Enzyme structure and function protection from gastrointestinal degradation using enteric coatings

Int J Biol Macromol. 2018 Nov:119:413-422. doi: 10.1016/j.ijbiomac.2018.07.143. Epub 2018 Jul 23.

Abstract

Bovine Serum Albumin (BSA) and Horseradish Peroxidase (HRP) have been encapsulated within microparticulated matrices composed of Eudragit RS100 by the water-in-oil-in-water double emulsion solvent evaporation method. Good encapsulation efficiencies were achieved for BSA and HRP, 88.4 and 95.8%, respectively. The stability of the loaded proteins was confirmed by using circular dichroism and fluorescence. The gastroresistance of the protein-loaded microparticles was evaluated under simulated gastric conditions demonstrating the preservation of the structural integrity of the proteins loaded inside the particles. The enzymatic activity of HRP after being released from the enteric microparticles was evaluated by using the peroxidase substrate, revealing that the released enzyme preserved its 100% function. The high drug loadings achieved, reduced cytotoxicity and efficient gastric protection point out towards the potential use of those carriers as oral delivery vectors of therapeutic proteins offering a more controlled targeted release in specific sites of the intestine and an enhanced gastrointestinal absorption.

Keywords: Enteric microparticles; Eudragit; Protein encapsulation; Protein stability; Sustained release.

MeSH terms

  • Acrylic Resins / chemistry
  • Biocatalysis
  • Caco-2 Cells
  • Drug Compounding / methods*
  • Gastrointestinal Tract / metabolism*
  • Horseradish Peroxidase / chemistry
  • Horseradish Peroxidase / metabolism*
  • Humans
  • Microspheres
  • Polymethacrylic Acids / chemistry
  • Serum Albumin, Bovine / metabolism
  • Solubility

Substances

  • Acrylic Resins
  • Polymethacrylic Acids
  • polymethacrylic acid
  • Serum Albumin, Bovine
  • Eudragit RS
  • Horseradish Peroxidase