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
期刊介绍: International Journal of Pharmaceutics: X offers authors with high-quality research who want to publish in a gold open access journal the opportunity to make their work immediately, permanently, and freely accessible. International Journal of Pharmaceutics: X authors will pay an article publishing charge (APC), have a choice of license options, and retain copyright. Please check the APC here. The journal is indexed in SCOPUS, PUBMED, PMC and DOAJ. The International Journal of Pharmaceutics is the second most cited journal in the "Pharmacy & Pharmacology" category out of 358 journals, being the true home for pharmaceutical scientists concerned with the physical, chemical and biological properties of devices and delivery systems for drugs, vaccines and biologicals, including their design, manufacture and evaluation. This includes evaluation of the properties of drugs, excipients such as surfactants and polymers and novel materials. The journal has special sections on pharmaceutical nanotechnology and personalized medicines, and publishes research papers, reviews, commentaries and letters to the editor as well as special issues.
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