Alamoudi Jawaher Abdullah, El-Masry Thanaa A, El-Nagar Maysa M F, El Zahaby Enas I, Elmorshedy Kadreya E, Gaballa Mohamed M S, Alshawwa Samar Zuhair, Alsunbul Maha, Alharthi Sitah, Ibrahim Hanaa A
Department of Pharmaceutical Sciences, College of Pharmacy, Princess Nourah bint Abdulrahman University, Riyadh, Saudi Arabia.
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Tanta University, Tanta, Egypt.
Front Pharmacol. 2024 Sep 9;15:1433793. doi: 10.3389/fphar.2024.1433793. eCollection 2024.
Hesperidin (Hes) protects different organs from damage by acting as a potent antioxidant and anti-inflammatory. This study aims to evaluate the gastroprotective effects of free hesperidin and its chitosan nanoparticles (HNPs) against ethanol-induced gastric ulcers in rats, hypothesizing that HNPs will enhance bioavailability and therapeutic efficacy due to improved solubility and targeted delivery. HNPs were synthesized via ion gelation and characterized using TEM, SEM, and zeta potential analyses. Key assessments included gastric acidity, histological analysis, and markers of inflammation, oxidative stress, and apoptosis. HNPs significantly decreased gastric acidity, reduced inflammatory and apoptotic markers, and enhanced antioxidant enzyme activities compared to free hesperidin and esomeprazole. Furthermore, Sirt-1, PGC-1α, HO-1, and FOXO1 gene expression were also evaluated. HNPs raised Sirt-1, PGC-1α, HO-1, and downregulated FOXO1, and they suppressed the activities of NF-κB p65, COX-2, IL-1β, CD86, FOXO1 P53, and caspase-3 and increased Sirt-1 activity. HNPs treatment notably restored antioxidant enzyme activity, reduced oxidative stress and inflammatory markers, and improved histological outcomes more effectively than free hesperidin and esomeprazole. These results indicate that chitosan nanoparticles significantly enhance the gastroprotective effects of hesperidin against ethanol-induced gastric ulcers, potentially offering a more effective therapeutic strategy. Further research should explore the clinical applications of HNPs in human subjects.
橙皮苷(Hes)作为一种强大的抗氧化剂和抗炎剂,可保护不同器官免受损伤。本研究旨在评估游离橙皮苷及其壳聚糖纳米颗粒(HNPs)对大鼠乙醇诱导的胃溃疡的胃保护作用,假设HNPs由于溶解度提高和靶向递送将增强生物利用度和治疗效果。通过离子凝胶法合成HNPs,并使用透射电子显微镜(TEM)、扫描电子显微镜(SEM)和zeta电位分析对其进行表征。主要评估包括胃酸度、组织学分析以及炎症、氧化应激和细胞凋亡的标志物。与游离橙皮苷和埃索美拉唑相比,HNPs显著降低了胃酸度,减少了炎症和凋亡标志物,并增强了抗氧化酶活性。此外,还评估了Sirt-1、PGC-1α、HO-1和FOXO1基因的表达。HNPs上调了Sirt-1、PGC-1α、HO-1并下调了FOXO1,它们抑制了NF-κB p65、COX-2、IL-1β、CD86、FOXO1 P53和caspase-3的活性并增加了Sirt-1活性。与游离橙皮苷和埃索美拉唑相比,HNPs治疗显著恢复了抗氧化酶活性,降低了氧化应激和炎症标志物,并更有效地改善了组织学结果。这些结果表明壳聚糖纳米颗粒显著增强了橙皮苷对乙醇诱导的胃溃疡的胃保护作用,可能提供一种更有效的治疗策略。进一步的研究应探索HNPs在人类受试者中的临床应用。