Abstract
The present research work was designed to prepare butenafine (BN)-loaded bilosomes (BSs) by the thin-film hydration method. BN is a sparingly water-soluble drug having low permeability and bioavailability. BSs are lipid-based nanovesicles used to entrap water-insoluble drugs for enhanced permeation across the skin. BSs were prepared by the thin-film hydration method and optimized by the Box–Behnken design (BBD) using lipid (A), span 60 (B), and sodium deoxycholate (C) as independent variables. The selected formulation (BN-BSo) was converted into the gel using Carbopol 940 as a gelling agent. The prepared optimized gel (BN-BS-og) was further evaluated for the gel characterization, drug release, drug permeation, irritation, and anti-fungal study. The optimized bilosomes (BN-BSo) showed a mean vesicle size of 215 ± 6.5 nm and an entrapment efficiency of 89.2 ± 1.5%. The DSC study showed that BN was completely encapsulated in the BS lipid matrix. BN-BSog showed good viscosity, consistency, spreadability, and pH. A significantly (p < 0.05) high release (81.09 ± 4.01%) was achieved from BN-BSo compared to BN-BSog (65.85 ± 4.87%) and pure BN (17.54 ± 1.37 %). The permeation study results revealed that BN-BSo, BN-BSog, and pure BN exhibited 56.2 ± 2.7%, 39.2 ± 2.9%, and 16.6 ± 2.3%. The enhancement ratio of permeation flux was found to be 1.4-fold and 3.4-fold for the BN-BS-og and pure BN dispersion. The HET-CAM study showed that BN-BSog was found to be nonirritant as the score was found within the limit. The antifungal study revealed a significant (p < 0.05) enhanced antifungal activity against C. albicans and A. niger. The findings of the study revealed that BS is an important drug delivery system for transdermal delivery.
Highlights
The transdermal delivery system has been of great interest to researchers, considering the low permeability of the stratum corneum, which represents the main barrier for the skin absorption of exogenous substances [1]
The prepared formulations particle size (Y1) and entrapment efficiency (Y2) were determined. These experimental values were added to the Box–Behnken design (BBD) software to evaluate the other statistical parameters
The suitability of BBD was expressed by a high value of the coefficient of determinants (0.9932 Y1 and 0.9985 Y2)
Summary
The transdermal delivery system has been of great interest to researchers, considering the low permeability of the stratum corneum, which represents the main barrier for the skin absorption of exogenous substances [1]. Different bilosomes have been prepared and evaluated for in vitro and in vivo studies [10,11,12] They have reported nano-sized vesicles and enhanced permeation and release of tested drugs. Butenafine (BN) is a broad-spectrum antifungal drug that belongs to benzylamine and has a potent fungicidal activity [18] It acts by preventing the biosynthesis of ergosterol and inhibiting the squalene monooxygenase enzyme [19]. There are different BN-loaded nanoformulations: PLGA-NP-laden chitosan nano-gel and NLCs-based gel were prepared and evaluated for different parameters [20,21] They have reported prolonged drug release and enhanced drug permeation and retention with antifungal activity. The prepared formulations particle size (Y1) and entrapment efficiency (Y2) were determined These experimental values were added to the BBD software to evaluate the other statistical parameters. Composition of butenafine bilosomes with vesicle size (Y1) and entrapment efficie3nocfy1(7Y2)
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
