Synthesis and characterization of lanthanum phosphate nanoparticles as carriers for 223Ra and 225Ra for targeted alpha therapy

Abstract

The in vitro retention of both parents and daughters results suggests that LaPO4 NPs are potentially effective carriers of radium isotopes.

Current Aspects of Radiopharmaceutical Chemistry

“…These studies revealed excellent retention of radioactivity in integrin positive tumors, and a complete biodistribution profile that was consistent with RGD-based radiopharmaceuticals [102]. In a recent publication, Summers, et al extended the evaluation of the FSC ligand by conjugating it to the anti-EGFR affibody, ZEGFR:23377 using a maleimide-based bioconjugation strategy to produce FSC-ZEGFR:23377 [103]. This bioconjugate was radiolabeled in a facile manner using [ 89 Zr]Zr(ox) 2 and radiochemical methods typically used to prepare [ 89 Zr]Zr-DFO-mAbs.…”

“…Consequent conjugation of LaPO 4 NPs to 201b mAb, targeting trombomodulin in lung endothelium was carried out using a lipoamide polyethylene glycol (dPEG)-COOH linker. Efficacy of the NPs-antibody conjugate system was demonstrated on reduced EMT-6 lung colonies [102,103].…”

“…(Table 4) [101]. 22 (IC 50 :~300 nM for HDAC1;~8 μM for HDAC3 [102]) is a potent, long-lasting, brain region-selective HDAC inhibitor that shows a dose-dependent increase in histone 3 acetylation in the rat brain [103]; however, no direct evidence was obtained for BBB permeability of 22. They synthesized [ 11 C]22 by direct incorporation of [ 11 C]CO 2 into the carbamate carbon [104].…”

An overview of nanoscale radionuclides and radiolabeled nanomaterials commonly used for nuclear molecular imaging and therapeutic functions

“…Standard biodistribution techniques and microSPECT/CT imaging of 225 Ac as well as the daughter radioisotopes showed that the NPs accumulated rapidly in mouse lung after intravenous injection. Rojas et al 109 also reported synthesis and characterization of LnPO 4 NPs as carriers for 223 Ra and 225 Ra for targeted alpha therapy. Sobol and co-workers 110 described the synthesis and targeting of gold-coated 177 Lu-containing LnPO 4 NPs as a potential theranostic agent for pulmonary metastatic disease.…”

Radiolabeled Nanoparticles in Nuclear Oncology

“…For this purpose, core lanthanum phosphate and core-shell (with up to two shells) nanoparticles were evaluated pertaining to their capability to retain 223 Ra and 225 Ra/ 225 Ac isotopes, and were shown to exhibit satisfactory retention abilities as radioisotope nanocarriers [120]. Mokhodoeva et al investigated the direct labeling of SPIONs with 223 Ra, the first alpha-emitting radioisotope with FDA approval for clinical application.…”