Complexation of hydroxytyrosol and 3,4-dihydroxyphenylglycol with pectin and their potential use for colon targeting

Carbohydr Polym. 2017 May 1:163:292-300. doi: 10.1016/j.carbpol.2017.01.027. Epub 2017 Jan 6.

Abstract

Hydroxytyrosol (HT) and 3,4-dihydroxyphenylglycol (DHPG) are two phenolic antioxidants naturally found in olive fruit with anti-inflammatory properties. This study explored the interaction of pectin with HT and DHPG via their encapsulation into pectinate beads. Purification by size exclusion chromatography, changes in the fluorescence spectrum of the HT and pectin, and MALDI TOF-TOF analysis suggested the existence of the phenol-pectin complexes. The entrapment efficiency, swelling properties, and in vitro release of HT and DHPG of the beads were studied. The results show that the beads can entrap the water soluble compounds HT and DHPG in sufficient amounts to reach the colon. The beads consisted of an important amount of pectin-bound HT or DHPG after two hours at gastric pH. This study highlights the potential use of HT-and DHPG-loaded pectinate gel beads for the colon-targeted delivery of these bioactive compounds to help prevent or relieve chronic inflammatory bowel disease.

Keywords: 3,4-Dihydroxyphenylglycol; Calcium pectin/alginate beads; Hydroxytyrosol; In vitro release; Phenol-pectin complex; virgin olive oil.

MeSH terms

  • Colon
  • Drug Delivery Systems*
  • Drug Liberation
  • Methoxyhydroxyphenylglycol / analogs & derivatives*
  • Methoxyhydroxyphenylglycol / chemistry
  • Olea / chemistry
  • Pectins / chemistry*
  • Phenylethyl Alcohol / analogs & derivatives*
  • Phenylethyl Alcohol / chemistry

Substances

  • 3,4-dihydroxyphenylethanol
  • Methoxyhydroxyphenylglycol
  • Pectins
  • Phenylethyl Alcohol
  • 3,4-dihydroxyphenylglycol