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Multifunctional Dendrimer-Entrapped Gold Nanoparticles Modified with RGD Peptide for Targeted Computed Tomography/Magnetic Resonance Dual-Modal Imaging of Tumors
journal contribution
posted on 2015-04-07, 00:00 authored by Qian Chen, Han Wang, Hui Liu, Shihui Wen, Chen Peng, Mingwu Shen, Guixiang Zhang, Xiangyang ShiWe
report the use of multifunctional dendrimer-entrapped gold nanoparticles
(Au DENPs) loaded with gadolinium (Gd) chelator/Gd(III) complexes
and surface-modified with thiolated cyclo(Arg-Gly-Asp-Phe-Lys(mpa))
(RGD) peptide for targeted dual-mode computed tomography (CT)/magnetic
resonance (MR) imaging of small tumors. In this study, amine-terminated
generation 5 poly(amidoamine) dendrimers were used as a nanoplatform
to be covalently modified with Gd chelator, RGD via a polyethylene
glycol (PEG) spacer, and PEG monomethyl ether. Then the multifunctional
dendrimers were used as templates to entrap gold nanoparticles, followed
by chelating Gd(III) ions and acetylation of the remaining dendrimer
terminal amines. The thus-formed multifunctional Au DENPs (in short,
Gd–Au DENPs-RGD) were characterized via different techniques.
We show that the multifunctional Au DENPs with a Au core size of 3.8
nm are water-dispersible, stable under different pH (5–8) and
temperature conditions (4–50 °C), and noncytotoxic at
a Au concentration up to 100 μM. With the displayed X-ray attenuation
property and the r1 relaxivity (2.643
mM–1 s–1), the developed Gd–Au
DENPs-RGD are able to be used as a dual-mode nanoprobe for targeted
CT/MR imaging of an αvβ3 integrin-overexpressing xenografted small tumor model in
vivo via RGD-mediated active targeting pathway. The developed multifunctional
Gd–Au DENPs-RGD may be used as a promising dual-mode nanoprobe
for targeted CT/MR imaging of different types of αvβ3 integrin-overexpressing cancer.