Cetuximab-conjugated chitosan-pectinate (modified) composite nanoparticles for targeting colon cancer

Int J Pharm. 2019 Dec 15:572:118775. doi: 10.1016/j.ijpharm.2019.118775. Epub 2019 Oct 31.

Abstract

In the present study, we successfully developed a cetuximab-conjugated modified citrus pectin-chitosan nanoparticles for targeted delivery of curcumin (Cet-MCPCNPs) for the treatment of colorectal cancer. In vitro analyses revealed that nanoparticles were spherical with size of 249.33 ± 5.15 nm, a decent encapsulation efficiency (68.43 ± 2.4%) and a 'smart' drug release profile. 61.37 ± 0.70% of cetuximab was adsorbed to the surface of the nanoparticles. Cellular uptake studies displayed enhanced internalization of Cet-MCPCNPs in Caco-2 (EGFR +ve) cells, which ultimately resulted in a significant reduction in cancer cell propagation. The cell cycle analysis indicated that Cet- MCPCNPs induced cell death in enhanced percentage of Caco-2 cells by undergoing cell cycle arrest in the G2/M phase. These data suggest that Cet-MCPCNPs represent a new and promising targeting approach for the treatment of colorectal cancer.

Keywords: Cetuximab; Chitosan; Colorectal cancer; Curcumin; Modified citrus pectin; Targeted delivery.

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Caco-2 Cells
  • Cell Cycle Checkpoints / drug effects
  • Cell Line, Tumor
  • Cetuximab / chemistry*
  • Cetuximab / pharmacology*
  • Chitosan / chemistry*
  • Colonic Neoplasms / drug therapy*
  • Curcumin / chemistry
  • Curcumin / pharmacology
  • Drug Delivery Systems / methods
  • Drug Liberation / physiology
  • G2 Phase Cell Cycle Checkpoints / drug effects
  • HCT116 Cells
  • Humans
  • Nanoparticles / chemistry*
  • Pectins / chemistry*

Substances

  • Antineoplastic Agents
  • citrus pectin
  • Pectins
  • Chitosan
  • Curcumin
  • Cetuximab