Exploration of RGD peptide-modified targeted delivery of doxorubicin using chitosan oligosaccharide-coated GQD

Tseng-Yu Yeh1, Jung-Hua Lin1, Yi-Jhen Jiang2

  • 1Department of Science Education, National Taipei University of Education, No.134, Sec. 2, Heping E. Rd., Da-an District, Taipei City 106, Taiwan.

Insights

This study explores graphene quantum dot (GQD) carriers for delivering RGD-modified doxorubicin (RGD-DOX) in cancer therapy. These novel drug delivery systems show high tumor targeting efficiency and reduced side effects.

Area of Science:

  • Biomedical Engineering
  • Nanotechnology
  • Oncology

Background:

  • Cancer therapy faces challenges with tumor targeting and systemic toxicity.
  • Pre-modified drugs with targeting ligands, like RGD-4C peptide, offer a potential solution.
  • RGD-modified doxorubicin (RGD-DOX) presents unique interactions with delivery systems and cancer cells.

Purpose of the Study:

  • To investigate two distinct graphene quantum dot (GQD)-based carriers for delivering RGD-DOX.
  • To evaluate the efficacy and safety of these novel drug delivery systems in cancer treatment.

Main Methods:

  • Two GQD carriers were developed: PEGylated GQDs with gold nanoparticles (APG) and chitosan oligosaccharide-coated GQD (CG).
  • Both carriers encapsulated RGD-DOX and demonstrated pH-responsive release in acidic tumor environments.
  • In vitro and in vivo studies assessed cellular apoptosis, tumor suppression, and systemic toxicity.

Main Results:

  • Both APG and CG carriers effectively delivered RGD-DOX, inducing significant cellular apoptosis via DNA damage and apoptotic markers.
  • In vivo experiments showed effective tumor suppression with reduced RGD-DOX dosage, indicating minimized systemic toxicity.
  • The RGD-pre-modified DOX delivered by GQD systems demonstrated high targeting efficiency.

Conclusions:

  • GQD-based drug delivery systems are validated as a novel strategy for RGD-pre-modified doxorubicin.
  • These systems offer high targeting efficiency and reduced potential side effects in cancer therapy.
  • The study presents a promising approach for designing advanced drug delivery systems.