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

• Published in: Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2019-08, Vol.180, p.68-74
• Main Authors: Hsu, Chin-Mu, Yu, Song-Cu, Tsai, Fuu-Jen, Tsai, Yuhsin
• Format: Article
• Language: English
• Subjects: 2-Hydroxypropyl-beta-cyclodextrin - chemistry; 2-Hydroxypropyl-beta-cyclodextrin - pharmacology; 2-Hydroxypropyl-β-cyclodextrin; Animals; Bioactivity; Biocompatible Materials - chemistry; Biocompatible Materials - pharmacology; Carbon Tetrachloride - administration & dosage; Cell Line, Tumor; Cell Survival - drug effects; Chemical and Drug Induced Liver Injury - drug therapy; Chemical and Drug Induced Liver Injury - metabolism; Chemical and Drug Induced Liver Injury - pathology; Coumaric Acids - chemistry; Coumaric Acids - pharmacology; Ferulic acid; Glycoconjugates - chemistry; Glycoconjugates - pharmacology; Hepatocytes - cytology; Hepatocytes - drug effects; Humans; Hydrophobic and Hydrophilic Interactions; In vitro; In vivo; Liver - drug effects; Liver - metabolism; Liver - pathology; Malondialdehyde - metabolism; Mice; Mice, Inbred ICR; Oxidative Stress - drug effects; Solubility; Solutions; Superoxide Dismutase - metabolism; Water - chemistry
• ISSN: 0927-7765; 1873-4367
• DOI: 10.1016/j.colsurfb.2019.04.020

[Display omitted] •A FA-HP-β-CD complex was prepared and characterized.•Hep3B cellular uptake of FA-HP-β-CD complex was higher than that of FA.•FA-HP-β-CD complex had a higher Hep3B cytotoxicity than of FA.•FA-HP-β-CD complex showed more protective effect from liver damage than FA. 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.