FORMULATION, OPTIMIZATION AND CHARACTERIZATION OF IBUPROFEN LOADED MICROEMULSION SYSTEM USING D-OPTIMAL MIXTURE DESIGN

Objective: The purpose of this study was to develop, optimize and characterize a stable microemulsion, with an improvement of the solubility of a poorly aqueous soluble drug, ibuprofen. Methods: Various oils (oleic acid, cottonseed oil, olive oil, argan oil, and labrafac® WL 1349), surfactants (tween® 80, tween® 40, tween® 20) and co-surfactants including polyethylene glycol 400, ethanol, 1-butanol, and propylene glycol were selected after solubility studies. Then, pseudo-ternary phase diagrams with surfactant/co-surfactant ratio of 1:2, 1:1, 2:1 and 3:1 were constructed and a D-optimal mixture design method was used to optimize the ibuprofen loaded microemulsion. The optimized microemulsion was evaluated for several characteristics including globule size, zeta potential, pH, conductivity, refractive index and stability studies. Results: Optimized microemulsion obtained was composed of oleic acid (6.88% w/w), tween® 80/1-butanol (3:1, 63.11% w/w) and water (30.00% w/w). The results obtained showed an average globule size of 117.5 nm, a zeta potential of-6.47 mV and a transmittance of 96.95±0.77%. The optimized formulation showed an improvement in the solubility of ibuprofen with unchanged characteristics for one month. Conclusion: The use of pseudo-ternary phase diagrams and mathematical modeling allows to obtain an optimal microemulsion with perfect stability for 1 mo and a better solubilization capacity of ibuprofen

SOLUBILIZATION OF CELECOXIB USING ORGANIC COSOLVENT AND NONIONIC SURFACTANTS OPTIMIZED BY EXPERIMENTAL DESIGN

Objective: The solubility of drug substances in water is one of the major factors taken into account in the formulation of oral solutions and parenteral forms. The present study aims to evaluate the utility of a mixture design in improving water solubility of celecoxib through a micellar system by the use of organic co solvent and nonionic surfactants that are well tolerated by the parenteral route.Methods: In our study, a design of experiments approach was tested using a mixture design of nonionic surfactants (Tween® 80 and Solutol®HS 15), an organic cosolvent (ethanol) and celecoxib. Solubility determination was based on the analysis of samples absorbance at 215 nm. A particles size measurement was conducted using a Dynamic Light Scattering at the point showing the maximum of solubility.Results: The results showed a significant solubility increase in most of tested mixtures. The analysis of the design space showed that the solubility of celecoxib varies very closely with the concentration of Tween® 80 associated with ethanol and Solutol®HS 15 in water. Run 19 containing 0.8% of celecoxib, 10% of ethanol, 2% of Tween® 80, 2% of Solutol®HS 15 and water q. s. for 100% w/w improved celecoxib solubility by about 90 %, and showed an average particles size of 9.67 nm.Conclusion: Micellar solubilisation associating a cosolvent and nonionic surfactants seems to improve celecoxib solubility significantly. Mixture design provides maximum information about the effects and the proportions of each component from a limited number of experiments.Keywords: Solubility, Celecoxib, Mixture design, Cosolvent, SurfactantsÂ

Skin hydration in postmenopausal women: argan oil benefit with oral and/or topical use

The aim of this study was to evaluate the effect of daily consumption and/or application of argan oil on skin hydration in postmenopausal women. Material and methods : Sixty postmenopausal women consumed butter during the stabilization period and were randomly divided into two groups for the intervention period: the treatment group absorbed alimentary argan oil (n = 30) and the control group olive oil (n = 30). Both groups applied cosmetic argan oil in the left volar forearm during a sixty days’ period. Evaluation of skin hydration, i.e. transepidermal water loss (TEWL) and water content of the epidermis (WCE) on both volar forearms of the two groups, were performed during three visits at D0, D30 and after sixty days (D60) of oils treatment. Results : The consumption of argan oil has led to a significant decrease in TEWL (p = 0.023) and a significant increase in WCE (p = 0.001). The application of argan oil has led to a significant decrease in TEWL (p = 0.01) and a significant increase in WCE (p < 0.001). Conclusions : Our findings suggest that the daily consumption and application of argan oil have improved the skin hydration by restoring the barrier function and maintaining the water-holding capacity

FORMULATION, CHARACTERISATION AND OPTIMISATION OF NATURAL ARGAN OIL MICROEMULSION FOR TOPICAL DELIVERY

Objective: The purpose of this study was to develop, optimize and characterize a stable microemulsion of Moroccan cosmetic Argan oil. Methods: In this work, microemulsion system was studied by construction of phase diagrams using titration method. At first various surfactants (Brij56®, Tween 80®, Solutol®, Tween 20® and Labrasol®) and various weight ratio surfactant/cosurfactant (1:0, 3:1, 2:1 and 1:1) were tested to select the optimal surfactant and concentration to use. The microemulsions with tween80 were evaluated with different techniques using various parameters such as droplet size, transmittance, viscosity and pH. Stability studies of these microemulsions were conducted for 8 weeks at 5°C, 25°C and 40°C, and underwent centrifugation at 3000 rpm and ultracentrifugation at 10 000 rpm. Results: The largest microemulsion formation area was achieved for the microemulsions containing Tween 80/PEG 400 at a ratio of 3:1. The obtained microemulsions M1 to M12 were homogeneous. More the percentage of PEG 400 increases, more the pH of the preparations and their viscosity decreases, while preparations with a high oil content have low transmittance. Thermodynamic and physical stability shows that only samples with a minimum of 31.5% of Tween 80 and a maximum of 9% of oil showed a good stability. Among the stable preparations, M11 (9% O, 10% W and 40.5/40.5% S/Cos) was the formula which exhibited properties such as transparency, soft acidic pH and low viscosity, making it suitable for cutaneous use. Conclusion: The use of pseudo-ternary phase diagrams allows for the development of an optimal microemulsion with perfect stability. Keywords: Microemulsion, Argan oil, surfactant, cosurfactant