Preparation, characterization and evaluation of the antioxidant capacity and antitumor activity of myricetin microparticles formated by supercritical antisolvent technology

Abstract Myricetin (MYR) shows a lot of pharmacological activity such as antioxidant capacity and antitumor activity. However, the poor aqueous solubility of MYR (2 μg/mL) limits its pharmaceutical applications. To improve the dissolution rate of MYR, microparticles and inclusion complexes of MYR were successfully prepared by supercritical antisolvent (SAS) technology. The effects of the drug concentration, temperature, pressure, CO2 and solution volumetric feeding rate on the formation of MYR microparticles and the MYR/hydroxypropyl-β-cyclodextrin (HP-β-CD) complex microparticles were investigated systematically. The physical and chemical properties of the MYR microparticles were characterized by SEM, DSC, FTIR and XRD. After SAS processed, the particle size of MYR microparticles decreased and the crystal form of MYR changed due to the complexation with HP-β-CD, which lead to enhanced solubility, dissolution rate and further improve the antioxidant activity and antitumor activity.