Graphene quantum dot formulation for cancer imaging and redox-based drug delivery

Nanomedicine. 2021 Oct:37:102408. doi: 10.1016/j.nano.2021.102408. Epub 2021 May 17.

Abstract

This work develops a new multifunctional biocompatible anticancer nanoformulation to provide targeted image-guided cancer-selective therapeutics. It consists of three active covalently bound components: (1) biocompatible nitrogen-doped graphene quantum dots (GQDs) as a multifunctional delivery and imaging platform, (2) hyaluronic acid (HA) unit targeted to the CD44 receptors on a variety of cancer cells, and (3) oxidative stress-based cancer-selective ferrocene (Fc) therapeutic. The biocompatible GQD platform synthesized from glucosamine exhibits high-yield intrinsic fluorescence. It is utilized for tracking Fc-GQD-HA formulation in vitro indicating internalization enhancement in HeLa cells targeted by the HA over non-cancer HEK-293 cells not overexpressing CD44 receptor. Fc-GQD-HA, non-toxic at 1 mg/mL to HEK-293 cells, induces cytotoxic response in HeLa enhanced over time, while therapeutic ROS generation by Fc-GQD-HA is ~3 times greater than that of Fc alone. This outlines the targeted delivery, imaging, and cancer-specific treatment capabilities of the new Fc-GQD-HA formulation enabling desired cancer-focused nanotherapeutic approach.

Keywords: Cancer therapy; Graphene quantum dots; Imaging; Redox-based drug delivery; Targeting.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Biocompatible Materials / chemistry
  • Biocompatible Materials / pharmacology
  • Doxorubicin / chemistry
  • Doxorubicin / pharmacology
  • Drug Delivery Systems*
  • Graphite / chemistry
  • Graphite / pharmacology*
  • HEK293 Cells
  • HeLa Cells
  • Humans
  • Hyaluronan Receptors / antagonists & inhibitors
  • Hyaluronan Receptors / genetics
  • Hyaluronic Acid / chemistry
  • Hyaluronic Acid / pharmacology
  • Neoplasms / diagnostic imaging*
  • Neoplasms / drug therapy*
  • Neoplasms / genetics
  • Neoplasms / pathology
  • Optical Imaging
  • Oxidation-Reduction / drug effects
  • Quantum Dots / chemistry

Substances

  • Antineoplastic Agents
  • Biocompatible Materials
  • CD44 protein, human
  • Hyaluronan Receptors
  • Graphite
  • Doxorubicin
  • Hyaluronic Acid