Potential of Naftifine Application for Transungual Delivery

Abstract

<jats:p>Naftifine is used to treat fungal skin infections as it inhibits dermatophytes, which are the cause of onychomycosis. However, naftifine’s ability to permeate the human nail barrier has not been investigated, thus, the antimycotic potential is not clearly established. This work aims to evaluate the effect of penetration enhancing factors on the accumulation of naftifine hydrochloride through human nail clippings. Naftifine polymeric nail lacquers with Eudragit RL100 were developed as a suitable delivery system. Low penetration of naftifine into nail has been determined as less than 10% of applied drug dose accumulated in the nail layers. Incorporation of thioglycolic acid into formulations resulted in increased accumulation of antifungal agent in the nail layers by 100% compared with a control group. Salicylic acid did not effect naftifine accumulation in the human nail. The permeation of naftifine through the nail increased by threefold when the thioglycolic acid-containing formulation was applied and the nail was pretreated with a fractional CO2 laser. Structural changes of the nail barrier, induced by fractional CO2 laser, were visualized by microscopy. The results suggest, that naftifine nail penetration could be significantly increased when physical and chemical enhancing factors are applied.</jats:p>

Quality by Design Guided Development of Polymeric Nanospheres of Terbinafine Hydrochloride for Topical Treatment of Onychomycosis Using a Nano-Gel Formulation

“…We used a multi-mechanism permeation enhancing pretreatment approach containing TGA and PEG 400, both having a demonstrated ability to enhance the permeability of nails [ 83 , 84 ]. TGA is a thiol permeation enhancer known to disrupt the disulfide bridges linking keratin molecules, and PEG 400 is a humectant which can cause hydration and swelling of the nail plate [ 85 ]. We believed that the dual enhancer pretreatment strategy could achieve better permeation enhancement of the nail plate by hydrating and swelling the nail plates and simultaneously disrupting disulfide linkages at a deeper level, because TGA could reach more deeply into the swollen nail plate.…”

Contemporary Techniques and Potential Transungual Drug Delivery Nanosystems for The Treatment of Onychomycosis

“…• Eudragit RS100 was used with triacetin (plasticizer) and affected the release of naftifine hydrochloride, while the incorporation of ethyl cellulose polymer was not applicable [66] Nail lacquer • The incorporation of thioglycolic acid enhanced the accretion of the drug in the nails by 100% compared to a control group, with a threefold increase in the permeation of the drug • A fractional CO 2 laser was used to enhance drug permeation [67] Table Terbinafine HCl Inhibition of squalene epoxidase, where the irreversible inhibition of this enzyme promotes intracellular squalene accumulation, resulting in the disruption of cell wall integrity…”