Title:Fluconazole Microemulsions: Preparation, Statistical Optimization by Two-level Factorial Design, and Physicochemical Evaluation
Volume: 21
Issue: 16
Author(s): Payam Khazaeli*, Abbas Pardakhty, Gholamreza Dehghannoudeh, Sina Safizade, Marzieh Sajadi Bami and Mandana Ohadi*
Affiliation:
- Pharmaceutics Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman,
Iran
- Department of Pharmaceutics, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran
- Pharmaceutics Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman,
Iran
Keywords:
Antifungal, semisolid, optimal, formulation, experimental design, SEM.
Abstract:
Background: Candida albicans is the yeast that causes the fungal infection known as candidiasis.
One of the standard methods for treating candida is the application of fluconazole. The low
solubility of fluconazole in aqueous media is a big problem in the use of this agent. Novel drug delivery
systems, such as microemulsions, could be applied to solve this problem. The main aim of this
study was to perform statistical optimization of the formulation and physicochemical characterization
of fluconazole microemulsion.
Methods: Optimization of the microemulsion formulation was done by using experimental design
software, and then fluconazole was loaded onto the best formulation at a concentration of 1 % w/w.
The physiochemistry of the microemulsion formulation was assessed by pH measurement, rheology
measurement, simultaneous thermal analysis, and Scanning Electron Microscopy (SEM).
Results: The two-level fractional factorial design application demonstrated the optimum formulation
to consist of surfactant, co-surfactant, oil content, and water, comprising 58%, 27%, 10%, and 5% of
the formulation, respectively. Desirable thermal mass was observed up to 150°C. The formulation
was a non-Newtonian shear-thinning liquid in terms of viscosity, with a reported pH between 6.5-7.
Conclusion: Considerably stable, high-quality microemulsion formulations containing fluconazole
are presented, which are applicable for antifungal skin candidiasis treatment in clinical trials.
