Uptake and Binding of At‐211 Into K‐ and Cs‐Derivatives of Alpha‐Zirconium Phosphate Nanoplatelets for Use as a Targeted Alpha Therapy Delivery Platform

Le résumé fourni par la source

The ion exchange behavior of K‐ and Cs‐derivatives of α‐zirconium phosphate, A‐ZrP, with the targeted alpha therapy (TAT) radionuclide 211 At, as At + and AtO + , has been investigated. The K‐ZrP shows strong affinity for both At + and AtO + , ≥99% uptake. The affinity to Cs‐ZrP was less pronounced, 87%–94% uptake, favoring At + . The binding strength was tested against several leaching solutions, including carbonate, phosphate buffered saline (PBS), 4‐(2‐hydroxyethyl)‐1‐piperazineethanesulfonic acid (HEPES) buffers, and ethylenediaminetetraacetic acid (EDTA) solutions at various concentrations (0.1–10 mM). K‐ZrP retained 211 At in all buffer and EDTA solutions up to 1 mM (<0.5% leaching). The Cs‐ZrP showed no leaching of At + , while AtO + leached (1%–3%) in the carbonate and HEPES buffers, along with all of the EDTA solutions, with complete retention only in the PBS buffer. In all cases, when the EDTA concentration reached 10 mM, 211 At leaching was observed. Once incorporated into the ZrP nanoplatelets, significant shielding of the α‐particles was observed, not only attenuating the intensity of the emission but also reducing the energy of the α‐particles themselves exiting the nanoplatelets. These properties provide the basis for K‐ZrP, and to a lesser extent, Cs‐ZrP to be further considered as potentially promising candidates for a delivery mechanism of 211 At for application in TAT.

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