Ex Vivo Permeation Study of Terbinafine Hydrochloride From Nanostructured Lipid Carriers-based Formulation

Background: Nanostructured lipid carriers (NLCs) are emerging as the second generation of lipid nanoparticles to solve the shortcomings of the first generation (structured lipid carriers). Terbinafine hydrochloride is used to treat various fungal skin diseases. Objectives: The study’s main objective was to study the drug release and permeation between NLC and NLC-based gel formulation to select the better one. Methods: A central composite face-cantered (α=1) design with two components (the amount of liquid lipid and the homogenization speed) and 13 runs were used through Design-Expert® software (version 7.1.5). Terbinafine hydrochloride-loaded NLC (TH_NLC) was produced by using the hot-homogenization technique. Fourier transform infrared study was done to determine drug excipients’ compatibility. Dynamic light scattering (DLS) was employed to determine particle size. Utilizing scanning electron microscopy (SEM), the morphology and shape of the TH_NLC formulation were examined. The hydrogel was filled with the optimized products chosen by point prediction in design expert software. These products were assessed by their pH, spreadability, viscosity, homogeneity, extrudability, and drug content. The in vitro drug release study and the ex vivo permeation investigation for the optimized TH_NLCopt and TH_NLCopt gel formulation were carried out using Franz diffusion cells Results: The formulation contains nanoscale particles, as evidenced by the size range of the particles (17.57 to 329.4 nm). Entrapment efficiency was 60.95% and 98% for TH_NLCopt TH_NLCopt gel, respectively. Within 7 hours, 96.35% and 83.37% of the drug were released from optimized NLC and NLC-based gel, respectively. The amount of drug that had penetrated the skin in 7 hours ranged from 54.19% to 31.16%, with a retention range of 22.46% to 61.87%. Conclusion: The topical delivery of the TH_NLC-based gel system is quite promising.