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Surface-Functionalized Ultrasmall Superparamagnetic Nanoparticles as Magnetic Delivery Vectors for Camptothecin

  1. Feride Cengelli1,†,
  2. Justyna A. Grzyb Dr.2,†,
  3. Auxia Montoro1,
  4. Heinrich Hofmann Prof. Dr.3,
  5. Stephen Hanessian Prof. Dr.2,
  6. Lucienne Juillerat-Jeanneret Dr.1

Article first published online: 3 APR 2009

DOI: 10.1002/cmdc.200800424

Issue

ChemMedChem

ChemMedChem

Special Issue: XIX NMMC Verona 2008

Volume 4, Issue 6, pages 988–997, June 8, 2009

Additional Information

How to Cite

Cengelli, F., Grzyb, Justyna A., Montoro, A., Hofmann, H., Hanessian, S. and Juillerat-Jeanneret, L. (2009), Surface-Functionalized Ultrasmall Superparamagnetic Nanoparticles as Magnetic Delivery Vectors for Camptothecin. ChemMedChem, 4: 988–997. doi: 10.1002/cmdc.200800424

Author Information

  1. 1

    Centre Hospitalier Universitaire Vaudois and University of Lausanne, University Institute of Pathology, Rue du Bugnon 25, CH-1011 Lausanne (Switzerland), Fax: (+41) 21-314-7115

  2. 2

    Department of Chemistry, University of Montreal, P.O. Box 6128, Station Centre-ville, Montreal, QC, H3C 3J7 (Canada), Fax: (+514) 343-5728

  3. 3

    Powder Technology Laboratory, Institute of Materials, Swiss Federal Institute of Technology, EPFL, MX-Ecublens, 1015 Lausanne (Switzerland)

  1. †

    These authors contributed equally to this work

  1. †

    These authors contributed equally to this work

Publication History

  1. Issue published online: 28 MAY 2009
  2. Article first published online: 3 APR 2009
  3. Manuscript Revised: 2 MAR 2009
  4. Manuscript Received: 11 DEC 2008

Funded by

  • Swiss National Scientific Research Foundation. Grant Number: 3152A0-105705
  • Swiss League and Research against Cancer. Grant Number: KLS-01308-02-2003
  • NSERC
  • FQRNT

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Keywords:

  • antitumor agents;
  • chemical functionalization;
  • drug delivery;
  • nanoparticles;
  • superparamagnetism

Abstract

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Drug–nanoparticle conjugates: The anticancer drug camptothecin (CPT) was covalently linked at the surface of ultrasmall superparamagnetic iron oxide nanoparticles (USPIOs) via a linker, allowing drug release by cellular esterases. Nanoparticles were hierarchically built to achieve magnetically-enhanced drug delivery to human cancer cells and antiproliferative activity.

The linking of therapeutic drugs to ultrasmall superparamagnetic iron oxide nanoparticles (USPIOs) allowing intracellular release of the active drug via cell-specific mechanisms would achieve tumor-selective magnetically-enhanced drug delivery. To validate this concept, we covalently attached the anticancer drug camptothecin (CPT) to biocompatible USPIOs (iron oxide core, 9–10 nm; hydrodynamic diameter, 52 nm) coated with polyvinylalcohol/polyvinylamine (PVA/aminoPVA). A bifunctional, end-differentiated dicarboxylic acid linker allowed the attachment of CPT to the aminoPVA as a biologically labile ester substrate for cellular esterases at one end, and as an amide at the other end. These CPT–USPIO conjugates exhibited antiproliferative activity in vitro against human melanoma cells. The intracellular localization of CPT–USPIOs was confirmed by transmission electron microscopy (iron oxide core), suggesting localization in lipid vesicles, and by fluorescence microscopy (CPT). An external static magnetic field applied during exposure increased melanoma cell uptake of the CPT–USPIOs.

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