Optimized Self-Nanoemulsifying Delivery System Based on Plant-Derived Oil Augments Alpha-Lipoic Acid Protective Effects Against Experimentally Induced Gastric Lesions

Abstract

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.

Nanotechnological Approaches to Enhance the Potential of α-Lipoic Acid for Application in the Clinic

“…This evidence was confirmed by a recent clinical trial in healthy volunteers, where the bioavailability of the R-(+)-α-lipoic acid/γ-CD complex demonstrated results 2.5 higher than the non-complexed R-(+)-α-lipoic acid [127]. Improve solubility [104] Improve bioavailability [105] Improve antioxidant activity [108] Nanocapsules and nanospheres…”

“…In another study, pumpkin oil was used to solubilize α-lipoic acid and develop a self-nanoemulsifying drug delivery system, stabilised by Tween 80 polyethylene glycol 200. The formulation demonstrates higher protective effects against gastric ulcer models compared to the free α-lipoic acid [ 104 ].…”