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大鼠口服槲皮素纳米乳的抗炎作用及毒理学分析

Anti-inflammatory Effect and Toxicology Analysis of Oral Delivery Quercetin Nanosized Emulsion in Rats.

作者信息

Hädrich Gabriela, Vaz Gustavo Richter, Maidana Michelle, Kratz Jadel Muller, Loch-Neckel Gecioni, Favarin Daniely Cornélio, Rogerio Alexandre de Paula, da Silva Flávio Manoel Rodrigues, Muccillo-Baisch Ana Luiza, Dora Cristiana Lima

机构信息

Laboratório de Nanotecnologia Aplicada à Saúde, Programa de Pós-Graduação em Ciências da Saúde, Universidade Federal do Rio Grande (FURG), Av Itália, Km 8, Rio Grande, RS, 96210-900,, Brazil.

Laboratório de Ensaios Farmacológicos e Toxicológicos, Instituto de Ciências Biológicas, Universidade Federal do Rio Grande (FURG), Rio Grande, RS, 96210-900,, Brazil.

出版信息

Pharm Res. 2016 Apr;33(4):983-93. doi: 10.1007/s11095-015-1844-6. Epub 2015 Dec 18.

Abstract

PURPOSE

This study evaluates the advantage of the quercetin encapsulation in nanosized emulsion (QU-NE) administered orally in rats in order to demonstrate its anti-oedematous and antioxidant effects as well as its toxicity.

METHODS

The nanocarriers were prepared using the hot solvent diffusion with the phase inversion temperature methods. The nanocarriers physicochemical properties were then investigated. The anti-edematous activity was tested using paw edema in rats. In addition, NF-kB expression in subcutaneous tissue of the paws was accessed by immunohistochemistry while the lipid peroxidation was analyzed in the liver by malondialdehyde reaction with thiobarbituric acid. Hematological, renal and hepatic toxicity as well as the genetic damage were also evaluated.

RESULTS

The results demonstrated that QU-NE exhibited pronounced anti-oedematous property comparable to drug diclofenac. This effect was associated with NF-κB pathway inhibition. The lipid peroxidation was also only reduced in rats treated with QU-NE. Besides this, no genetic damage, hematological, renal or hepatic toxicities were observed after administration of QU-NE.

CONCLUSIONS

These results suggest that quercetin nanosized emulsion exhibits anti-oedematous and antioxidant properties and does not demonstrate toxic effects. This indicates that it has a potential application in the treatment of inflammatory diseases.

摘要

目的

本研究评估槲皮素纳米乳剂(QU-NE)经大鼠口服给药的优势,以证明其抗水肿和抗氧化作用以及毒性。

方法

采用热溶剂扩散和相转变温度法制备纳米载体。然后研究纳米载体的物理化学性质。使用大鼠爪部水肿试验抗水肿活性。此外,通过免疫组织化学检测爪部皮下组织中NF-κB的表达,同时通过丙二醛与硫代巴比妥酸反应分析肝脏中的脂质过氧化。还评估了血液学、肾脏和肝脏毒性以及遗传损伤。

结果

结果表明,QU-NE表现出与双氯芬酸相当的显著抗水肿特性。这种作用与NF-κB途径的抑制有关。脂质过氧化也仅在接受QU-NE治疗的大鼠中降低。除此之外,给予QU-NE后未观察到遗传损伤、血液学、肾脏或肝脏毒性。

结论

这些结果表明,槲皮素纳米乳剂具有抗水肿和抗氧化特性,且未显示出毒性作用。这表明它在炎症性疾病的治疗中具有潜在应用价值。

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