4.4 Article

Optimized protocol for the radioiodination of hydrazone-type polymer drug delivery systems

Journal

APPLIED RADIATION AND ISOTOPES
Volume 95, Issue -, Pages 129-134

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.apradiso.2014.10.016

Keywords

Doxorubicin; Hydrazone; Polymer conjugate; Radiolabeling; Radioiodination; poly[N-(2-hydroxypropyl)methacrylamide]

Funding

  1. Ministry of Industry and Trade of the Czech Republic [MPO TIP FR-TI4/625]
  2. Grant Agency of the Czech Republic [P304-12-0950]
  3. Academy of Sciences of the Czech Republic [M200501201]
  4. Ministry of Education, Youth and Sports [MSMT KONTAKT II LH14079]

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Hydrazone conjugates of polymers with doxorubicin represent a very promising tool for cancer chemotherapy. However, these conjugates are very difficult to radiolabel with iodine radionuclides, which possess otherwise very advantageous nuclear properties to, e.g., follow biodistribution. In this study, we developed a robust protocol for the high-yield radioiodination of hydrazone-type drug delivery systems with doxorubicin. In particular, it is crucial that the polymer radioiodination step be performed before the deprotection of the hydrazide and doxorubicin binding. (C) 2014 Elsevier Ltd. All rights reserved.

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