Synthesis, radiolabelling, and biological assessment of folic acid-conjugated G-3 99mTc-dendrimer as the breast cancer molecular imaging agent

IET Nanobiotechnol. 2020 Sep;14(7):628-634. doi: 10.1049/iet-nbt.2020.0176.

Abstract

Hence, in this study, the authors aimed to develop a dendrimer-based imaging agent comprised of poly(ethylene glycol) (PEG)-citrate, technetium-99 m (99mTc), and folic acid. The dendrimer-G3 was synthesised and conjugated with folic acid, which confirmed by Fourier transform infrared, proton nuclear magnetic resonance, dynamic light scattering, and transition electron microscopy. 2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-Tetrazolium-5-Carboxanilide cytotoxicity assay kit was used to measure the cellular toxicity of dendrimer. Imaging and biodistribution studies were conducted on the mice bearing tumour. The results showed that the fabricated dendrimer-G3 has a size of 90 ± 3 nm, which was increased to 100 ± 4 nm following the conjugation with folic acid. The radiostablity investigation showed that the fabricated dendrimers were stable in the human serum at various times. Toxicity assessment confirmed no cellular toxicity against HEK-293 cells at 0.25, 0.5, 1, 2, 4, and 8 mg/μl concentrations. The in vivo studies demonstrated that the synthesised dendrimers were able to provide a bright SPECT image applicable for tumour detection. In conclusion, the authors' study documented the positive aspects of PEG-citrate dendrimer conjugated with folic acid as the SPECT contrast agent for breast cancer detection.

MeSH terms

  • Animals
  • Biocompatible Materials / chemistry
  • Body Weight
  • Breast Neoplasms / drug therapy*
  • Chromatography, Liquid
  • Citric Acid / chemistry
  • Contrast Media
  • Dendrimers / chemical synthesis
  • Female
  • Folic Acid / chemistry*
  • HEK293 Cells
  • Humans
  • Light
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Materials Testing
  • Mice
  • Mice, Nude
  • Microscopy, Electron, Transmission
  • Molecular Imaging / methods
  • Polyethylene Glycols / chemistry
  • Radionuclide Imaging
  • Radiopharmaceuticals / chemical synthesis
  • Scattering, Radiation
  • Spectroscopy, Fourier Transform Infrared
  • Technetium / chemistry*
  • Tissue Distribution

Substances

  • Biocompatible Materials
  • Contrast Media
  • Dendrimers
  • Radiopharmaceuticals
  • Citric Acid
  • Polyethylene Glycols
  • Technetium
  • Folic Acid