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

Mohammed Muqtader Ahmed; Farhat Fatima; Md Khalid Anwer; Elmutasim Osman Ibnouf; Mohd Abul Kalam; Aws Alshamsan; Mohammed F Aldawsari; Ahmed Alalaiwe; Mohammad Javed Ansari

doi:10.1016/j.jsps.2021.04.010

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

Saudi Pharm J. 2021 May;29(5):467-477. doi: 10.1016/j.jsps.2021.04.010. Epub 2021 Apr 27.

Authors

Mohammed Muqtader Ahmed¹, Farhat Fatima¹, Md Khalid Anwer¹, Elmutasim Osman Ibnouf², Mohd Abul Kalam³, Aws Alshamsan³, Mohammed F Aldawsari¹, Ahmed Alalaiwe¹, Mohammad Javed Ansari¹

Affiliations

¹ Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, P.O. Box 173, AlKharj 11942, Saudi Arabia.
² Department of Pharmaceutical Microbiology College of Pharmacy, Prince Sattam Bin Abdulaziz University, P.O. Box 173, AlKharj 11942, Saudi Arabia.
³ Nanobiotechnology Unit, Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.

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/cm².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.

Keywords: Antifungal study; Flux; In-vitro diffusion; Nanosponges; Topical gel.