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Publications

Journal Article Epublish 1 citation

PubMed: 41667650 DOI: 10.1038/s44303-026-00142-1

A single-step radiolabeling strategy for PET, SPECT, and therapeutic radionuclides using nanoparticles as a universal chelator.

Npj Imaging 4(1):8

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

Affiliations

  • Nanomedicina, Imagen y modelos 3D (NI3D), Instituto de Química Médica (IQM/CSIC), Madrid, Spain.
  • Nanomedicina, Imagen y modelos 3D (NI3D), Instituto de Química Médica (IQM/CSIC), Madrid, Spain. Universidad Autónoma de Madrid, Escuela de Doctorado Cantoblanco, Madrid, Spain.
  • Cardiovascular Risk Factors and Brain Function Programme, Centro Nacional de Investigaciones Cardiovasculares (CNIC) Carlos III, Madrid, Spain.
  • Instituto de Investigación Sanitaria Fundación Jiménez Díaz (IIS-FJD), Madrid, Spain.
  • CIC biomaGUNE, Basque Research and Technology Alliance (BRTA), Donostia San Sebastián, Spain.
  • Institute for Biomedical Research Sols-Morreale (IIBM), CSIC-UAM, Madrid, Spain. Biomedical Research Networking Centre on Rare Diseases (CIBERER), Institute of Health Carlos III, Madrid, Spain.
  • Instituto de Nanociencia y Materiales de Aragón, INMA (CSIC-Universidad de Zaragoza) and CIBER-BBN, Zaragoza, Spain.
  • Unidad de Aplicaciones Médicas de las Radiaciones Ionizantes, Centro de Investigaciones Energéticas, Medioambientales y Tecnológicas (CIEMAT), Madrid, Spain.
  • Nanomedicina, Imagen y modelos 3D (NI3D), Instituto de Química Médica (IQM/CSIC), Madrid, Spain. CIBER Enfermedades Respiratorias (CIBERES), Madrid, Spain.
  • Institute for Biomedical Research Sols-Morreale (IIBM), CSIC-UAM, Madrid, Spain.
  • Biomedical Research Networking Centre on Rare Diseases (CIBERER), Institute of Health Carlos III, Madrid, Spain.
  • School of Biomedical Engineering and Imaging Sciences, King's College London, London, UK.
  • Centro de Neurociencias Cajal - CSIC, Alcalá de Henares, Spain.
  • CIC biomaGUNE, Basque Research and Technology Alliance (BRTA), Donostia San Sebastián, Spain. CIBER Enfermedades Respiratorias (CIBERES), Madrid, Spain. Ikerbasque, Basque Foundation for Science, Bilbao, Spain. NMR and Imaging in Biomedicine Group, Department of Chemistry in Pharmaceutical Sciences, Pharmacy School, University Complutense Madrid, Madrid, Spain.
  • CIBER Enfermedades Respiratorias (CIBERES), Madrid, Spain.
  • Institute of Materials Science of Barcelona (ICMAB-CSIC), Campus of the UAB, Bellaterra, Spain.
  • Nanomedicina, Imagen y modelos 3D (NI3D), Instituto de Química Médica (IQM/CSIC), Madrid, Spain.
  • CIBER Enfermedades Respiratorias (CIBERES), Madrid, Spain.

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 68Ga, 64Cu, 89Zr, 99mTc, 201Tl, 111In, 67Ga, 177Lu, 223Ra, and 225Ac 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.

MeSH

Chelating Agents, Nanoparticles, Radiopharmaceuticals, Tomography, Emission-Computed, Single-Photon, Glioblastoma, Therapeutics