PREPARATION AND CHARACTERIZATION OF RESVERATROL/HYDROXYPROPYL‐<i>β</i>‐CYCLODEXTRIN INCLUSION COMPLEX USING SUPERCRITICAL ANTISOLVENT TECHNOLOGY

Abstract

ABSTRACT The inclusion complex of resveratrol (RV) and hydroxypropyl‐ β ‐cyclodextrin (HP‐ β ‐CD) prepared by supercritical antisolvent (SAS) process was investigated to improve its aqueous solubility. The phase solubility diagram with HP‐ β ‐CD was classified as A L type, and the calculated apparent complexation constant (K C ) was 5,988 M −1 at 298K. Inclusion complexes were analyzed by differential scanning calorimetry (DSC), powder X‐ray diffractometry (PXRD), Fourier‐transform infrared spectroscopy (FT‐IR) and scanning electron microscopy (SEM). No endothermic and characteristic diffraction peaks corresponding to RV were observed for the inclusion complex in DSC and PXRD. FT‐IR study demonstrated the presence of intermolecular hydrogen bonds between RV and HP‐ β ‐CD in inclusion complex, resulting in the formation of amorphous form. Furthermore, the SAS‐processed RV/ HP‐ β ‐CD powders showed a significant enhancement in the solubility of RV (up to 25.13 mg/mL) in an aqueous medium. The percent dissolution of RV increased considerably and about 100% of RV was dissolved within 5–10 min. PRACTICAL APPLICATIONS In this study, the supercritical antisolvent (SAS) process was effectively utilized to prepare solid‐state inclusion complexes of resveratrol (RV) and hydroxypropyl‐ β ‐cyclodextrin (HP‐ β ‐CD). The SAS‐processed RV/HP‐ β ‐CD powders showed a significant enhancement in the solubility of RV (up to 25.13 mg/mL) in an aqueous medium. The percent dissolution of RV increased considerably and about 100% of RV was dissolved within 5–10 min. This work thoroughly overcomes the high hydrophobicity and sensitivity of resveratrol to air and light, so that obviously enlarges the application in pharmaceutical, chemical, food and cosmetic industries.