Formulation and in vitro evaluation of topical nanosponge-based gel containing butenafine for the treatment of fungal skin infection

Abstract

In the current study, four formulae (BNS1-BNS4) of butenafine (BTF) loaded nanosponges (NS) were fabricated by solvent emulsification technology, using different concentration of ethyl cellulose (EC) and polyvinyl alcohol (PVA) as a rate retarding polymer and surfactant, respectively. Prepared NS were characterized for particle size (PS), polydispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE) and drug loading (DL). Nanocarrier BNS3 was optimized based on the particle characterizations and drug encapsulation. It was further evaluated for physicochemical characterizations; FTIR, DSC, XRD and SEM. Selected NS BNS3 composed of BTF (100 mg), EC (200 mg) and 0.3% of PVA showed, PS (543 ± 0.67 nm), PDI (0.330 ± 0.02), ZP (−33.8 ± 0.89 mV), %EE (71.3 ± 0.34%) and %DL (22.8 ± 0.67%), respectively. Fabricated NS also revealed; polymer-drug compatibility, drug-encapsulation, non-crystalline state of the drug in the spherical NS as per the physicochemical evaluations. Optimized NS (BNS3) with equivalent amount of (1%, w/w or w/v) BTF was incorporated into the (1%, w/w or w/v) carbopol gel. BTF loaded NS based gel was then evaluated for viscosity, spreadability, flux, drug diffusion, antifungal, stability and skin irritation studies. BNS3 based topical gels exhibited a flux rate of 0.18 (mg/cm 2 .h), drug diffusion of 89.90 ± 0.87% in 24 h with Higuchi model following anomalous non-Fickian drug release. The BNS3 based-gel could be effective against pathogenic fungal strains.

Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal Activity

“…The absence of the drug peak in BLs was due to the complete entrapment into the lipid bilayer or the solubilization of the drug in the lipid matrix. A similar type of finding was reported in the literature in a BN nanosponge [ 19 ] and tenoxicam bilosomes [ 2 ].…”

“…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 ]. It is slightly soluble in water and readily soluble in organic solvents.…”

“…They have reported prolonged drug release and enhanced drug permeation and retention with antifungal activity. In another study, Ahmed et al prepared and evaluated a butenafine nanosponge-based gel by the solvent emulsification method [ 19 ]. The prepared formulation exhibited an enhanced flux of 0.18 (mg/cm 2 h) and a drug diffusion of 89.90 ± 0.87% in 24 h. It also exhibited effective activity against pathogenic fungal strains.…”

Green Synthesized Silver Nanoparticles Using Tridax Procumbens for Topical Application: Excision Wound Model and Histopathological Studies

“…The sample solution was prepared by dispersing 1 gm of AgNPs in deionized-purified water of 10 mL. The electrode was then dipped, and reading was noted, and the measurement of the sample was performed in triplicate [30].…”

Design of Olmesartan Medoxomil-Loaded Nanosponges for Hypertension and Lung Cancer Treatments

“…We observed that the pharmacokinetic profile of these carriers was increased 1.64-fold in terms of bioavailability compared to the pure apremilast suspension [ 8 ]. Moreover, in another study, we demonstrated that butenafine-loaded NSs could enhance the therapeutic efficacy through channeling the drug deeper into the skin layers at the target site to completely eradicate fungal infections [ 15 ]. In addition, starch derivatives and especially, cyclodextrin-based NSs have recently emerged due to the excellent properties owing to their distinct structure [ 16 , 17 ].…”