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

• Published in: IET nanobiotechnology 2020-09, Vol.14 (7), p.628-634
• Main Authors: Zamani, Saedeh, Shafeie‐Ardestani, Mehdi, Bitarafan‐Rajabi, Ahmad, Khalaj, Ali, Sabzevari, Omid
• Format: Article
• Language: English
• Subjects: 2,3‐bis‐(2‐methoxy‐4‐nitro‐5‐sulfophenyl)‐2H‐tetrazolium‐5‐carboxanilide cytotoxicity assay; Animals; biochemistry; Biocompatible Materials - chemistry; biodistribution; biological organs; biomedical materials; Body Weight; bone; breast cancer molecular imaging agent; Breast Neoplasms - drug therapy; bright SPECT image; cancer; cellular biophysics; cellular toxicity; Chromatography, Liquid; Citric Acid - chemistry; Contrast Media; Dendrimers - chemical synthesis; dendrimer‐based imaging agent; dendrimer‐G3; dynamic light scattering; electrospinning; Female; Folic Acid - chemistry; folic acid‐conjugated G‐399m Tc‐dendrimer; Fourier transform infrared spectra; HEK293 Cells; human serum; Humans; Light; light scattering; Magnetic Resonance Spectroscopy; Mass Spectrometry; Materials Testing; Mice; Mice, Nude; Microscopy, Electron, Transmission; Molecular Imaging - methods; PEG‐citrate dendrimer; poly(ethylene glycol)‐citrate; Polyethylene Glycols - chemistry; polymers; proton magnetic resonance; proton nuclear magnetic resonance; Radionuclide Imaging; Radiopharmaceuticals - chemical synthesis; Scattering, Radiation; single photon emission computed tomography; Spectroscopy, Fourier Transform Infrared; technetium; Technetium - chemistry; Tissue Distribution; toxicity assessment; toxicology; transition electron microscopy; transmission electron microscopy; tumour detection; tumours
• ISSN: 1751-875X; 1751-8741; 1751-875X
• DOI: 10.1049/iet-nbt.2020.0176

Hence, in this study, the authors aimed to develop a dendrimer‐based imaging agent comprised of poly(ethylene glycol) (PEG)‐citrate, technetium‐99 m (99m Tc), 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.