99mTc radiolabeling of polyethylenimine capped carbon dots for tumor targeting: synthesis, characterization and biodistribution

Int J Radiat Biol. 2021;97(7):977-985. doi: 10.1080/09553002.2021.1919781. Epub 2021 May 5.

Abstract

Purpose: Due to the favorable physicochemical properties and the biocompatibility, carbon dots (CDs) have gained a great attention as a tumor targeting agent. This study investigates polyethylenimine capped CDs (PEI capped CDs) as a prospective nanocarrier of technetium-99m (99mTc) for tumor targeting. Technetium-labeled CDs could be introduced as a promising candidate for single photon emission tomography (SPECT) imaging.

Materials and methods: Polyethylenimine capped CDs were prepared by hydrothermal method using hyperbranched PEI and citric acid. For a purpose of comparison, citrate capped CDs were also prepared by microwave irradiation. Both types of CDs were characterized and radiolabeled with 99mTc using sodium borohydride (NaBH4) as a reducing agent. Biodistribution and tumor targeting efficiency of the produced radiolabeled CDs have been studied in Earlich ascites tumor mice model.

Results: Citrate capped CDs and PEI capped CDs have been synthesized successfully and characterized. High radiochemical yield of 99mTc-citrate capped CDs 99mTc-PEI capped CDs was obtained (97 ± 0.7 and 90 ± 0.2, respectively). Biodistribution studies of 99mTc-labeled PEI capped CDs have shown a potential tumor uptake (10 ± 0.5% Radioactivity/gram tumor) with high target to non-target ratio (T/NT) around 7 at 1-h post injection. 99mTc-citrate capped CDs have achieved a lower tumor uptake level (3.8 ± 0.3% Radioactivity/gram tumor 1 h post injection).

Conclusion: This study introduces PEI capped CDs as a promising nanocarrier of 99mTc for efficient tumor targeting. Technetium-labeled PEI capped CDs could be utilized as a potential SPECT tumor imaging agent.

Keywords: Carbon dots; Polyethylenimine; Technetium-99m; Tumor.

MeSH terms

  • Animals
  • Carbon / chemistry*
  • Cell Line, Tumor
  • Chemistry Techniques, Synthetic
  • Humans
  • Isotope Labeling
  • Mice
  • Nanoparticles / chemistry*
  • Polyethyleneimine / chemical synthesis
  • Polyethyleneimine / chemistry*
  • Polyethyleneimine / pharmacokinetics*
  • Radiochemistry
  • Technetium / chemistry*
  • Tissue Distribution
  • Tomography, Emission-Computed, Single-Photon

Substances

  • Technetium
  • Carbon
  • Polyethyleneimine