱发肝损伤的大鼠体内,叶黄素-β-CD-MOF 的保肝效果优于未加工的叶黄素。这项研究为预防对乙酰氨基酚引起的肝损伤提供了一种新方法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

β-Cyclodextrin metal-organic framework as a green carrier to improve the dissolution, bioavailability, and liver protective effect of luteolin

β-Cyclodextrin metal-organic framework as a green carrier to improve the dissolution, bioavailability, and liver protective effect of luteolin

The incidence of acetaminophen-induced liver injury has increased, but effective prevention methods are limited. Although luteolin has hepatoprotective activity, its low solubility and bioavailability limit its applications. Cyclodextrin metal-organic frameworks (CD-MOFs) possess 3D-network structures and large inner cavities, which make them excellent carriers of poorly soluble drugs. In this study, we used CD-MOFs as carriers to improve the dissolution of luteolin and assessed their antioxidant activity, bioavailability, and hepatoprotective effects. Luteolin was loaded into β-CD-MOF, γ-CD-MOF, β-CD, and γ-CD, and characterized by powder X-ray diffractometry (PXRD) and thermogravimetric analysis (TGA). Our results showed that luteolin-β-CD-MOF was the most stable. The main driving forces were hydrogen bonds and van der Waals forces, as determined by molecular simulation. The loading capacity of luteolin-β-CD-MOF was 14.67 wt%. Compared to raw luteolin, luteolin-β-CD-MOF exhibited a 4.50-fold increase in dissolution and increased antioxidant activity in vitro. Luteolin-β-CD-MOF increased the bioavailability of luteolin by approximately 4.04- and 11.07-fold in healthy rats and liver injured rats induced by acetaminophen in vivo, respectively. As determined by biochemical analysis, luteolin-β-CD-MOF exhibited a better hepatoprotective effect than raw luteolin in rats with acetaminophen-induced liver injury. This study provides a new approach for preventing acetaminophen-mediated liver damage.

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来源期刊
International Journal of Pharmaceutics: X
International Journal of Pharmaceutics: X Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
6.60
自引率
0.00%
发文量
32
审稿时长
24 days
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