Sulconazole-Loaded Solid Lipid Nanoparticles for Enhanced Antifungal Activity: In Vitro and In Vivo Approach

Area of Science:

• Pharmaceutical Sciences
• Nanotechnology
• Dermatology

Background:

• Topical delivery of hydrophobic drugs for infectious diseases faces challenges with conventional formulations.
• Solid lipid nanoparticles (SLNs) offer potential for cell-specific delivery and sustained release of hydrophobic drugs.

Purpose of the Study:

• To fabricate and optimize sulconazole (SCZ)-loaded solid lipid nanoparticles (SLNs).
• To formulate an SLN-based topical gel for enhanced antifungal activity.
• To evaluate the efficacy of the developed formulation against fungal infections.

Main Methods:

• SLNs were prepared using glyceryl monostearate, Phospholipon® 90 H, and tween 20, then characterized for size, PDI, zeta potential, and encapsulation efficiency.
• Sulconazole-loaded SLNs (SCZ-SLNs) were incorporated into a carbopol-based gel, optimized for rheological properties and skin compatibility.
• Antifungal activity was assessed in vitro against Candida albicans and Trichophyton rubrum, and in vivo in rabbits with induced skin fungal infections.

Main Results:

• Optimized SCZ-SLNs exhibited favorable characteristics: particle size (89.81 ± 2.64 nm), PDI (0.311 ± 0.07), zeta potential (-26.98 ± 1.19), and high encapsulation efficiency (86.52 ± 0.53%).
• Sustained drug release of 85.29% was observed over 12 hours.
• The SLN-based topical gel showed enhanced antifungal activity compared to a conventional SCZ gel and promoted faster healing of skin fungal infections in rabbits with restored dermal architecture.

Conclusions:

• Formulating solid lipid nanoparticles into a topical gel is an effective strategy for delivering hydrophobic drugs against fungal infections.
• The developed SLN-based gel offers an advantageous drug delivery system for treating mycosis, improving therapeutic outcomes.