Microemulsion based topical hydrogel of sertaconazole: formulation, characterization and evaluation

Area of Science:

• Pharmaceutical Sciences
• Dermatology
• Drug Delivery Systems

Background:

• Cutaneous fungal infections pose a significant therapeutic challenge.
• Topical drug delivery systems require optimization for enhanced efficacy.
• Microemulsions offer potential for improved drug permeation and stability.

Purpose of the Study:

• To develop and characterize a microemulsion-based hydrogel for topical sertaconazole delivery.
• To evaluate the in vitro and ex vivo performance of the developed hydrogel.
• To assess the efficacy and safety of the formulation for treating fungal infections.

Main Methods:

• Microemulsion regions were determined using pseudo-ternary phase diagrams.
• Hydrogel formulations of sertaconazole microemulsions (HSM) were prepared using oleic acid, Tween 80, propylene glycol, and water.
• Characterization included in vitro and ex vivo permeation studies, skin retention analysis, and skin sensitivity tests on rabbits.

Main Results:

• An optimized formulation (HSM-4) demonstrated significantly higher sertaconazole permeation rates compared to other HSMs and a commercial cream.
• HSM-4 exhibited enhanced skin drug retention (3x higher than commercial cream) and stability.
• HSM-4 showed a larger zone of inhibition against Candida albicans and no signs of skin irritation in animal studies.

Conclusions:

• The microemulsion-based hydrogel (HSM-4) is a promising topical delivery system for sertaconazole.
• The formulation enhances drug permeation and retention, leading to improved antifungal activity.
• This approach may allow for reduced sertaconazole concentration in treating cutaneous fungal infections.