Abstract
Terbinafine hydrochloride, although one of the prominent antifungal agents, suffers from low drug permeation owing to its hydrophobic nature. The approach of nanosponge formulation may thus help to resolve this concern. Thus, the present research was envisioned to fabricate the nanosponge hydrogel of terbinafine hydrochloride for topical delivery since nanosponge augments the skin retentivity of the drug. The optimized formulation was obtained using Box Behnken Design. The dependent and independent process parameters were also determined wherein polyvinyl alcohol (%), ethylcellulose (%), and tween 80 (%) were taken as independent process parameters and particle size, polydispersity index (PDI), and entrapment efficiency (EE) were the dependent parameters. The nanosponge was then incorporated into the hydrogel and characterized. In-vitro drug release from the hydrogel was 90.20 ± 0.1% which was higher than the drug suspension and marketed formulation. In vitro permeation potential of the developed formulation through rat skin showed a flux of 0.594 ± 0.22 µg/cm2/h while the permeability coefficient was 0.059 ± 0.022 cm/s. Nanosponge hydrogel was evaluated for non-irritancy and antifungal activity against C. albicans and T. rubrum confirming the substantial outcome. Tape stripping studies exhibited ten times stripping off the skin quantified 85.6 ± 0.21 μg/cm2. The confocal analysis justified the permeation potential of the prepared hydrogel. The mean erythemal score was 0.0, confirming that the prepared hydrogel did not cause erythema or oedema. Therefore, based on results obtained, nanosponge hydrogel formulation is a potential carrier for efficient topical delivery of terbinafine hydrochloride.
Highlights
Fungal infections currently account for about the fourth common disease in the world that affects millions of people every year, about 25% of the world’s population, mostly adults
The attributes, i.e., particle size, EE, and polydispersity index (PDI), were selected as CQA which offers its respective advantages towards the developed systems
Response surface methodology (RSM) is a potential optimization tool wherein, multiple factors and their interactions could be ascertained with a minimal number of experimental runs
Summary
Fungal infections currently account for about the fourth common disease in the world that affects millions of people every year, about 25% of the world’s population, mostly adults. To overcome the lacunas, hydrogels are tailored and widely used for topical application The fact that they are widely gaining impetus is attributable to their swelling property in association with their adhesiveness and potential to modulate the drug release [8]. Terbinafine hydrochloride (TH) is the fungicidal allylamine drug that kills the fungal organisms It acts as a non-competitive inhibitor of squalene epoxidase lodging within the fungi cell membrane. The highest in vivo skin deposition and antifungal activity were demonstrated in the developed formulation [16]. The purpose of the research undertaken is to formulate and optimize NS of TH and further incorporate it into the hydrogel This step would be superseded by the in vitro release and permeation studies followed by an antifungal activity.
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