New Polyurethane Nail Lacquers for the Delivery of Terbinafine: Formulation and Antifungal Activity Evaluation

作者：Gregori Valdes Barbara S; Serro Ana Paula; Gordo Paulo M; Silva Alexandra; Goncalves Lidia; Salgado Ana; Marto Joana; Baltazar Diogo; dos Santos Rui Galhano; Bordado Joao Moura; Ribeiro Helena Margarida^*

来源：Journal of Pharmaceutical Sciences, 2017, 106(6): 1570-1577.

DOI：10.1016/j.xphs.2017.02.017

• polyurethane
• nail lacquers
• morphology
• biocompatibility
• bioadhesion
• wettability
• terbinafine
• in vitro release
• antifungal activity

Onychomycosis is a fungal nail infection. The development of new topical antifungal agents for the treatment of onychomycosis has focused on formulation enhancements that optimize the pharmacological characteristics required for its effective treatment. Polyurethanes (PUs) have never been used in therapeutic nail lacquers. The aim of this work has been the development of new PU-based nail lacquers with antifungal activity containing 1.0% (wt/wt) of terbinafine hydrochloride. The biocompatibility, wettability, and the prediction of the free volume in the polymeric matrix were assessed using a human keratinocytes cell line, contact angle, and Positron Annihilation Lifetime Spectroscopy determinations, respectively. The morphology of the films obtained was confirmed by scanning electron microscopy, while the nail lacquers' bioadhesion to nails was determined by mechanical tests. Viscosity, in vitro release profiles, and antifungal activity were also assessed. This study demonstrated that PU-terbinafine-based nail lacquers have good keratinocyte compatibility, good wettability properties, and adequate free volume. They formed a homogenous film after application, with suitable adhesion to the nail plate. Furthermore, the antifungal test results demonstrated that the terbinafine released from the nail lacquer Formulation A PU 19 showed activity against dermatophytes, namely Trichophyton rubrum.

• 出版日期2017-6
• 单位河北医科大学