4.7 Article

Synthesis and characterization of novel 99mTc-DGC nano-complexes for improvement of heart diagnostic

Journal

BIOORGANIC CHEMISTRY
Volume 96, Issue -, Pages -

Publisher

ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2020.103572

Keywords

Biodegradable; Biocompatible; Dendrimer; Glucosamine; Chelator free; Radiolabeling

Funding

  1. Tehran University of Medical Sciences

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In this research, early diagnosis of cardiovascular diseases can reduce their mortality and burden. In our study, we developed a new nano-agent, Tc-99m-Dendrimer Glyco Conjugate (Tc-99m-DGC), and assessed its safety and capability for myocardial viability scan. To develop Tc-99m-DGC, we first synthesized the dendrimer and then, glucose has been conjugated. Afterwards, we measured toxicity of the product on normal cells by XTT and apoptosis/necrosis methods. We compared the myocardial viability scan (measured by SPECT and dynamic planar imaging) in two rabbit models, with and without infarction. We also assessed the biodistribution of Tc-99m-DGC in rats with no infarction. DGC synthesis was confirmed by Fourier transform infrared (FT-IR), proton nuclear magnetic resonance (H-1 NMR), liquid chromatography-mass spectrometry (LC-MS), dynamic light scattering (DLS) and static light scattering techniques (SLS). Then radiochemical purity (RCP) was done to present the stability and potential of DGC to complex formation with Tc-99m. In vitro cytotoxicity showed nontoxic concentration up to 8 mg/mL. Single Photon Emission Computed Tomography (SPECT) and dynamic planar imaging clearly showed the accumulation of Tc-99m-DGC in myocardial. Biodistribution result showed the 2.60% accumulation of Tc-99m-DGC in myocardial after 2 h. Our findings indicated Tc-99m-DGC to be safe and can accurately diagnose myocardial infarctions at early stages. Human studies to further assess such effects are critical.

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