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

Ondřej Sedláček; Jan Kučka; Martin Hrubý

doi:10.1016/j.apradiso.2014.10.016

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

Appl Radiat Isot. 2015 Jan:95:129-134. doi: 10.1016/j.apradiso.2014.10.016. Epub 2014 Oct 27.

Authors

Ondřej Sedláček¹, Jan Kučka¹, Martin Hrubý²

Affiliations

¹ Institute of Macromolecular Chemistry AS CR, v.v.i., Heyrovsky Sq. 2, 162 06 Prague 6, Czech Republic.
² Institute of Macromolecular Chemistry AS CR, v.v.i., Heyrovsky Sq. 2, 162 06 Prague 6, Czech Republic. Electronic address: mhruby@centrum.cz.

PMID: 25464189
DOI: 10.1016/j.apradiso.2014.10.016

Abstract

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.

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