Journal of Radioanalytical and Nuclear Chemistry

, Volume 314, Issue 2, pp 1337–1345 | Cite as

Synthesis and in vitro evaluation of an antiangiogenic cancer-specific dual-targeting 177Lu-Au-nanoradiopharmaceutical

  • Abraham González-Ruíz
  • Guillermina Ferro-Flores
  • Erika Azorín-Vega
  • Blanca Ocampo-García
  • Flor de Maria Ramírez
  • Clara Santos-Cuevas
  • Luis De León-Rodríguez
  • Keila Isaac-Olivé
  • Myrna Luna-Gutiérrez
  • Enrique Morales-Ávila


The aim of this research was to synthesize and chemically characterize a cancer-specific 177Lu-Au-nanoradiopharmaceutical based on gold nanoparticles (NPs), the nuclear localization sequence (NLS)-Arg-Gly-Asp peptide and an aptamer (HS-pentyl-pegaptanib) to target both the α(v)β(3) integrin and the vascular endothelial growth factor (VEGF) overexpressed in the tumor neovasculature, as well as to evaluate by the tube formation assay, the nanosystem capability to inhibit angiogenesis. 177Lu-NP-RGD-NLS-Aptamer was obtained with a radiochemical purity of 99 ± 1%. Complete inhibition of tube formation (angiogenesis) was demonstrated when endothelial cells (EA.hy926), cultured in a 3D-extracellular matrix support, were treated with the developed nanosystem.


Lutetium-177 177Lu-gold nanoparticles Antiangiogenic agent RGD HS-pentyl-pegaptanib VEGF inhibition α(v)β(3) integrin 



This study was supported by the Mexican National Council of Science and Technology (CONACYT-SEP-CB-2014-01-242443). This research was carried out as part of the activities of the “Laboratorio Nacional de Investigación y Desarrollo de Radiofármacos, CONACyT”.

Supplementary material

10967_2017_5465_MOESM1_ESM.docx (498 kb)
Supplementary material 1 (DOCX 499 kb)


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Copyright information

© Akadémiai Kiadó, Budapest, Hungary 2017

Authors and Affiliations

  • Abraham González-Ruíz
    • 1
    • 2
  • Guillermina Ferro-Flores
    • 1
  • Erika Azorín-Vega
    • 1
  • Blanca Ocampo-García
    • 1
  • Flor de Maria Ramírez
    • 1
  • Clara Santos-Cuevas
    • 1
  • Luis De León-Rodríguez
    • 3
  • Keila Isaac-Olivé
    • 2
  • Myrna Luna-Gutiérrez
    • 1
  • Enrique Morales-Ávila
    • 2
  1. 1.Instituto Nacional de Investigaciones Nucleares, Carretera México-Toluca S/NOcoyoacacMexico
  2. 2.Universidad Autónoma del Estado de México, Paseo Tollocan S/NTolucaMexico
  3. 3.The University of AucklandAucklandNew Zealand

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