Characterization of in vitro and in vivo bioactivity of a ferulic acid-2-Hydroxypropyl-β-cyclodextrin inclusion complex.

Ferulic acid (FA) belongs to the family of phenolic acids and exhibits a wide variety of biological activities. However, the bioavailability of FA is not optimal, owing to its limited aqueous solubility. Several methods have been developed to increase FA bioavailability and enhance its cytoprotective effects. Complexing FA with cyclodextrins (CDs) may provide an alternative method to approach these goals. In this study, we prepared an FA-2-hydroxypropyl-β-CD (FA-HP-β-CD) complex, at a 1:1 M ratio of FA to HP-β-CD, which was characterized by 1H NMR, two-dimensional rotating frame spectroscopy and differential scanning calorimetry. Aqueous solubility of FA was improved after complexing with HP-β-CD. Furthermore, in vitro and in vivo experimental results indicated that the FA-HP-β-CD complex had greater bioactivity than FA alone. Therefore, we can conclude that the limitations of FA usage due to low aqueous solubility and bioavailability can be overcome by creating an HP-β-CD inclusion complex with the hydrophobic FA.