Bilastine

Oudah SA, et al. OpenNano, 2025, 21, 100230.

Bilastine was engineered into a nanosuspension to overcome its poor solubility and limited oral bioavailability. Using an anti-solvent precipitation method, bilastine (10 mg) dissolved in methanol was introduced at 0.5 mL/min into deionized water containing hydrophilic stabilizers, with anti-solvent/solvent ratios of 3:1-7:1. Continuous stirring (500-1500 rpm) facilitated nucleation and solvent evaporation, enabling precise control of particle size. Experimental design optimization identified Soluplus at a 1:1 stabilizer-to-drug ratio, a 6:1 anti-solvent ratio, and 820 rpm stirring as optimal, yielding ~84 nm particles with a narrow PDI. The lyophilized nanosuspension was subsequently incorporated into orodispersible films using solvent casting with PVA/HPMC matrices, producing rapidly disintegrating films that significantly enhanced bilastine dissolution performance.

Bodapati ATS, et al. Journal of Molecular Structure, 2024, 1301, 137385.

This case study demonstrates the experimental characterization of Bilastine binding to calf thymus DNA (ct-DNA), emphasizing its minor groove association. UV-visible spectroscopy revealed hypochromic effects and yielded a binding constant on the order of 10⁵ M⁻¹, indicating moderate affinity. Fluorescence quenching experiments, performed across 298-308 K, showed temperature-dependent static and dynamic quenching, enabling thermodynamic analysis that identified hydrophobic forces as the dominant driving mechanism (ΔH° ≈ 41.5 kJ mol⁻¹; ΔS° ≈ 236 J mol⁻¹ K⁻¹). Site-specific probing using ethidium bromide and Hoechst dyes, together with viscosity and DNA melting assays, experimentally confirmed Bilastine's preference for the minor groove rather than intercalation. Circular dichroism spectra demonstrated that the binding event did not perturb the B-form DNA conformation. Complementary molecular docking positioned Bilastine along the DNA minor groove curvature, reinforcing the experimentally observed binding mode.