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Radiolanthanide-labeled HA particles in the treatment of rheumatoid arthritis: ready-to-use cold kits for rapid formulation in hospital radiopharmacy

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Abstract

Hydroxyapatite (HA) [Ca10(PO4)6(OH)2] particles radiolabeled with a variety of β− emitting lanthanide radionuclides and also pseudolanthanide 90Y have been proposed for the treatment of arthritis. A ready-to-use cold kit of HA particles (1–10 µm size) was developed for fast and convenient formulation of radiolanthanide-labeled HA particles at hospital radiopharmacy. Six radionuclides namely, 169Er, 177Lu, 153Sm, 166Ho, 142Pr and 90Y, having β− emissions of a wide range of energy [Eβ(max) = 0.34–2.28 MeV] were identified and produced by thermal neutron activation. Clinical doses of HA particles labeled with these radionuclides were prepared in high yield (>97 %) and radiochemical purity (>99 %) using the cold kits. Pre-clinical studies of 177Lu–HA carried out in Wistar rats bearing arthritis in knee joints revealed no leakage of the activity from the joints. In preliminary clinical investigation using 333 ± 46 MBq doses of the same preparation, significant improvement in the disease conditions was reported in patients with chronic rheumatoid arthritis of knee joints.

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Acknowledgments

Research at the Bhabha Atomic Research Centre is part of the ongoing activities of the Department of Atomic Energy, India and fully supported by government funding. The authors are grateful to Dr. Gursharan Singh, Head, Isotope Application and Radiopharmaceuticals Division, Bhabha Atomic Research Centre, for his support and encouragement. The authors are also thankful to the staff members of Irradiation Co-ordination Group of Isotope Application and Radiopharmaceuticals Division for their help.

Conflict of interest

The authors declare that they have no conflict of interests, financial, scientific or otherwise with other people or organizations in the publication of this article.

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Authors and Affiliations

  1. Isotope Application and Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Trombay, Mumbai, 400 085, India

    Sudipta Chakraborty, K. V. Vimalnath, A. Rajeswari & Ashutosh Dash

  2. Experimental Animal Facility and Radioisotope Laboratory, Radiation Biology and Health Sciences Division, Bhabha Atomic Research Centre, Trombay, Mumbai, 400 085, India

    H. D. Sarma

  3. Nuclear Medicine and PET Services, Kovai Medical Centre and Hospital, Coimbatore, 641014, India

    Ajit Shinto & E. R. Radhakrishnan

Authors
  1. Sudipta Chakraborty
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  2. K. V. Vimalnath
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  3. A. Rajeswari
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  4. H. D. Sarma
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  5. Ajit Shinto
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  6. E. R. Radhakrishnan
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  7. Ashutosh Dash
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Correspondence to Sudipta Chakraborty.

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Chakraborty, S., Vimalnath, K.V., Rajeswari, A. et al. Radiolanthanide-labeled HA particles in the treatment of rheumatoid arthritis: ready-to-use cold kits for rapid formulation in hospital radiopharmacy. J Radioanal Nucl Chem 302, 875–881 (2014). https://doi.org/10.1007/s10967-014-3309-5

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  • DOI: https://doi.org/10.1007/s10967-014-3309-5

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