Transdermal platform for the delivery of the antifungal drug naftifine hydrochloride based on porous vaterite particles

Development of a skin-targeted particulate delivery system providing an extended or sustained release of the payload and a localized therapeutic effect is one of the main challenges in the treatment of fungal skin infections. In the topical administration of antifungals, the drug should penetrate into the stratum corneum and lower layers of the skin in effective concentrations. Here, we introduce biodegradable calcium carbonate carriers containing 4.9% (w/w) of naftifine hydrochloride antimycotic allowing the efficient accumulation into the skin appendages. The proposed particulate formulation ensures the enhancement of the local drug concentration, prolongation of the payload release, and control over its rate. Furthermore, it provides a highly efficient cellular uptake and excellent bioavailability in vitro and enables a deep penetration during transfollicular delivery in vivo. The enhanced fungi growth inhibition efficiency of naftifine-loaded calcium carbonate carriers compared to naftifine solution makes them a promising alternative to creams and gels currently existing on the market.

Automated summary

The development of a skin-targeted particulate delivery system that provides extended release of antifungal drugs is essential for treating fungal skin infections. The biodegradable calcium carbonate carriers containing naftifine hydrochloride showed efficient accumulation into the skin appendages, enhancing drug concentration and release control.