Bilastine-Loaded Transethosome Based Nanogel for the Treatment of Allergic Reactions: An In vitro Characterization

Abstract

Objective: The goal of the current study was to formulate and evaluate bilastine-loaded transethosomal nanogel. Bilastine has 60% oral bioavailability, which restricts the rate of absorption and dissolution and classifies it under BCS class II drugs, which can be overcome by incorporating bilastine in transethosomal nanogel formulation in the treatment of urticaria. Methods: Bilastine-loaded transethosomes were prepared using a thin film hydration method with different proportions of Tween 80 and ethanol by using a rotary evaporator and incorporated into a transethosomal gel using Carbopol 934 as a polymer by dispersion method. Results: The bilastine-loaded transethosomal formulation was optimized by using the “Box Behnken design” and evaluated for various parameters. The optimized formulation was found to be stable, as determined by the zeta potential of −27.0 mV and polydispersity index (PDI) of 0.167, and vesicle size was found to be 183nm and exhibiting the maximum entrapment efficiency of up to 80.23%. The drug content of the transethosomal gel was found to be 81.56%. The best results were obtained with a transethosomal gel prepared with 1% Carbopol 934 (TF7G2). The optimized batch showed prolonged in-vitro release of bilastine for 8 hrs. Ex vivo skin permeation studies showed 76.23 ± 2.63% permeation in comparison with plain gel. Conclusion: Transethosomal nanogel batches were optimized based on drug content, viscosity, uniformity of drug content, zeta potential, spreadability, pH, drug release, and stability testing, exhibiting good results. The results of this investigation showed that the transethosomal nanogel loaded with bilastine might be used to improve bilastine delivery through the skin with greater bioavailability.