Development and Assessment of a Self-Nanoemulsifying Drug Delivery System Containing Bilastine: An Effective Strategy to Improve Dissolution

Background: Innovative approaches, including self-nanoemulsifying drug delivery systems, have the potential to solve a variety of drug formulation challenges, such as solubility, stability, and bioavailability. The drug candidate in this research is the strong and extremely selective H1-antihistamine, bilastine, that belongs to BCS II with low solubility and high permeability. Objective: This research aims to formulate an oral self-nanoemulsion of bilastine to improve dissolution. Methods: A total of fifteen liquid self-nanoemulsion drug delivery systems (SNEDDS) formulas were developed using oleic acid, cremophor, and Transcutol as the appropriate oils, stabilizers, and co-stabilizers based on the solubility studies of bilastine in various oils, stabilizers, and co-stabilizers. We used pseudoternary phase diagrams to look at the behavior of the component phases and the area of the nanoemulsion. The physicochemical properties of the formulas, in addition to thermodynamic stability, droplet size, polydispersity index, zeta potential, self-emulsification time, drug content, and durability of the developed formulations, were assessed. Results: This study demonstrated that formula 5, with a 20% oleic acid, 27% cremophor, and 53% Transcutol composition, had lower globular size, acceptable drug content, better in-vitro drug release, and ex-vivo permeability characteristics than pure bilastine powder. Conclusions: The mentioned factors all point to the preparation of self-nanoemulsifying drug delivery systems as a potential means for improving the dissolution of poorly soluble drugs like bilastine.