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Int J Pharm ; 585: 119400, 2020 Jul 30.
Article in English | MEDLINE | ID: mdl-32512222

ABSTRACT

Drug delivery into the human nail plate for the treatment of onychomycosis is difficult due to limited permeability of the nail plate. Semisolid poloxamer 407-based formulations have recently shown promising results for drug delivery into and through the nail plate. In this study, liquid poloxamer 407-based emulsions loaded with sertaconazole nitrate have been developed and the permeation behavior was determined in vitro using modified Franz diffusion cells. The antifungal efficacy was evaluated in an infected nail plate model, where the growth inhibition of Trichophyton rubrum was observed. Bovine hoof plates and keratin films made from human hair were used as models for the human nail plate. In both cases, formulations with low viscosity and high water content showed best results despite a lower solubility of sertaconazole nitrate, suggesting that the composition of the vehicle plays a major role in permeation through the membrane. In addition, an API content close to saturation solubility had a positive effect on permeation.


Subject(s)
Antifungal Agents/pharmacology , Chemistry, Pharmaceutical/methods , Emulsions/chemistry , Imidazoles/pharmacology , Poloxamer/chemistry , Thiophenes/pharmacology , Trichophyton/drug effects , Animals , Cattle , Hair , Hoof and Claw/metabolism , Humans , Keratins/metabolism , Microbial Sensitivity Tests , Solubility , Viscosity
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