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. 2021 Mar 30;19(1):15593258211001259.
doi: 10.1177/15593258211001259. eCollection 2021 Jan-Mar.

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

Shaimaa M Badr-Eldin  1   2 , Usama A Fahmy  1 , Hibah M Aldawsari  1   3 , Osama A A Ahmed  1   3 , Nabil A Alhakamy  1   3   4   5 , Solomon Z Okbazghi  6 , Mohamed A El-Moselhy  7   8 , Adel F Alghaith  9 , Aliaa Anter  7 , Asmaa I Matouk  7 , Wael Ali Mahdi  9 , Sultan Alshehri  9   10 , Rana Bakhaidar  1
Affiliations

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

Shaimaa M Badr-Eldin et al. Dose Response. .

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.

Keywords: COX2; alpha-lipoic acid; gastritis; indomethacin; nanotechnology; stomatitis.

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Conflict of interest statement

Declaration of Conflicting Interests: The author(s) declared no potential conflicts of interest with respect to the research, authorship, and/or publication of this article.

Figures

Figure 1.
Figure 1.
Diagnostic plots for droplet size of ALA SNEDS; (A) studentized residuals vs. predicted values plot and (B) predicted vs. actual values plot.
Figure 2.
Figure 2.
2D contour plot (A) and 3D surface plot (B) for the effect of mixture components on the droplet size of ALA SNEDDS.
Figure 3.
Figure 3.
Bar graphs showing the effect of indomethacin (IND), pure alpha-lipoic acid (ALA), and alpha-lipoic acid formula (ALA-F) on ulcer index (A), preventive index (B), and stomach photos from different groups (C). Data are presented as mean ± S.E.M. # Significantly different from indomethacin at P < 0.05, ### significantly different from indomethacin at P < 0.001.
Figure 4.
Figure 4.
Bar graphs showing the effect of indomethacin (IND), pure alpha-lipoic acid (ALA), alpha-lipoic acid formula (ALA-F) and vehicle on mucosal level of MDA. Data are presented as mean ± S.E.M. *** Significantly different from control at P < 0.001, ### significantly different from indomethacin at P < 0.001. Effect of pure alpha-lipoic acid and lipoic acid formulations on serum total antioxidant capacity.
Figure 5.
Figure 5.
Bar graphs showing the effect of indomethacin (IND), pure alpha-lipoic acid (ALA), and alpha-lipoic acid formula (ALA-F) on serum total antioxidant capacity (TAC). Data are presented as mean ± S.E.M. ** significantly different from control at P < 0.01, ## significantly different from indomethacin at P < 0.01, $$ significantly different from ALA-R at P < 0.01.
Figure 6.
Figure 6.
Representative photomicrographs of H&E-stained stomach sections of: (A) control group, (B) indomethacin treated group, (C) pure ALA + indomethacin, (D) ALA formula + indomethacin, (E) vehicle treated group. Magnification = 200×. H&E stain.
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