Abstract

LIPOSPHERE-BASED FLUCONAZOLE GEL: AN EFFICIENT TOPICAL CARRIER FOR ANTIFUNGAL TREATMENT

Manu N.*, Sudha B. S.

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Abstract

This study aimed to design and characterize fluconazole-loaded lipospheres to enhance the drug’s solubility, skin permeation, and local bioavailability. Fluconazole, a third-generation triazole antifungal agent, is widely used in the treatment of systemic and superficial fungal infections. As a BCS Class II drug with low aqueous solubility and high permeability, its oral bioavailability remains limited. To overcome these drawbacks, fluconazole-loaded lipospheres were formulated for topical delivery using the melt-dispersion method. Method and Results: Preformulation studies included UV-spectrophotometric analysis, drug–excipient compatibility by FTIR, and solubility determination. The calibration curve of fluconazole was linear in the range of 10–100 μg/mL. FTIR spectra confirmed no significant interaction between drug and excipients. Lipospheres were prepared using stearic acid and compritol as core lipids and soya lecithin as a stabilizer. The prepared formulations were evaluated for particle size, entrapment efficiency, drug content, and in vitro release. Particle sizes ranged from 45 μm to 95.8 μm, entrapment efficiency from 51.7% to 89.5%, and drug content from 55.74% to 96.27%. Among the batches, formulations F2 and F5 exhibited optimal characteristics and were incorporated into a topical gel. The gel showed a pH of 5.75, viscosity of 3144 cP, spreadability of 11.33 g·cm², and 96.21% drug release. Conclusion: The optimized liposphere-based gel demonstrated enhanced fluconazole release and favorable physicochemical properties compared to conventional formulations. The findings suggest that lipospheres are a promising delivery system for improving the topical bioavailability and enhanced permeation of poorly water-soluble drugs like fluconazole.

Keywords: Fluconazole, lipospheres, topical delivery, antifungal, melt dispersion, sustained release.