Enhancement of the permeability and activities of epigallocatechin gallate by quaternary ammonium chitosan/fucoidan nanoparticles

Carbohydr Polym. 2020 Aug 15:242:116312. doi: 10.1016/j.carbpol.2020.116312. Epub 2020 May 15.

Abstract

Epigallocatechin gallate (EGCG) has many biological functions; however, the use of EGCG in biomedical and food industries was limited due to its poor oral absorption and high susceptibility to degradation. In this study, a mucoadhesive quaternary chitosan was synthesized and combined with fucoidan (FD) (or depolymerized lower molecular weight fucoidan, LMWF) to prepare EGCG-loaded nanoparticles, which extended EGCG release over 300 min and enhanced the transepithelial permeation of EGCG using Caco-2 cells as a model for intestinal absorption. The nanoparticls protected EGCG against degradation in phosphate buffer (pH 6.8) and the remaining EGCG was 1.7-folds higher than the control (EGCG alone). The additive effects of EGCG combined with FD or LMWF in the nanoparticles increased the DPPH radical scavenging activity and the enzyme inhibitory activity against α-amylase (2.82-4.92 fold increase) and α-glucosidase (1.35-1.67 fold increase), while quaternary chitosan helped to enhance the antibacterial effect of EGCG.

Keywords: Antibacterial; Antioxidat; Drug delivery; EGCG; Enzyme inhibitory; Fucoidan; Hypoglycemic; Nanoparticles; Oral absorption; Quaternary chitosan.

MeSH terms

  • Catechin / analogs & derivatives*
  • Catechin / chemistry
  • Catechin / pharmacology
  • Chitosan / chemical synthesis
  • Chitosan / chemistry*
  • Chitosan / pharmacology
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology
  • Fucus / chemistry
  • Nanoparticles / chemistry*
  • Particle Size
  • Polysaccharides / chemistry*
  • Polysaccharides / pharmacology
  • Quaternary Ammonium Compounds / chemistry*
  • Quaternary Ammonium Compounds / pharmacology
  • Surface Properties
  • alpha-Amylases / antagonists & inhibitors
  • alpha-Amylases / metabolism
  • alpha-Glucosidases / metabolism

Substances

  • Enzyme Inhibitors
  • Polysaccharides
  • Quaternary Ammonium Compounds
  • Catechin
  • Chitosan
  • fucoidan
  • epigallocatechin gallate
  • alpha-Amylases
  • alpha-Glucosidases