Non-Covalent Loading of Anti-Cancer Doxorubicin by Modularizable Peptide Self-Assemblies for a Nanoscale Drug Carrier

Molecules. 2017 Nov 6;22(11):1916. doi: 10.3390/molecules22111916.

Abstract

We prepared nanoscale, modularizable, self-assembled peptide nanoarchitectures with diameters less of than 20 nm by combining β-sheet-forming peptides tethering a cell-penetrating peptide or a nuclear localization signal sequence. We also found that doxorubicin (Dox), an anti-cancer drug, was non-covalently accommodated by the assemblies at a ratio of one Dox molecule per ten peptides. The Dox-loaded peptide assemblies facilitated cellular uptake and subsequent nuclear localization in HeLa cells, and induced cell death even at low Dox concentrations. This peptide nanocarrier motif is a promising platform for a biocompatible drug delivery system by altering the targeting head groups of the carrier peptides.

Keywords: anti-cancer doxorubicin; cell-penetrating peptide; drug delivery system; nuclear-localization signal; peptide self-assembly.

MeSH terms

  • Antibiotics, Antineoplastic / chemistry
  • Antibiotics, Antineoplastic / pharmacology*
  • Cell Survival / drug effects
  • Cell-Penetrating Peptides / chemistry*
  • Cell-Penetrating Peptides / pharmacology
  • Doxorubicin / chemistry
  • Doxorubicin / pharmacology*
  • Drug Delivery Systems
  • HeLa Cells
  • Humans
  • Nanoparticles / chemistry
  • Nuclear Localization Signals / chemistry*
  • Particle Size

Substances

  • Antibiotics, Antineoplastic
  • Cell-Penetrating Peptides
  • Nuclear Localization Signals
  • Doxorubicin