Anjum Sumaira, Soliman Mohamed Mohamed, Althobaiti Fayez, Albattal Shatha B, Dar Momina Riaz, Inam Mubashara, Khan Amna Komal, Elshehawi Ahmed, Mujahid Huma
Department of Biotechnology, Kinnaird College for Women University, Jail Road, Lahore 54000, Pakistan.
Department of Clinical Laboratory Sciences, Turabah University College, Taif University, P.O. Box 11099, Taif 21944, Saudi Arabia.
Toxicol Res (Camb). 2025 May 15;14(3):tfaf034. doi: 10.1093/toxres/tfaf034. eCollection 2025 Jun.
Peptic ulcer is a chronic inflammatory disorder affecting large portion of population with difficulty in treatment. Treatment options include inhibition of gastric acid secretion, histamine inhibitors, eradication of infection and tissue lining protection. These therapeutic options have several side effects, low bioavailability and bio-distribution. To further increase bioavailability, control release, stability, site specific delivery and minimize organoleptic side effects of phytochemical, nano-encapsulation is a suitable strategy. Chitosan is a suitable nano-carrier for drug delivery applications in treating peptic ulcer as it is biodegradable, biocompatible, safe and cost-effective. Therefore, (FR) leaf extract was loaded into chitosan NPs by ion gelation method for in vivo anti-ulcerative activity in indomethacin-induced peptic ulcer rats. Results showed that FR extract was successfully loaded into CNPs with 84% encapsulation efficiency while the size of empty CNPs was reported to be 620.3 nm as compared to FR-loaded CNPs 811.5 nm. FR-loaded CNPs showed homogeneous size distribution as well greater physical stability. Furthermore, in vivo studies revealed gastro-protective activity of FR-loaded CNPs in reducing the ulcer index (UI) to 0.51 (71.30% inhibition) while indomethacin only untreated rats showed UI 2.99 and insignificant ulcer inhibition 11.02%. Furthermore, FR-loaded CNPs restored gastric pH, healed rat stomach completely without ulcers or hemorrhagic spot and improved antioxidants and blood profiles compared to plant extract or CNPs. These findings confirmed the effective application of extract loaded CNPs as anti-ulcer agents and reinforces the importance of nano-encapsulation in improving drug efficacy.
消化性溃疡是一种慢性炎症性疾病,影响着很大一部分人群,治疗困难。治疗选择包括抑制胃酸分泌、组胺抑制剂、根除感染和保护组织内膜。这些治疗选择有多种副作用、低生物利用度和生物分布性。为了进一步提高生物利用度、控制释放、稳定性、位点特异性递送并使植物化学物质的感官副作用最小化,纳米封装是一种合适的策略。壳聚糖是一种适用于治疗消化性溃疡药物递送应用的纳米载体,因为它可生物降解、生物相容、安全且具有成本效益。因此,通过离子凝胶法将(FR)叶提取物负载到壳聚糖纳米粒中,用于吲哚美辛诱导的消化性溃疡大鼠的体内抗溃疡活性研究。结果表明,FR提取物成功负载到壳聚糖纳米粒中,包封率为84%,而据报道,空壳聚糖纳米粒的尺寸为620.3纳米,相比之下,负载FR的壳聚糖纳米粒尺寸为811.5纳米。负载FR的壳聚糖纳米粒显示出均匀的尺寸分布以及更高的物理稳定性。此外,体内研究表明,负载FR的壳聚糖纳米粒具有胃保护活性,可将溃疡指数(UI)降低至0.51(抑制率71.30%),而仅用吲哚美辛处理的未治疗大鼠的溃疡指数为2.99,溃疡抑制率为11.02%,无统计学意义。此外,与植物提取物或壳聚糖纳米粒相比,负载FR的壳聚糖纳米粒恢复了胃pH值,使大鼠胃完全愈合,无溃疡或出血点,并改善了抗氧化剂和血液指标。这些发现证实了负载提取物的壳聚糖纳米粒作为抗溃疡剂的有效应用,并强化了纳米封装在提高药物疗效方面的重要性。