Sertaconazole Nitrate

Sertaconazole Nitrate is a broad-spectrum imidazole approved for topical treatment of tinea pedis. Sertaconazole has dual mechanisms: inhibition of ergosterol synthesis via P450 blockade and direct membrane disruption causing leakage of intracellular components, resulting in both fungistatic and fungicidal effects. Its lipophilic benzothiophene structure enhances stratum corneum penetration with minimal systemic absorption.
In vitro studies show potent activity against dermatophytes and Candida spp., with MIC values generally lower than bifonazole and miconazole, and comparable or superior to terbinafine for yeasts. Sertaconazole also demonstrated activity against fluconazole-resistant dermatophyte strains. Pharmacokinetic data indicate high drug concentrations in stratum corneum, far exceeding MICs.

Fig. 1 Mechanism of action of Sertaconazole Nitrate. (Pfaller M A, Sutton D A. 2006)

Sertaconazole nitrate-loaded ultraflexible liposomes were developed using the thin-film hydration-sonication technique and optimized by a 32 factorial design with phospholipid and sodium cholate concentrations as independent variables. The optimized liposomes exhibited vesicle sizes of 104.40 to 151.90 nm, zeta potential values of -21.50 to -51.20 mV, and entrapment efficiencies of 77.60 to 86.04 percent. The optimized formulation was incorporated into a carbopol gel base. Compared with the marketed formulation, the nanovesicular gel demonstrated higher drug permeation and skin deposition, a larger zone of inhibition against Candida albicans, and superior antifungal activity in a Trichophyton mentagrophytes-infected rat model.
The formulation showed no signs of skin irritation and remained stable at 4, 25, and 40°C for 3 months. The ultraflexible liposomal gel successfully enhanced the overall effectiveness of sertaconazole nitrate as a promising nanocarrier for topical antifungal therapy.

Fig. 2 In vitro antifungal activity of Sertaconazole Nitrate-UFL-Gel and marketed formulation. (Peram M R.; et al. 2025)