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Influence of different 99mTc cores on the physicochemical and biodistribution behaviours of 99mTc-labelled complexes of pamidronate dithiocarbamate

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Abstract

This study sought to evaluate the impact of 99mTcO and 99mTc≡N cores on the physicochemical and biodistribution properties of 99mTc-labelled complexes of pamidronate dithiocarbamate. We successfully converted the commercially available pamidronate to pamidronate dithiocarbamate (PAMDTC) and its 99mTc-labelled complexes were prepared with high radiochemical yield (97.95 ± 0.59% and 97.66 ± 1.53% for 99mTcN-PAMDTC and 99mTcO-PAMDTC, respectively). Both complexes were stable in vitro. The partition coefficient results showed that both of them were hydrophilic and 99mTcN-PAMDTC exhibited more hydrophilic than 99mTcO-PAMDTC. The binding rate of 99mTcN-PAMDTC to human serum albumin was lower than that of 99mTcO-PAMDTC. 99mTcN-PAMDTC performed better affinity to hydroxyapatite than 99mTcO-PAMDTC. From the biodistribution study results, 99mTcN-PAMDTC showed higher bone uptake and ratios of bone/blood and bone/muscle at 4 h post-injection. Further, single photon emission computed tomography (SPECT) imaging study of 99mTcN-PAMDTC showed that there was a clear accumulation in bone, suggesting it would be a potential novel bone imaging agent. It was concluded that different 99mTc cores had an important impact on the physicochemical and biological properties of 99mTc-labelled complexes of pamidronate dithiocarbamate.

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Acknowledgements

The work was financially supported, in part, by National Natural Science Foundation of China (21771023).

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Authors and Affiliations

  1. Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, 100875, China

    Xiaoqing Song, Yue Wang & Junbo Zhang

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  1. Xiaoqing Song
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  2. Yue Wang
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  3. Junbo Zhang
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Correspondence to Junbo Zhang.

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Xiaoqing Song and Yue Wang are joint first authors.

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Song, X., Wang, Y. & Zhang, J. Influence of different 99mTc cores on the physicochemical and biodistribution behaviours of 99mTc-labelled complexes of pamidronate dithiocarbamate. J Radioanal Nucl Chem 316, 313–319 (2018). https://doi.org/10.1007/s10967-018-5727-2

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  • DOI: https://doi.org/10.1007/s10967-018-5727-2

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