Abstract
This study aims to develop chitosan-based voriconazole nanoparticles (NPs) using spray-drying technique. The effect of surfactants and polymers on the physicochemical properties, in vitro release, and permeation of NPs was investigated. The prepared NPs containing various surfactants and polymers (e.g., Tween 20 (T20), Tween 80 (T80), sodium lauryl sulfate (SLS), propylene glycol (PG), and Polyethylene glycol-4000 (PEG-4000)) were physiochemically evaluated for size, zeta potential, drug content, percent entrapment efficiency, in vitro release, and permeation across rats’ skin. A Franz diffusion cell was used for evaluating the in vitro release and permeation profile. The voriconazole-loaded NPs were investigated for antifungal activity against Candida albicans (C. albicans). The prepared NPs were in the nano range (i.e., 160–500 nm) and positively charged. Images taken by a scanning electron microscope showed that all prepared NPs were spherical and smooth. The drug content of NPs ranged from 75% to 90%. Nanoparticle formulations exhibited a good in vitro release profile and transport voriconazole across the rat’s skin in a slow control release manner. The NPs containing SLS, T80, and PG exhibited the best penetration and skin retention profile. In addition, the formulation exhibited a potential antifungal effect against C. albicans. It was concluded that the development of chitosan NPs has a great potential for the topical delivery of voriconazole against fungal infection.
Highlights
IntroductionSuperficial fungal infections of the hair, skin, and nails form the most numerous and widespread group of all mycoses [1]
Fungal infections are one of the major healthcare problems worldwide
The lowest size of NPs was obtained from the formulations VRZNB (167 ± 8.23 nm), followed by VRZND (189 ± 7.34 nm), VRZNE (202 ± 9.12 nm), and VRZNC (210 ± 9.11 nm), which is an ideal size for the transdermal or topical drug delivery system
Summary
Superficial fungal infections of the hair, skin, and nails form the most numerous and widespread group of all mycoses [1]. They are most often caused by dermatophytes and yeasts. Voriconazole (log P: 1.8) is a second-generation triazole available in both intravenous and oral formulations [4]. It has a wide spectrum against Candida spp., Aspergillus spp., and Cryptococcus neoformans, including those resistant to other commonly used antifungal agents. Its intravenous administration is reported to cause heart rhythm problems [6]. A need exists for a topical delivery system to overcome the limitations and enhance the antifungal effect of voriconazole against cutaneous candidiasis [7]
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