Development and Evaluation of Luliconazole-Loaded Microsponge Gel for Improved Topical Retention and Reduced Irritation

Purpose

Traditional topical therapies often require high drug concentrations, leading to irritation and poor patient compliance. The aim of this study is to develop a microsponge-based gel formulation of Luliconazole that enables controlled drug release, enhances retention within the skin layers, and reduces the irritation.

Methods

Luliconazole microsponge were formulated using solvent diffusion method using a quasi-emulsion system and optimized through a 3² factorial design to study the effects of Eudragit S-100 and Dichloromethane. The microsponges were evaluated for their particle size, drug entrapment efficiency, and in vitro release profile. The optimized formulation was then incorporated into a Carbopol-based gel, which was subsequently assessed for its physicochemical characteristics, in vitro drug release, antifungal efficacy against Candida albicans, and for skin irritation.

Results

The optimized microsponge had a particle size of 30–70 µm, entrapment efficiency of 91.35 ± 1.06 %, and controlled drug release (83.67 ± 2.11 % of LCZ over 12 h). The gel showed suitable pH (6.8–7.4), viscosity (2160 cPs), and higher drug content in LCZMG3 compared to other formulations. The antifungal study demonstrated a clear zone of inhibition, and skin irritation tests showed minimal irritation with controlled release and prolonged drug retention in skin layers.

Conclusion

The luliconazole microsponge gel exhibited superior antifungal activity, reduced irritation, and improved local drug retention compared to marketed preparations. This novel formulation holds promise for effective, patient-friendly treatment of fungal infections with enhanced compliance.