A single-step radiolabeling strategy for PET, SPECT, and therapeutic radionuclides using nanoparticles as a universal chelator
Year: 2026
Type: article
Abstract: Radiopharmaceuticals that combine diagnostic and therapeutic isotopes are at the forefront of novel cancer treatments. A crucial element is the method of attaching radioisotopes to biomolecules using chelator-based techniques that are widely used clinically. Selection from available chelators is essential because this choice influences the physicochemical and biological characteristics of the final radiopharmaceutical. Numerous chelators exist because none fulfill all ideal conditions: rapid and complete binding to radiometals at low concentrations and with metallic impurities, high thermodynamic and kinetic stability in vivo, easy bioconjugation, and, key for this work, achieving these for many radiometals from the growing list of medical isotopes. We demonstrate how nanotechnology may change this. Ten nano-radiotracers were synthesized, incorporating radiometals such as 68 Ga, 64 Cu, 89 Zr, 99m Tc, 201 Tl, 111 In, 67 Ga, 177 Lu, 223 Ra, and 225 Ac into the nanoparticle core. The versatility of the platform was demonstrated through proof-of-concept experiments, including passive targeting in glioblastoma, active targeting of thrombosis, intratumoral radiotherapy in glioblastoma, and renal clearance optimization. This nanotracer addresses traditional challenges in radiopharmaceutical development, offering a single platform with consistent physicochemical and biological properties regardless of the radioisotope used for robust diagnostic and therapeutic applications.
Source: npj Imaging
Authors: Aitor Herraiz, Andrea Rodríguez-San-Pedro, Marta Casquero-Veiga, Unai Cossío, Nuria Arias-Ramos, Lucía Gutiérrez, Eduardo Romero-Sanz, Víctor Manuel Luján-Rodríguez, Carlos Cerón, Marta Oteo, Ana González-Paredes, Pilar López-Larrubia, Rafael T. M. de Rosales, Marta Cortes-Canteli, Miguel A. Morcillo, Jesús Ruiz-Cabello, Juan Pellico, Fernando Herranz
Institutions: Consejo Superior de Investigaciones Científicas, Instituto de Química Médica, Universidad Autónoma de Madrid, Spanish National Centre for Cardiovascular Research, Instituto de Investigación Sanitaria Fundación Jiménez Díaz, CIC biomaGUNE, Instituto de Salud Carlos III, Instituto de Investigaciones Biomédicas Sols-Morreale, Centre for Biomedical Network Research on Rare Diseases, Universidad de Zaragoza, Instituto de Nanociencia y Materiales de Aragón, Centro de Investigaciones Energéticas, Medioambientales y Tecnológicas, Centro de Investigación Biomédica en Red de Enfermedades Respiratorias, King's College London, Centro de Neurociencias Cajal, Ikerbasque, Universidad Complutense de Madrid, Institut de Ciència de Materials de Barcelona
Language: English
Subfield: Radiology, Nuclear Medicine and Imaging
Field: Medicine
Domain: Health Sciences
Open Access status: gold
Estimated APC paid: $2,790
OpenAlex ID: W7128548396
