cRGD-functionalized, DOX-conjugated, and ⁶⁴Cu-labeled superparamagnetic iron oxide nanoparticles for targeted anticancer drug delivery and PET/MR imaging.

Abstract:

:Multifunctional and water-soluble superparamagnetic iron oxide (SPIO) nanocarriers were developed for targeted drug delivery and positron emission tomography/magnetic resonance imaging (PET/MRI) dual-modality imaging of tumors with integrin α(v)β₃ expression. An anticancer drug was conjugated onto the PEGylated SPIO nanocarriers via pH-sensitive bonds. Tumor-targeting ligands, cyclo(Arg-Gly-Asp-d-Phe-Cys) (c(RGDfC)) peptides, and PET ⁶⁴Cu chelators, macrocyclic 1,4,7-triazacyclononane-N, N', N″-triacetic acid (NOTA), were conjugated onto the distal ends of the PEG arms. The effectiveness of the SPIO nanocarriers as an MRI contrast agent was evaluated via an in vitro r₂ MRI relaxivity measurement. cRGD-conjugated SPIO nanocarriers exhibited a higher level of cellular uptake than cRGD-free ones in vitro. Moreover, cRGD-conjugated SPIO nanocarriers showed a much higher level of tumor accumulation than cRGD-free ones according to non-invasive and quantitative PET imaging, and ex vivo biodistribution studies. Thus, these SPIO nanocarriers demonstrated promising properties for combined targeted anticancer drug delivery and PET/MRI dual-modality imaging of tumors.

journal_name

Biomaterials

journal_title

Biomaterials

authors

Yang X,Hong H,Grailer JJ,Rowland IJ,Javadi A,Hurley SA,Xiao Y,Yang Y,Zhang Y,Nickles RJ,Cai W,Steeber DA,Gong S

doi

10.1016/j.biomaterials.2011.02.006

subject

Has Abstract

pub_date

2011-06-01 00:00:00

pages

4151-60

issue

17

eissn

0142-9612

issn

1878-5905

pii

S0142-9612(11)00144-X

journal_volume

32

pub_type

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