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

Dose-Response ◽  
2021 ◽  
Vol 19 (2) ◽  
pp. 155932582110136
Author(s):  
Mohamed F. Radwan ◽  
Mohamed A. El-Moselhy ◽  
Walied M. Alarif ◽  
Mohamed Orif ◽  
Nabil K. Alruwaili ◽  
...  

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.

2017 ◽  
Vol 68 (2) ◽  
pp. 331-336
Author(s):  
Gabriela Isopencu ◽  
Mirela Marfa ◽  
Iuliana Jipa ◽  
Marta Stroescu ◽  
Anicuta Stoica Guzun ◽  
...  

Nigella sativa, also known as black cumin, an annual herbaceous plant growing especially in Mediterranean countries, has recently gained considerable interest not only for its use as spice and condiment but also for its healthy properties of the fixed and essential oil and its potential as a biofuel. Nigella sativa seeds fixed oil, due to its high content in linoleic acid followed by oleic and palmitic acid, could be beneficial to human health. The objective of this study is to determine the optimum conditions for the solvent extraction of Nigella sativa seeds fixed oil using a three-level, three-factor Box-Behnken design (BBD) under response surface methodology (RSM). The obtained experimental data, fitted by a second-order polynomial equation were analysed by Pareto analysis of variance (ANOVA). From a total of 10 coefficients of the statistical model only 5 are important. The obtained experimental values agreed with the predicted ones.


Author(s):  
Gomes Acg ◽  
Lima Mcpm ◽  
Caliari M ◽  
Alves Dg ◽  
Machado Alb ◽  
...  

Due to the technological importance that the extrusion process represents in the application of fast food, the objective of this work was to apply pregelatinized rice and sorghum flours in the development of an instant preparation soup and to evaluate its centesimal, technological, and their sensorial analysis. Ten formulations of the instant soup were prepared from the mixtures experimental design. According to the experimental results, it can be stated that the predicted values corroborated with the experimental values, that is, a mixture was obtained for the instant soup with the characteristics of water absorption, water solubility, color, luminosity and viscosity close to the predicted by the models. After the physical and chemical analysis, the microbiological characterization of the best formulation defined by the desirability test was used, which demonstrated that the product is suitable to microbiological standards. The results obtained showed that the 80:10:10 instant soup formulation of pregelatinized rice flour, pregelatinized sorghum flour and potato starch allowed the experimental development of a new product with good nutritional characteristics benefits. It was obtained a food with good technological characteristics solubility and absorption in water, good viscosity, light color and with good sensory acceptance by the tasters.


2020 ◽  
Vol 12 ◽  
Author(s):  
Sagar R. Pardeshi ◽  
Harshal A. Mistari ◽  
Rakhi S. Jain ◽  
Pankaj R. Pardeshi ◽  
Rahul L. Rajput ◽  
...  

Background: Moxifloxacin is a BCS class I drug used in the treatment of bacterial conjunctivitis and keratitis. Despite its high water solubility, it possesses limited bioavailability due to anatomical and physiological constraints associated with the eyes which required multiple administrations to achieve a therapeutic effect. Objective: In order to prolong drug release and to improve antibacterial efficacy for the treatment of bacterial keratitis and conjunctivitis, moxifloxacin loaded nanoemulsion was developed. Methods: The concentration of oil (oleic acid), surfactant (tween 80), and cosurfactant (propylene glycol) were optimized by employing a 3-level 2-factorial design of experiment for the development of nanoemulsion. The developed nanoemulsion was characterized by particle size distribution, viscosity, refractive index, pH, drug content and release, transmission electron microscopy (TEM), and antibacterial study. The compatibility of the drug with the excipients was accessed by Fourier transform infrared spectroscopy (FTIR). Result: The average globule size was found to be 198.20 nm. The TEM study reveals the globules were nearly spherical and are well distributed. In vitro drug release profile for nanoemulsion shown sustained drug release (60.12% at the end of 6 h) compared to drug solution, where complete drug released within 2 h. The antibacterial effectiveness of the drug-loaded nanoemulsion was improved against S. aureus compared with the marketed formulation. Conclusion: The formulated sustained release nanoemulsion could be a promising alternative to eye drop with improved patient compliance by minimizing dosing frequency with improved antibacterial activity.


Dose-Response ◽  
2021 ◽  
Vol 19 (1) ◽  
pp. 155932582110012
Author(s):  
Shaimaa M. Badr-Eldin ◽  
Usama A. Fahmy ◽  
Hibah M. Aldawsari ◽  
Osama A. A. Ahmed ◽  
Nabil A. Alhakamy ◽  
...  

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.


2018 ◽  
Vol 7 (2) ◽  
Author(s):  
Amnah M.A. Alsuhaibani

In this study, the gross composition and mineral content of Nigella sativa seed powder (NSP) and fatty acid composition of Nigella sativa oil (NSO) were investigated. The ability of NSP, extract (NSE) and NSO in reducing the effects of cisplatin-induced renal toxicity in Sprague-Dawley rats were examined. The obtained results showed that NSP contains high amounts of carbohydrates, protein, and fiber while NSO has higher amounts of linoleicacid, oleic acid, and myristic acid. Rats treated with NSP, NSO, and NSE exhibitedreducedserum levels of urea, creatinine, and potassium, and a significant increase of Na, Na/K, vitamin D, nutritional markers, and antioxidant enzymes compared to the cisplatin-induced renal toxicity group receiving no Nigella sativa seed treatment. This study determined that all powder, oil, and extracts of N. sativa contain potent bioactive components that may aid in treatment against cisplatininduced renal toxicity in rats.


Author(s):  
Himanshu Paliwal ◽  
Ram Singh Solanki ◽  
Chetan Singh Chauhan

The purpose of conducting this study was to prepare an oral microemulsion formulation of Rosuvastatin calcium (RC) to improve its water solubility. Oil in water microemulsion was formulated using Oleic acid, Tween 80 and Polyethylene Glycol-400(PEG-400) as oil, surfactant and co-surfactant, respectively. The ideal proportion of surfactant: co-surfactant (Smix) was chosen by constructing pseudoternary diagrams. The microemulsion formulations which proved to be stable after thermodynamic stability testing were further evaluated for physical characteristics. Selected formulations were evaluated for droplet size, zeta potential, polydispersity index, viscosity and % drug content. The results were suggestive that optimized microemulsion formulation (F2) was thermodynamically stable and clear having a droplet size of 74.29 nm and zeta potential of -18.44.  In vitro dissolution study for optimized microemulsion was performed using a dialysis bag method and cumulative % drug release was determined. The result from the release study was indicative of improved solubility of Rosuvastatin calcium which may serve to boost up the oral bioavailability of drug.


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