Topical antifungal bigels: Formulation, characterization and evaluation

Area of Science:

• Pharmaceutical Sciences
• Dermatology
• Materials Science

Background:

• Topical antifungal treatments are crucial for managing superficial mycoses.
• Bigels offer a versatile drug delivery system combining hydrogel and oleogel properties.
• Ciclopirox olamine and terbinafine hydrochloride are established antifungal agents.

Purpose of the Study:

• To formulate and characterize bigels containing ciclopirox olamine and terbinafine hydrochloride for topical antifungal therapy.
• To evaluate the physical stability and drug release profiles of the developed bigels.
• To assess the in vitro antifungal efficacy against Microsporum canis.

Main Methods:

• Bigels were prepared using poloxamer 407 hydrogel and a polyethylene/liquid paraffin oleogel mixture.
• Physical stability was assessed at room temperature and elevated temperature (40 °C).
• In vitro drug release studies were conducted, varying drug incorporation and oleogel concentration.
• Antifungal activity was evaluated against Microsporum canis.

Main Results:

• Bigels exhibited excellent physical stability for at least six months at room temperature and four months at 40 °C.
• Increased oleogel concentration reduced the amount of drug released.
• Drug release varied based on the incorporation site of ciclopirox olamine and terbinafine hydrochloride.
• Optimal drug incorporation led to the highest release rates.
• All bigel formulations demonstrated significant inhibition of Microsporum canis growth.

Conclusions:

• Bigels incorporating ciclopirox olamine and terbinafine hydrochloride are physically stable and effective topical antifungal formulations.
• The drug release characteristics can be modulated by formulation composition and drug incorporation strategy.
• These bigels represent a promising drug delivery system for topical treatment of fungal infections.