Formulation and evaluation of itraconazole-loaded film-forming solutions for treatment of onychomycosis

Abstract

The formulations of film-forming solutions containing itraconazole (ITZ) were developed using clove oil, dichloromethane (DCM), isopropyl alcohol (IPA), polyvinyl butyral (PVB), polysorbate 80 (P80), and water as excipients for topical treatment of onychomycosis. Their physicochemical properties, stability, in vitro release, and antifungal activity were evaluated. The optimal formulations were transparent viscous solutions which formed translucent films within 10 min after application. Formulation components, especially PVB and P80, influenced on characteristics of the film-forming solutions and their resultant films. The stability data indicated that three formulations, i.e., F4, F7, and F8, were physically and chemically stable at room temperature (RT: 25℃) for three months. The data obtained from the stable formulations showed that they sustained drug release up to 24 h and kinetic profiles fitted to Korsmeyer and Peppas model. The synergistic antifungal activity of clove oil and ITZ against C. albicans and T. rubrum was found in all stable formulations. In summary, ITZ-loaded film-forming solutions have been proven to be good alternatives for treatment of onychomycosis.