Synthesis and characterisation of chitosan-encapsulated genistein: its anti-proliferative and anti-angiogenic activities

J Microencapsul. 2020 Jun;37(4):305-313. doi: 10.1080/02652048.2020.1740804. Epub 2020 Mar 20.

Abstract

Aims: The study was carried out to synthesise and characterise the chitosan-encapsulated genistein (CHI-En/Gen) and determine its anti-cancer and anti-angiogenic properties.Methods: The cytotoxic and anti-angiogenic activity of CHI-En/Gen was performed using MTT and chorioallantoic membrane assay. The molecular action was determined using flow cytometry and gene expression.Results: The synthesised CHI-En/Gen was in submicron size, spherical in shape and with entrapment efficiency and loading efficiency of 76.8% (w/w) and 32.6% (w/w), respectively. The CHI-En/Gen notably inhibited the growth and proliferation of human colorectal cancer cells (HT-29) while did not affect the viability of human dermal fibroblast as normal cell. The flow cytometry and the caspase-3 gene expression analyses revealed the apoptotic cells death in the HT-29 cells. Moreover, the encapsulated genistein showed anti-angiogenic activity.Conclusion: The CHI-En/Gen appeared as a promising carrier for the colon delivery of genistein to be used in complementary health approaches for the cancer prevention.

Keywords: Encapsulation; chitosan; colorectal cancer cells; delivery; genistein.

MeSH terms

  • Angiogenesis Inhibitors / administration & dosage*
  • Angiogenesis Inhibitors / chemistry
  • Angiogenesis Inhibitors / pharmacology*
  • Animals
  • Anticarcinogenic Agents / administration & dosage*
  • Anticarcinogenic Agents / chemistry
  • Anticarcinogenic Agents / pharmacology*
  • Caspase 3 / drug effects
  • Cell Proliferation / drug effects
  • Chick Embryo
  • Chitosan
  • Chorioallantoic Membrane / drug effects
  • Drug Carriers
  • Drug Delivery Systems
  • Flow Cytometry
  • Gene Expression Regulation, Neoplastic / drug effects
  • Genistein / administration & dosage*
  • Genistein / chemistry
  • Genistein / pharmacology*
  • HT29 Cells
  • Humans
  • Particle Size

Substances

  • Angiogenesis Inhibitors
  • Anticarcinogenic Agents
  • Drug Carriers
  • Chitosan
  • Genistein
  • CASP3 protein, human
  • Caspase 3