DEVELOPMENT AND OPTIMIZATION OF FAST-DISSOLVING BILASTINE SUBLINGUAL FILMS USING STATISTICAL DESIGN

Objective: This present research study was undertaken with the objective of formulating a fast-dissolving sublingual film of pre-solubilized bilastine. The aim was to overcome the need for acidic gastric media for the solubilization of bilastine, eliminating the concern of reduced bioavailability due to interaction with food and providing a faster onset of action, owing to the high vascularity in the sublingual region. Methods: Solubility enhancement of bilastine was achieved by inclusion-complex formation of bilastine and Hydroxypropyl Beta-Cyclodextrin (2-HP-β-CD). Fast-dissolving sublingual films were formulated by incorporating bilastine-2-HP-β-CD in the film prepared using the solvent casting method, wherein the sublingual film formulation was optimized using the Design of Experiments (DoE) approach by applying 23 factorial designs. The optimized sublingual film was evaluated. Results: Evaluation tests revealed that the optimized sublingual film possessed adequate flexibility and tensile strength. It exhibited a faster in vitro drug release of 97.41%, which was achieved in 7 min compared to a 35.77% in vitro drug release demonstrated by the pure drug-containing film. This indicates a 2.7-fold enhancement in dissolution with an average disintegration time of 41.66±0.57 s. The ex vivo permeation studies showed an in vitro drug release of 95.21%, indicating good permeation. Conclusion: Based on the research findings obtained, it is possible to conclude that the developed quick-dissolving sublingual film of bilastine possessed an enhanced dissolution profile and exhibited a faster onset of action. These results demonstrate the potential to avoid food interactions and improve patient compliance. Incorporating bilastine into sublingual films offers superior benefits over conventional oral formulations, such as circumventing hepatic first-pass metabolism and providing quick relief. Thus, it serves as a potential alternative for the treatment of chronic urticaria and allergic rhinitis.