Sunoqrot Suhair, Abu Shalhoob Mohammad, Jarrar Yazun, Hammad Alaa M, Al-Ameer Hamzeh J, Al-Awaida Wajdy
Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman 11733, Jordan.
Department of Basic Medical Sciences, Faculty of Medicine, Al-Balqa Applied University, Al-Salt 19117, Jordan.
ACS Omega. 2024 Jan 31;9(7):7881-7890. doi: 10.1021/acsomega.3c07602. eCollection 2024 Feb 20.
Curcumin (CUR) is a natural product with known anti-inflammatory, antioxidant, and hepatoprotective properties. The aim of this study was to formulate CUR into a polymeric nanoparticle (NP) formulation and examine its potential hepatoprotective activity in an animal model of diclofenac (DIC)-induced hepatotoxicity. CUR was loaded into polymeric NPs composed of poly(ethylene glycol)-polycaprolactone (PEG-PCL). The optimal CUR NPs were evaluated against DIC-induced hepatotoxicity in mice, by studying the histopathological changes and gene expression of drug-metabolizing ( and ) and () genes in the livers of the animals. The optimal NPs were around 67 nm in diameter with more than 80% loading efficiency and sustained release. Histological findings of mice livers revealed that CUR NPs exhibited a superior hepatoprotective effect compared to free CUR, and both groups reduced DIC-mediated liver tissue injury. While treatment with DIC alone or with CUR and CUR NPs had no effect on gene expression, and genes were upregulated in the DIC-treated group, and this effect was reversed by CUR both as a free drug and as CUR NPs. Our findings present a promising application for nanoencapsulated CUR in the treatment of nonsteroidal anti-inflammatory drugs-induced liver injury and the associated dysregulation in the expression of hepatic drug-metabolizing enzymes.
姜黄素（CUR）是一种具有抗炎、抗氧化和肝保护特性的天然产物。本研究的目的是将姜黄素制成聚合物纳米颗粒（NP）制剂，并在双氯芬酸（DIC）诱导的肝毒性动物模型中研究其潜在的肝保护活性。将姜黄素负载到由聚（乙二醇）-聚己内酯（PEG-PCL）组成的聚合物纳米颗粒中。通过研究动物肝脏中药物代谢（ 和 ）和 （ ）基因的组织病理学变化和基因表达，评估最佳姜黄素纳米颗粒对DIC诱导的小鼠肝毒性的作用。最佳纳米颗粒直径约为67nm，负载效率超过80%，且具有缓释性能。小鼠肝脏的组织学结果显示，与游离姜黄素相比，姜黄素纳米颗粒具有更好的肝保护作用，两组均减轻了DIC介导的肝组织损伤。虽然单独使用DIC或与姜黄素和姜黄素纳米颗粒联合治疗对 基因表达没有影响，但在DIC治疗组中 和 基因上调，而游离姜黄素和姜黄素纳米颗粒形式的姜黄素均可逆转这种作用。我们的研究结果为纳米包封姜黄素在治疗非甾体抗炎药诱导的肝损伤及相关肝药物代谢酶表达失调方面提供了一个有前景的应用。
