SYNTHESIS, CHARACTERIZATION AND IN VIVO BEHAVIOR OF 177Lu-DMSA-SPIONs

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Abstract
Combined radionuclide therapy with magnetic nanoparticles has been a research focus as a promising approach for tumor therapy. In this study, superparamagnetic iron oxide nanoparticles (SPIONs) were synthesized using the co-precipitation method and coated with meso-1,2- dimercaptosuccinic acid (DMSA). Structural investigations showed that DMSA-coated SPIONs had a particle size of 140.3±6.5 nm in diameter with a spherical morphology. With a zeta potential of −35.1 mV, functionalization with DMSA led to increase the stability of the nanoparticles in solution. DMSA-SPIONs were radiolabeled with 177Lu in high radiolabeling yield (86.6 ± 2.1%, and after separation by magnetic decantation >99%), showing high in vitro stability in saline and human serum up to 96 h. After intratumoral injection into mouse colorectal CT-26 or breast 4T1 subcutaneous tumors, the radiolabeled nanoparticles remained well localized at the injection site over a 14-day period, with limited leakage.