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Radiosynthesis, radiochemical, and biological characterization of 177 Lu‐labeled diethylenetriamine penta‐acetic acid
Author(s) -
Akbar Muhammad U.,
Bokhari Tanveer H.,
Ahmad Muhammad R.,
Zia Khalid M.,
Roohi Samina,
Ayub Nimra,
Sohaib Muhammad
Publication year - 2019
Publication title -
journal of cellular biochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.028
H-Index - 165
eISSN - 1097-4644
pISSN - 0730-2312
DOI - 10.1002/jcb.28712
Subject(s) - diethylenetriamine , radiosynthesis , biodistribution , chemistry , radiochemistry , yield (engineering) , acetic acid , chromatography , paper chromatography , thin layer chromatography , nuclear medicine , in vitro , medicine , materials science , biochemistry , positron emission tomography , organic chemistry , metallurgy
Diethylenetriamine penta‐acetic acid (DTPA), when complexed with a gamma (γ)‐emitter radioisotope like 99m 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 177 Lu‐labeled radiopharmaceutical with high radiochemical yield, which can be used for diagnostic purposes and therapeutic purposes also. The single and well‐defined 177 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 177 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 177 Lu at specific conditions (pH 7.0, 15 minutes reaction time at 100 °C). 177 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 177 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 177 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.