The formation of inclusion complexes between beta-cyclodextrin with the two beta-blockers, atenolol and celiprolol, have been studied in the aqueous environment and in the solid state by nuclear magnetic resonance (NMR) spectroscopy, X-ray, differential scanning calorimetry (DSC) and scanning electron microscopy (SEM) techniques. The magnitude of the chemical shifts of the interior and exterior beta-cyclodextrin protons in the presence of each beta-blocker indicated that these are included within the beta-cyclodextrin cavity. In aqueous solution they form 1:1 complexes. In the solid state the formation of the beta-cyclodextrin/atenolol (celiprolol) complexes is confirmed by X-ray, DSC and SEM, also employed to characterize pure substances and their physical mixtures.