Optimization of Thymoquinone-Loaded Self-Nanoemulsion for Management of Indomethacin-Induced Ulcer

Abstract

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.

Development of a Multifunctional Oral Dosage Form via Integration of Solid Dispersion Technology with a Black Seed Oil-Based Self-Nanoemulsifying Drug Delivery System

“…Previous studies have shown that thymoquinone (TMQ), a major constituent of black seed oil (BSO), possesses gastroprotective effects and can help treat peptic ulcers more potently when formulated using a SNEDDS-based delivery approach [17]. Additional research found BSO to be more effective than TMQ alone for reducing peptic ulcer indices in animal models [14].…”

“…Furtherm et al prepared a TMQ-loaded SNEDDS to study the impact of increasing dr on the therapeutic effects. Their study reported that the formulated TMQ-S creased the ulcer index by 2-fold compared to free TMQ alone, as indicated ings [17]. Despite their reported in vivo activity, the FDA has not yet approve extracts or concentrated thymoquinone for treating any medical conditions l lesterol, diabetes, or high blood pressure.…”

“…In light of this, several reports revealed that black seed oil (BSO) has a protective and healing effect on gastric ulcers [14,15]. Along with this, various studies showed that the administration of thymoquinone (TMQ), the major constituent in BSO, reduces peptic ulcers produced by NSAIDs and other agents like ethanol [16][17][18]. In detail, Kanter et al studied the impact of BSO and TMQ on gastric ulcers in rats.…”

Modulation of engineered nanomaterial interactions with organ barriers for enhanced drug transport

“…207 Similarly, to investigate the gastroprotective effect in a rat model, in silico response and contour plots have been used to optimize the globule size of self-nano emulsion particles, where the predicted sizes were similar to the actual value measured (67.7 nm calculated versus 64.8 nm actual). 208 Adding automation for the high throughput screening of nanoparticle formulations is necessary to improve optimization speed and predict biological interactions such as solubility and potential penetration capabilities. 209,210 3.3.1.…”