Badr-Eldin Shaimaa M, Fahmy Usama A, Aldawsari Hibah M, Ahmed Osama A A, Alhakamy Nabil A, Okbazghi Solomon Z, El-Moselhy Mohamed A, Alghaith Adel F, Anter Aliaa, Matouk Asmaa I, Mahdi Wael Ali, Alshehri Sultan, Bakhaidar Rana
Faculty of Pharmacy, Department of Pharmaceutics, King Abdulaziz University, Jeddah, Saudi Arabia.
Faculty of Pharmacy, Department of Pharmaceutics and Industrial Pharmacy, Cairo University, Cairo, Egypt.
Dose Response. 2021 Mar 30;19(1):15593258211001259. doi: 10.1177/15593258211001259. eCollection 2021 Jan-Mar.
Peptic ulcer disease is an injury of the alimentary tract that leads to a mucosal defect reaching the submucosa. Alpha-lipoic acid (ALA), a natural potent antioxidant, has been known as a gastroprotective drug yet its low bioavailability may restrict its therapeutic efficacy. This study aimed to formulate and optimize ALA using a self-nanoemulsifying drug delivery system (SNEDDS) with a size of nano-range, enhancing its absorption and augmenting its gastric ulcer protection efficacy. Three SNEDDS components were selected as the design factors: the concentrations of the pumpkin oil (X1, 10-30%), the surfactant tween 80 (X2, 20-50%), and the co-surfactant polyethylene glycol 200 (X3, 30-60%). The experimental design for the proposed mixture produced 16 formulations with varying ALA-SNEDDS formulation component percentages. The optimized ALA-SNEDDS formula was investigated for gastric ulcer protective effects by evaluating the ulcer index and by the determination of gastric mucosa oxidative stress parameters. Results revealed that optimized ALA-SNEDDS achieved significant improvement in gastric ulcer index in comparison with raw ALA. Histopathological findings confirmed the protective effect of the formulated optimized ALASNEDDS in comparison with raw ALA. These findings suggest that formulation of ALA in SNEDDS form would be more effective in gastric ulcer protection compared to pure ALA.
消化性溃疡病是一种消化道损伤，会导致黏膜缺损直至黏膜下层。α-硫辛酸（ALA）是一种天然强效抗氧化剂，已知是一种胃保护药物，但其低生物利用度可能会限制其治疗效果。本研究旨在使用粒径在纳米范围内的自纳米乳化药物递送系统（SNEDDS）来制备和优化ALA，以提高其吸收并增强其胃溃疡保护效果。选择三种SNEDDS成分作为设计因素：南瓜油浓度（X1，10 - 30%）、表面活性剂吐温80（X2，20 - 50%）和助表面活性剂聚乙二醇200（X3，30 - 60%）。针对所提出的混合物的实验设计产生了16种具有不同ALA - SNEDDS制剂成分百分比的制剂。通过评估溃疡指数和测定胃黏膜氧化应激参数，对优化后的ALA - SNEDDS配方的胃溃疡保护作用进行了研究。结果显示，与未加工的ALA相比，优化后的ALA - SNEDDS在胃溃疡指数方面有显著改善。组织病理学结果证实，与未加工的ALA相比，所制备的优化后的ALA - SNEDDS具有保护作用。这些发现表明，与纯ALA相比，以SNEDDS形式制备的ALA在胃溃疡保护方面更有效。
