Development of carvedilol-cyclodextrin inclusion complexes using fluid-bed granulation: a novel solid-state complexation alternative with technological advantages

Objectives This study sought to evaluate the achievement of carvedilol (CARV) inclusion complexes with modified cyclodextrins (HP beta CD and HP gamma CD) using fluid-bed granulation (FB). Methods The solid complexes were produced using FB and spray drying (SD) and were characterised by differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), powder X-ray diffraction, SEM, flowability and particle size analyses and in vitro dissolution. Key findings The DSC, FTIR and powder X-ray diffraction findings suggested successful CARV inclusion in the modified beta- and gamma-cyclodextrins, which was more evident in acidic media. The CARV dissolution rate was similar to 7-fold higher for complexes with both cyclodextrins prepared using SD than for raw CARV. Complexes prepared with HPbCD using FB also resulted in a significant improvement in dissolution rate (similar to 5-fold) and presented superior flowability and larger particle size. Conclusions The findings suggested that FB is the best alternative for large-scale production of solid dosage forms containing CARV. Additionally, the results suggest that HP gamma CD could be considered as another option for CARV complexation because of its excellent performance in inclusion complex formation in the solid state.