Radiosynthesis, radiochemical, and biological characterization of Lu-labeled diethylenetriamine penta-acetic acid.

J Cell Biochem 2019 Apr 17. Epub 2019 Apr 17.

Department of Medical Sciences, Pakistan Institute of Engineering and Applied Sciences, Islamabad, Pakistan.

Diethylenetriamine penta-acetic acid (DTPA), when complexed with a gamma (γ)-emitter radioisotope like Tc, is used for renal function diagnosis and many other diagnostic applications. The main aim of this study was to develop a novel and versatile single-step methodology for the synthesis of a new Lu-labeled radiopharmaceutical with high radiochemical yield, which can be used for diagnostic purposes and therapeutic purposes also. The single and well-defined Lu-DTPA complex was radiochemically characterized by paper chromatography, thin-layer chromatography, high-performance liquid chromatography, and electrophoresis techniques. Dependence of the labeling yield of Lu-DTPA complex on different factors was studied in detail. Biological evaluation was also performed in a normal rabbit by developing images under a γ camera at various time intervals. More than 99% labeling yield was obtained by reacting DTPA with Lu at specific conditions (pH 7.0, 15 minutes reaction time at 100 °C). Lu-DTPA complex showed high stability both at room temperature and in vitro. Biodistribution studies in normal mice indicated the fractional renal uptake of intravenously administered Lu-DTPA complex, which reached in the kidneys within 2-3 minutes. Scintigraphy showed rapid clearance from the body. Based on these results, we propose that Lu-DTPA complex might be used as an ideal candidate for functional evaluation of kidneys and the urinary tract, especially when needed to be transported to long-range consumer sites, because of its suitable half-life.

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https://onlinelibrary.wiley.com/doi/abs/10.1002/jcb.28712
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http://dx.doi.org/10.1002/jcb.28712DOI Listing
April 2019
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