Abstract
The present study describes a novel method for the low energy cyclotron production and radiochemical isolation of no-carrier-added 132/135La3+ from bulk natBa. This separation strategy combines precipitation and single-column extraction chromatography to afford an overall radiochemical yield (92 ± 2%) and apparent molar activity (22 ± 4 Mbq/nmol) suitable for the radiolabeling of DOTA-conjugated vectors. The produced 132/135La3+ has a radiochemical and radionuclidic purity amenable for 132La/135La-based cancer theranostic applications. Longitudinal PET/CT images acquired using the positron-emitting 132La and ex vivo biodistribution data separately corroborated the accumulation of unchelated 132/135La3+ ions in bone and the liver.
Highlights
Targeted Radionuclide Therapy (TRT) using electron-emitting radiometals has shown efficacy in the treatment of several malignancies
As target preparation was performed in air, the target was immediately installed on the cyclotron and exposed to high vacuum to limit barium oxidation
The irradiation of the target was performed at a proton energy of
Summary
Targeted Radionuclide Therapy (TRT) using electron-emitting radiometals has shown efficacy in the treatment of several malignancies. Given the high linear energy transfer (LET) of Auger electrons, isotopes decaying by electron capture have the potential to locally deposit dose in target tissue while sparing normal tissues. In this regard, 135La (t1/2 = 19.93 h, 100% EC) is promising due to its suitable decay characteristics (Fig. 1A) and chemical properties resembling other common therapeutic radiometals (e.g., 177Lu, 90Y or 225Ac). Reported production cross-sections for 13xLa radioisotopes from 12–70 MeV of natBa targets show that differential decay kinetics form 135La with high radionuclidic purity at energies available on most medical cyclotrons[1,2,3,4]. Our goal was to develop an optimized production method for 132/135La with a chemical purity suitable for chelation and in vivo PET imaging of radiolabeled, targeted theranostic pharmaceuticals
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