Formulation development of Sertaconazole loaded nanoemulsion and gel for the management of deep skin fungal infection: in vitro, ex-vivo and in vivo characterizations
摘要
The aim of the current study was to prepare nanoemulsion and gel system for Sertaconazole to enhance its ability to target deep skin fungal infections. The nanoemulsion and gel were physicochemically evaluated for size, zetapotential, morphology, entrapment efficiency, drug content (n = 3) followed by in vitro release using phosphate buffer solution pH 5.5, ex vivo permeation and skin retention studies using phosphate buffer solution pH 7.4 as the receptor medium. In vivo study was performed in rats (n = 3) to compare the antifungal efficacy of prepared nanoemulsion and gel system with commercial cream. Drug is compatible with excipients and polymer used as suggested by ATR-FTIR analysis. The size and zeta potential of nanoemulsion were in the range of 182.87 ± 0.36 to 201.25 ± 0.58 nm and − 8.35 ± 0.02 to -12.3 ± 0.57mV, and globule shape is almost spherical. The in vitro release of nanoemulsion was 86.4% to 96.30%, which is controlled by incorporating into gel system (65.4% to 81.2%). Nanoemulsion loaded gel showed controlled release and permeation behavior as compared to simple nanoemulsion. Skin drug retention is higher in case of gel as compared to nanoemulsions (FSNEG6-19.3%; FSNE6-11.4%). Maximum skin drug retention was observed with FSNEG6 consisting of tween 80, PEG400, almond oil and carbopol, showing enhanced skin penetration. The nanoemulsion and gel system is non-irritant when applied on rats’ skin. The in vivo study revealed significant treatment effect of optimized gel formulation (FSNEG6) as compared to nanoemulsion and commercial cream. Thus, it was concluded that the developed nanoemulsion gel maybe considered as an effective delivery system for Sertaconazole into deep skin layers for effective treatment of fungal infections.