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

Abstract

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 aim of 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.