Improved efficacy of fluconazole against candidiasis using bio-based microemulsion technique

Area of Science:

• Pharmaceutical Sciences
• Mycology
• Materials Science

Background:

• Candida albicans is a prevalent fungal pathogen causing infections in immunocompromised individuals.
• Fluconazole, a common antifungal, faces challenges due to poor water solubility and emerging drug resistance.
• Novel drug delivery systems are needed to enhance fluconazole's efficacy and overcome resistance.

Purpose of the Study:

• To develop a unique microemulsion drug delivery system for fluconazole to treat candidiasis.
• To improve the solubility and bioavailability of fluconazole.
• To enhance the antifungal activity of fluconazole against Candida albicans.

Main Methods:

• Development of an oil-in-water microemulsion using clove oil, Tween 20, and water, guided by a ternary phase diagram.
• Physicochemical characterization of the microemulsion system.
• Transmission electron microscopy (TEM) to determine particle size and morphology.
• Antifungal activity assessment using fluorescence and scanning electron microscopy.

Main Results:

• A stable, clear oil-in-water microemulsion system was successfully developed.
• Fluconazole particle size was significantly reduced from microns to 10-65 nm without high-energy methods.
• The optimized microemulsion demonstrated significantly enhanced antifungal activity compared to bulk fluconazole, with a minimum inhibitory concentration of 8 µg/ml.
• The microemulsion system exhibited a uniform, spherical structure.

Conclusions:

• The developed microemulsion system represents an effective oral drug delivery strategy for fluconazole.
• This novel system improves fluconazole's efficacy against Candida albicans, potentially overcoming drug resistance.
• The microemulsion formulation offers a promising approach for treating candidiasis.