Targeted RGD nanoparticles for highly sensitive in vivo integrin receptor imaging

Contrast Media & Molecular Imaging
Ren-Yen LinYun-Ming Wang

Abstract

A new magnetic resonance imaging (MRI) contrast bearing RGD peptide is reported. In this study, ultrasmall superparamagnetic iron oxide (USPIO) nanoparticles with various sizes were prepared. Particles sizes between 6 and 13 nm were tuned by varying the stirring rate. Remarkable negative contrast was observed because USPIO nanoparticles (13.1  ±  2.1 nm) generated high transversal relaxivity r₂ (188  ±  3 m m(-1)  s(-1) ) and saturation magnetization (94 emu g(-1) Fe). The USPIO nanoparticles were coated with PDA [2-(pyridyldithio)-ethylamine; PDA nanoparticles] containing functional polymer, which can be readily synthesized by Michael addition. The PDA nanoparticles were conjugated with RGD peptide (RGD nanoparticles) for targeting the specific site. The target specificity and high relaxivity allowed RGD nanoparticles to differentiate the expression level of integrin receptor on several cell lines and tumors (MCF-7, A-549, HT-29 and HT-1080) by in vitro and in vivo MR imaging. Importantly, a remarkable negative contrast (-51.3 ± 6.7%) was observed for in vivo MR imaging of MCF-7 tumor. This result implies that the RGD nanoparticles that greatly enhance the MR imaging are highly sensitive for early stage tumor detection.

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Citations

Feb 28, 2013·Therapeutic Delivery·Neelesh Kumar MehraNarendra K Jain
Sep 3, 2014·Journal of Controlled Release : Official Journal of the Controlled Release Society·Nathalie SchleichVéronique Préat
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Apr 11, 2019·Molecular Pharmaceutics·Barbara AlbertiniNathalie Wauthoz

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