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.
Method:
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 8hrs. 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.
result:
The Bilastine loaded transethosomal formulation was found to be stable, which was confirmed by the zeta potential of −27.0 mV and polydispersity index (PDI) of 0.167, vesicle size was found to be 183nm, exhibiting the maximum entrapment efficiency of up to 80.23%. It was determined that 81.56% of the transethosomal gel contained drug. The best results were obtained with a transethosomal gel which was prepared with 1