Optimizing fluconazole-embedded transfersomal gel for enhanced antifungal activity and compatibility studies

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Dermatology

Background:

• Fungal infections pose a significant global health challenge.
• Fluconazole is a widely used antifungal medication.
• Developing advanced drug delivery systems can improve therapeutic outcomes.

Purpose of the Study:

• To formulate and characterize a fluconazole-loaded transfersomal gel for topical antifungal treatment.
• To optimize the formulation using a central composite design.
• To evaluate the enhanced drug diffusion and antifungal efficacy of the transfersomal gel.

Main Methods:

• Transfersomes were prepared using the thin-film hydration technique with soya lecithin and Span 80.
• Formulation optimization was guided by a central composite design, analyzing entrapment efficiency and in vitro drug diffusion.
• The optimized formulation was incorporated into a xanthan gum gel base and subjected to comprehensive physicochemical, in vitro, ex vivo, and antifungal evaluations.

Main Results:

• Differential Scanning Calorimetry (DSC) confirmed compatibility between fluconazole and soya lecithin.
• Optimized transfersomal gel exhibited high entrapment efficiency (95.0% ± 2.2%) and significant in vitro drug diffusion (81% ± 2%).
• Scanning Electron Microscopy (SEM) revealed well-formed spherical transfersomes, and ex vivo studies indicated enhanced antifungal potential.

Conclusions:

• Fluconazole-loaded transfersomal gel offers a promising approach for improved topical antifungal therapy.
• The developed formulation demonstrates enhanced drug permeation and potent antifungal activity.
• Transfersomal technology can be effectively utilized to improve the delivery of antifungal agents like fluconazole.