Journal
CHEMMEDCHEM
Volume 4, Issue 6, Pages 988-997Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.200800424
Keywords
antitumor agents; chemical functionalization; drug delivery; nanoparticles; superparamagnetism
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Funding
- Swiss National Scientific Research Foundation [3152A0-105705]
- Swiss League and Research against Cancer [KLS-01308-02-2003]
- NSERC (Canada)
- FQRNT (Province of Quebec)
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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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