Characterization and in vitro anticancer properties of chitosan-microencapsulated flavan-3-ols-rich grape seed extracts

Int J Biol Macromol. 2017 Nov;104(Pt A):1039-1045. doi: 10.1016/j.ijbiomac.2017.07.022. Epub 2017 Jul 4.

Abstract

Studies have fully demonstrated that a diet rich in fruit and vegetables may reduce the incidence of tumors. In particular, Grape Seed Extract (GSE) has been shown to carry on chemopreventive and antitumor activity thanks to the numerous beneficial substances it contains. The purpose of this work was to create a biocompatible matrix containing GSE in order to obtain microparticles able to modulate its biopharmaceutical parameters. The spray-drying technique was chosen in order to realize chitosan microparticles characterized by a mean diameter of 4-10μm and a positive surface charge that decreased after GSE encapsulation. The evaluation of the pharmacological activity of the GSE and these GSE-loaded chitosan microparticles on different cancer cells together with CLSM investigation evidenced an increase in the antitumor effect promoted by the polysaccharide as a consequence of the enhanced cell interaction. Therefore GSE-loaded chitosan microparticles may be an innovative drug delivery system useful for the treatment of certain cancer-related diseases.

Keywords: Cancer; Chitosan microparticles; Grape seed extract; Mucin.

MeSH terms

  • A549 Cells
  • Adhesiveness
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Caco-2 Cells
  • Chitosan / chemistry*
  • Drug Compounding
  • Flavonoids / chemistry*
  • Grape Seed Extract / chemistry*
  • Grape Seed Extract / pharmacology*
  • Humans
  • Mucous Membrane / chemistry

Substances

  • Antineoplastic Agents
  • Flavonoids
  • Grape Seed Extract
  • flavan-3-ol
  • Chitosan