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Indium-111 labeled bleomycin for targeting diagnosis and therapy of liver tumor: optimized preparation, biodistribution and SPECT imaging with xenograft models

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Abstract

In this work, the preparation of 111In radiolabeled bleomycin (111In-BLM) was optimized systematically and used for SPECT imaging of liver cancer xenograft models. 111In-BLM with a high radiochemical yield (> 99%) could be obtained at pH 0.5–1 at a mixture ratio of 9:1 (111In/BLM, mCi/mg). The radiochemical purity of 111In-BLM retained > 99% in either buffers or serum for 3 days. Biodistribution of 111In-BLM revealed its excellent stability in vivo. The SPECT imaging studies showed 111In-BLM has great specificity to liver tumor xenograft. All the results implied 111In-BLM is a potential radiopharmaceutical for targeting diagnosis and therapy of liver tumor.

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Acknowledgements

This Study was supported by Key Research Development Project of Sichuan Provincial Department of Science and Technology (2018SZ0022), Strategic Cooperation Project of Luzhou Municipal People’s Government of Sichuan University (2018CDLZ-09) and the Open Project Program of Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province. We would like to thank the cyclotron operation crew Xiaodong Liao of Sichuan University for his help in performing irradiations. Besides, the authors thank Guangfu Liu and Chi Qi from the Affiliated Hospital of Southwest Medical University for their expert knowledge and technical advice for SPECT imaging.

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Correspondence to Mingshuang Wang or Yuanyou Yang.

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Tang, Y., Liu, W., Li, F. et al. Indium-111 labeled bleomycin for targeting diagnosis and therapy of liver tumor: optimized preparation, biodistribution and SPECT imaging with xenograft models. J Radioanal Nucl Chem 322, 545–551 (2019). https://doi.org/10.1007/s10967-019-06801-5

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