title: Multifunctional dendrimer-entrapped gold nanoparticles modified with RGD peptide for targeted computed tomography/magnetic resonance dual-modal imaging of tumors.
abstract: We 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.
authors.forename: Qian
authors.initials: Q
authors.lastname: Chen
authors.affiliation: §Department of Radiology, Shanghai First People's Hospital, School of Medicine, Shanghai Jiaotong University, Shanghai 200080, People's Republic of China.
authors.forename: Han
authors.initials: H
authors.lastname: Wang
authors.forename: Hui
authors.initials: H
authors.lastname: Liu
authors.forename: Shihui
authors.initials: S
authors.lastname: Wen
authors.affiliation: ∥Department of Radiology, School of Medicine, Shanghai Tenth People's Hospital Affiliated with Tongji University, Shanghai 200072, People's Republic of China.
authors.forename: Chen
authors.initials: C
authors.lastname: Peng
authors.forename: Mingwu
authors.initials: M
authors.lastname: Shen
authors.affiliation: §Department of Radiology, Shanghai First People's Hospital, School of Medicine, Shanghai Jiaotong University, Shanghai 200080, People's Republic of China.
authors.forename: Guixiang
authors.initials: G
authors.lastname: Zhang
authors.affiliation: ⊥CQM-Centro de Química da Madeira, Universidade da Madeira, Campus da Penteada, 9000-390 Funchal, Portugal.
authors.forename: Xiangyang
authors.initials: X
authors.lastname: Shi
mesh_terms: D000818:Animals; D002470:Cell Survival / Q000187:drug effects; D050091:Dendrimers / Q000737:chemistry*; D006046:Gold / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008279:Magnetic Resonance Imaging; D008297:Male; D053768:Metal Nanoparticles / Q000737:chemistry; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D009374:Neoplasms, Experimental / Q000175:diagnosis*; D009842:Oligopeptides / Q000737:chemistry / Q000494:pharmacology; D014018:Tissue Distribution; D014057:Tomography, X-Ray Computed; D014407:Tumor Cells, Cultured
chemical_list: D050091:Dendrimers; D009842:Oligopeptides; D006046:Gold; C047981:arginyl-glycyl-aspartic acid