Radwan Mohamed F, El-Moselhy Mohamed A, Alarif Walied M, Orif Mohamed, Alruwaili Nabil K, Alhakamy Nabil A
Department of Chemistry, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia.
Department of Pharmacology, School of Pharmacy, Ibn Sina National College, Jeddah, Saudi Arabia.
Dose Response. 2021 May 10;19(2):15593258211013655. doi: 10.1177/15593258211013655. eCollection 2021 Apr-Jun.
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.
为提高黑种草籽油的主要成分百里醌（TQ）的水溶性，制备了载TQ的自纳米乳化药物递送系统（SNEDDS）。以杏仁油（AO）（油相；X1）、吐温80（表面活性剂；X2）和聚乙二醇200（PEG 200）（助表面活性剂；X3）为自变量对SNEDDS制剂进行优化。结果表明，液滴尺寸范围为65至320nm。此外，系统估算值与液滴尺寸的实验值之间达成了高度一致。为评估优化后的载TQ的SNEDDS与未乳化的TQ相比对吲哚美辛（Indo.）诱导的胃溃疡的胃保护作用，对溃疡指数和组织病理学变化进行了评估。相对于未乳化的TQ，优化后的载TQ的SNEDDS对Indo.诱导的溃疡显示出更好的胃保护活性。此外，与未乳化的TQ相比，载TQ的SNEDDS的胃保护指数提高了2倍。这归因于TQ的强抗氧化活性和细胞保护活性。这些结果表明通过优化的SNEDDS提高了TQ的疗效。
