Polymeric microparticles-based formulation for the eradication of cutaneous candidiasis: development and...

Area of Science:

• Pharmaceutical Sciences
• Dermatology
• Nanotechnology

Background:

• Cutaneous candidiasis is a common fungal infection, often severe in AIDS patients.
• Conventional topical treatments (creams, gels) cause adverse skin effects and systemic absorption.
• Novel drug delivery systems are needed to improve topical antifungal therapy.

Purpose of the Study:

• To prepare and characterize clotrimazole-loaded poly(lactic-co-glycolic acid) (PLGA) microspheres for targeted dermal delivery.
• To evaluate the efficacy of PLGA microspheres in a gel formulation for treating cutaneous candidiasis.

Main Methods:

• Clotrimazole-loaded PLGA microspheres were prepared using an oil-in-water emulsion evaporation technique.
• Microspheres were characterized for particle size, entrapment efficiency, and skin penetration.
• Antifungal activity was assessed in experimentally induced cutaneous candidiasis in immunosuppressed guinea pigs.

Main Results:

• Optimized PLGA microspheres had a particle size of 2.9 µm and 74.85% drug entrapment.
• Microsphere gel showed significantly higher skin drug retention compared to marketed gel.
• Confocal microscopy confirmed microsphere penetration up to 50 µm into the dermal layer.
• In-vivo studies demonstrated superior therapeutic activity and lower fungal load with the microsphere gel.

Conclusions:

• PLGA microspheres are effective carriers for targeted dermal delivery of clotrimazole.
• This novel system overcomes limitations of conventional topical antifungal formulations.
• PLGA microparticulate systems show promise for treating invasive fungal infections.