Polymeric nanocapsules containing ozonated oil and terbinafine hydrochloride as a potential alternative treatment against dermatophytes

Abstract

Terbinafine hydrochloride (TBF) is a synthetic allylamine whose mechanism of action consists of inhibiting an enzyme squalene epoxidase which participates in the first stage of ergosterol synthesis preventing cell membrane formation and promoting a fungistatic effect. Ozonated oils are used as a form of topical application of ozone, which is a promising treatment for acute and chronic skin infections, producing reactive oxygen species (ROS) that cause cellular damage and death of microorganisms. This study aimed to develop and characterize polymeric nanocapsules, obtained by interfacial deposition of preformed polymer method, containing 0.5% TBF and 5% ozonated sunflower seed oil (OZ) with potential treatment against dermatophytosis. The polymeric nanocapsules were characterized by particle size, zeta potential, pH, drug content, encapsulation efficiency and stability. We also evaluated the in vitro drug release, in vitro skin permeation and in vitro antifungal activity. The particle size was around 150 nm (PDI of 0.12 and Span 1.13), the zeta potential was around +6, the pH was 2.2. The drug content was around 94% with an encapsulation efficiency of 53%. The nanocapsule were capable to control the drug release and the skin permeation. The in vitro susceptibility test showed greater potential of the nanocapsules containing TBF and OZ against all strains of dermatophytes tested, compared to the drug solution. Therefore, the developed polymeric nanocapsules containing TBF and OZ can be considered potential candidate for the treatment of dermatophytosis, with possible high efficacy and reduction in frequency of applications.