Meclizine-loaded nanostructured lipid carriers to manage nausea and vomiting: Oral bioavailability improvement

Abstract

Abstract Meclizine shows poor oral bioavailability and slow onset of action due to its low water solubility and poor permeability. In the present study, meclizine-loaded nanostructured lipid carriers (NLCs) were developed to improve oral bioavailability of meclizine. NLCs were prepared using Gelucire (solid-lipid), Capryol (liquid-lipid), and Tween 80 by hot homogenization and ultrasonication techniques. Scanning electron microscopy revealed smooth and spherical shape of NLCs. Zetasizer measurements indicated the particle size of NLCs in the range of 19–155 nm. The zeta potential values (−20 to − 28 mV) suggested the stability of NLCs. The ex vivo intestinal permeability study demonstrated increase in the permeation of NLCs with decrease in the size of the nanoparticles. The pharmacokinetic profile in rabbit model demonstrated a 2.69-fold increase in oral bioavailability of NLCs (Mz-NLCs-25) compared to that of the unprocessed meclizine powder. Conclusively, the study demonstrated the potential of NLCs in improving oral bioavailability of meclizine to effectively manage vomiting and nausea during pregnancy.