Tumor Targeting by RGD-Grafted PLGA-Based Nanotheranostics Loaded with Paclitaxel and Superparamagnetic Iron Oxides

  • Fabienne Danhier
  • Pierre Danhier
  • Nathalie Schleich
  • Chrystelle Po
  • Sophie Laurent
  • Pierre Sibret
  • Christine Jérôme
  • Vincent Poucelle
  • Bernard Gallez
  • Véronique Préat
Part of the Methods in Pharmacology and Toxicology book series (MIPT)


Theranostic nanoparticles have the potential to revolutionize cancer diagnosis and therapy. Many groups have demonstrated differential levels of tumor growth between tumors treated by targeted or untargeted nanoparticles; however, only few have shown in vivo efficacy in both therapeutic and diagnostic approach. Herein, we first develop and characterize dual-paclitaxel (PTX)/superparamagnetic iron oxide (SPIO)-loaded PLGA-based nanoparticles grafted with the RGD peptide, for a theranostic purpose. Second, we compare in vivo different strategies in terms of targeting capabilities: (1) passive targeting via the EPR effect, (2) active targeting of αvβ3 integrin via RGD grafting, (3) magnetic guidance via a magnet placed on the tumor, and (4) the combination of the magnetic guidance and the active targeting of αvβ3 integrin. In this chapter, we present the general flowchart applied for this project: (1) the polymer and SPIO synthesis, (2) the physicochemical characterization of the nanoparticles, (3) the magnetic properties of the nanoparticles, and (4) the in vivo evaluation of the nanoparticles for their therapeutic and diagnosis purposes. We employ the electron spin resonance spectroscopy and magnetic resonance imaging to both quantify and visualize the accumulation of theranostic nanoparticles into the tumors.


PLGA-nanoparticles SPIO Paclitaxel Cancer therapy Magnetic resonance imaging Tumor targeting Nanotheranostic 



This work is supported by grants from the Université catholique de Louvain (F.S.R.) and Fonds National de la Recherche Scientifique (F.R.S.-F.N.R.S.). F. Danhier is a Postdoctoral F.R.S.-F.N.R.S. Research Fellow. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.


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Copyright information

© Springer Science+Business Media New York 2015

Authors and Affiliations

  • Fabienne Danhier
    • 1
  • Pierre Danhier
    • 2
  • Nathalie Schleich
    • 1
  • Chrystelle Po
    • 2
  • Sophie Laurent
    • 3
  • Pierre Sibret
    • 4
  • Christine Jérôme
    • 4
  • Vincent Poucelle
    • 5
  • Bernard Gallez
    • 2
  • Véronique Préat
    • 1
  1. 1.Louvain Drug Research Institute, Advanced Drug delivery and BiomaterialsUniversité catholique de LouvainBrusselsBelgium
  2. 2.Louvain Drug Research Institute, Laboratory of Biomedical Magnetic ResonanceUniversité catholique de LouvainBrusselsBelgium
  3. 3.Department of General, Organic, and Biomedical Chemistry, NMR and Molecular Imaging LaboratoryUniversité de MonsMonsBelgium
  4. 4.Center for Education and Research on MacromoleculeUniversité de LiègeLiègeBelgium
  5. 5.Unité de Chimie organique et médicinaleUniversité catholique de LouvainLouvain-la-NeuveBelgium

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