name of research: Design, Optimization and Characterization of Self-Nanoemulsifying Drug Delivery Systems of Bilastine

Self-nanoemulsifying drug delivery systems are innovative methods that have a potential to resolve a variety of drug formulation issues, including solubility, stability and bioavailability. Bilastine is a potent and high selective H1-antihistamine. The aimof this study is to develop bilastine as an oral self-nanoemulsion to enhance its permeability and possibility of lymphatic transport. Based on the solubility investigations of bilastine in some oils, surfactants and cosurfactants, fifteen formulas of liquid self-nanoemulsion drug delivery systems (SNEDDS) were formulated utilizing oleic acid, tween 60 and transcutol as oil, surfactant and co-surfactant respectively. Pseudoternary phase diagrams were used to evaluate the component phase behavior and the area of the nanoemulsion. The prepared formulas were evaluated for particle size, polydispersity index, zeta-potential, self-emulsification time, drug content, and robustness to dilution. When compared to the pure drug powder, the produced SNEDDS formulations showed enhanced drug release. This study showed that a formula 8 with a 20% oleic acid, 40% tween 60, and 40% transcutol composition exhibited lower particle size (71.976 ± 0.23 nm)and higher zeta-potential (-20.32) with acceptable drug content (95 %± 0.42) compared to other formulas and better in-vitro drug release characteristics than pure bilastine powder. All of these criteria favor the development of self-nano emulsifying drug delivery systems as a potential approach to enhance the bioavailability of drugs like bilastine that are poorly soluble.Keywords: Antihistaminic drug, Bilastine, SNEDDS, Transcutol, Tween 60 .Introduction Bilastine (BL) is a new, well tolerated second generation H1-antihistamine. It is indicated for the treatment of chronic spontaneous urticaria and seasonal rhino conjunctivitis (1). BL is also effective in all nasal symptoms including obstruction and in allergic conjunctivitis (2). It belongs to BCS class II (3). Its chemical formula is C28H37N3O3 and its Mwt is 463.61 Dalton, Log Pis 2.41(4). Its bioavailability is about 60%(5). Self-nanoemulsifying drugdelivery systems(SNEDDS)are lipid-based formulations that, when in contact with the aqueous medium of gastrointestinasecretionswhile being lightly stirred by peristaltic activity, generate a small oil-in-water nanoemulsion (6). The drug is presented in solubilized state in this spontaneous emulsion, and the droplets small size creates a significant amount of interfacial area on the surface for absorbing drug (7). These factors together lead to enhance bioavailability. 1Corresponding author E-mail:ishraqalmualla@yahoo.comReceived: 28/4 /2023Accepted: 22/ 6 /2023Iraqi Journal of Pharmaceutical Sciences