Abstract: One of the progressive ways for increasing oral bioavailability of drug substances with poor solubility is nanoparticles preparation. Glibenclamide (Biopharmaceutical Classification System class II) was chosen as a model compound with low solubility and high permeability. Nanoparticles were prepared either by the antisolvent precipitation – solvent evaporation method or by the emulsion solvent evaporation method. Sodium dodecyl sulphate and macrogol 6000 were used as stabilizing excipients in aqueous solutions with the mass concentrations of 1, 3 and 5%. Acetone and dichloromethane were used as glibenclamide solvents. Ten samples were characterized by dynamic light scattering. The particles size of seven samples ranged from 4.4 to 27.0 nm.