Transungual Permeation of the Voriconazole Nail Lacquer Against Trichophyton Rubrum

Abstract

Voriconazole was obtained as a gift sample from Cipla Pvt. Ltd., Mumbai, India; which was chosen as the model antifungal agent. Cellulose nitrate RS, thioglycolic acid, potassium dihydrogen phosphate, and disodium hydrogen phosphate were purchased from Qualigens Fischer Scientific. Aqueous solutions were prepared using deionised water supplied by Millipore water purification system, France. The pH was analyzed using the pH meter (Lab India) ABSTRACT The oral therapies encounter side effects and topical therapies for nail diseases are limited by poor permeability of nail plate. An optimal penetration enhancer would improve drug delivery through nail plate facilitating new possibilities for treating neighboring target sites if the systemic circulation is reached. The purpose of study was to determine amount of voriconazole permeating through the nail plate from the nail lacquer formulation containing permeation enhancer and to demonstrate its susceptibility to the onchomycotic dermatophyte. The permeability studies were performed on avulsed human cadaver nail plates using modified Franz diffusion apparatus containing phosphate buffer saline in the acceptor chamber. The amount of Voriconazole permeated was quantitatively determined by the UV spectrophotometer. The amount of Voriconazole remaining in the nail after permeation had been retrieved by milling test. The addition of thioglycolic acid, 5% improved the permeability of the drug by 0.7 as the enhancement factor. The formulation followed zero order kinetics and Korsmeyer-Peppas mechanism of drug release on analyzing on DDSolver. The voriconazole flux of 5592.1 µg/cm/min and 596.75 µg/cm/min had been observed at 24 and 48 hours aliquots respectively for the nail lacquer containing an enhancer. Significantly higher permeation rates were achieved in the presence of an enhancer. The inhibitory zones for the voriconazole transungual nail lacquer were evaluated by testing against the dermatophyte, Trichophyton rubrum on Sabouraud's Dextrose Agar. The effective zones of inhibitions suggested Voriconazole nail lacquer exhibiting moderate antifungal activity for the onchomycosis treatment.

Transungual Delivery of Ketoconazole Nanoemulgel for the Effective Management of Onychomycosis

“…Apart from that, they can be formulated into a variety of formulation types, such as foams, creams, liquids, sprays and gels (13). There are many topical formulations, like nail lacquers (14)(15)(16)(17), creams (18)(19)(20), ointments (21,22), bio-adhesive patch (23) and solutions (24,25), which are being used for the treatment of nail infections, but gel is being preferred because it fulfils the required dermatological properties, such as thixotropy, greaselessness, emollient and non-staining nature, ease in spreadability, etc. Gel can be defined as a semisolid system, which consists of dispersion of particles with interpenetration of liquid.…”

Onıcomycosıs and Treatment Approaches

“…Ayrıca, geçirgenleştirici olarak tioglikolik asit kullanılan bir çalışmada kafeinin tırnaktan geçişini kolaylaştırdığı bildirilmiştir. Yapılan bir çalışmada vorikonazol tırnak cilasına %5 tiyoglikolik asit eklenmesi, ilacın geçirgenliğinin artmasıyla sonuçlanmıştır (Khengar, Jones, Turner, Forbes ve Brown, 2007;Tandel, Agrawal ve Wankhede, 2012).…”

Antifungal Nail Lacquer Loaded with Extract of Cissus quadrangularis for Treatment of Onychomycosis

“…Yellow-brown patches appear at lateral border of nail. 5,6 The masses of horny debris disperse and nail plate rapidly becomes thickened and broken. The irritation, pain and pressure also are the secondary effects.…”