Optimization of Thymoquinone-Loaded Self-Nanoemulsion for Management of Indomethacin-Induced Ulcer.
Dose Response. 2021 Apr-Jun;19(2):15593258211013655. Epub 2021 May 10. PMID: 33994890
Mohamed F Radwan
To improve the water solubility of thymoquinone (TQ), a major constituent of Nigella sativa seed oil, a TQ-loaded self-nanoemulsifying drug delivery system (SNEDDS) was prepared. The SNEDDS formulation was optimized using almond oil (AO) (Oil; X1), tween 80 (surfactant; X2) and polyethylene glycol 200 (PEG 200) (cosurfactant; X3) compounds as independent variables. The results showed that the globule size ranged from 65 to 320 nm. In addition, a strong agreement was reached between the system estimation and the experimental values of globule size. To evaluate the gastroprotective effect of optimized TQ-loaded SNEDDS against indomethacin (Indo.)-induced gastric ulcers in comparison with non-emulsified TQ, the ulcer index and histopathological changes were estimated. Optimized TQ-loaded SNEDDS showed improved gastroprotective activity against Indo.-induced ulcers relative to the non-emulsified TQ. In addition, the gastroprotective index was improved by 2-fold in TQ-loaded SNEDDS as compared to non-emulsified TQ. This is attributed to the strong antioxidant and the cytoprotective activities of the TQ. These results demonstrate enhancement of the efficacy of TQ through the optimized SNEDDS.