Canagliflozin-loaded magnetic nanoparticles as potential treatment of hypoxic tumors in combination with radiotherapy

Nanomedicine (Lond). 2018 Oct;13(19):2435-2454. doi: 10.2217/nnm-2018-0145. Epub 2018 Oct 12.

Abstract

Aim: To synthesize magnetic nanoparticles loaded with the SGLT2-inhibitor canagliflozin (CANA) and evaluate its anticancer potential under normoxic and hypoxic conditions in combination or not with radiotherapy.

Material & methods: Iron oxide nanoparticles were synthesized via an alkaline hydrolytic precipitation of iron precursor in the presence of poly(methacrylic acid)-graft-poly(ethyleneglycol methacrylate). CANA was conjugated to the nanoparticles using N-ethyl-N'-(3-dimethyl aminopropyl) carbodiimide (EDC)/N-hydroxysuccinimide chemistry. The anticancer efficacy of the nanoparticles was evaluated in cancer cell lines and in a mouse PDV C57 tumor model.

Results: In the mouse xenograft cancer model, the combination of CANA-loaded nanoparticles with radiotherapy (in the presence of an external magnetic field at the tumor site) exhibited higher antitumor activity compared with the combination of free CANA with radiotherapy.

Conclusion: The results obtained indicate the potential that the combination of selective delivery of a SGLT2 inhibitor such as CANA with radiotherapy holds as an anticancer treatment.

Keywords: canagliflozin; hypoxia; magnetic nanoparticles.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Canagliflozin / chemistry
  • Canagliflozin / pharmacology*
  • Combined Modality Therapy
  • Ferric Compounds / chemistry
  • Humans
  • Magnetite Nanoparticles / administration & dosage
  • Magnetite Nanoparticles / chemistry
  • Mice
  • Neoplasms / drug therapy*
  • Neoplasms / genetics
  • Neoplasms / radiotherapy
  • Sodium-Glucose Transporter 2 / drug effects
  • Sodium-Glucose Transporter 2 Inhibitors / chemistry
  • Sodium-Glucose Transporter 2 Inhibitors / pharmacology*
  • Tumor Hypoxia / drug effects*
  • Xenograft Model Antitumor Assays

Substances

  • Ferric Compounds
  • Magnetite Nanoparticles
  • SLC5A2 protein, human
  • Sodium-Glucose Transporter 2
  • Sodium-Glucose Transporter 2 Inhibitors
  • Canagliflozin
  • ferric oxide