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Functionalizing NaGdF4:Yb,Er Upconverting Nanoparticles with Bone-Targeting Phosphonate Ligands: Imaging and In Vivo Biodistribution

1
CIC biomaGUNE, Paseo de Miramón 182, 20014 Donostia, Spain
2
Donostia International Physics Center (DIPC), Manuel Lardizabal Ibilbidea 4, 20018 Donostia, Spain
3
Ikerbasque, Basque Foundation for Science, 48011 Bilbao, Spain
*
Authors to whom correspondence should be addressed.
Current address: BASF SE, Department of Material Physics & Analytics, Carl-Bosch-Strasse 38, 67056 Ludwigshafen, Germany.
Inorganics 2019, 7(5), 60; https://doi.org/10.3390/inorganics7050060
Received: 11 December 2018 / Revised: 12 April 2019 / Accepted: 19 April 2019 / Published: 30 April 2019
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Abstract

Lanthanide-doped upconverting nanoparticles (UCNPs) transform near infrared light (NIR) into higher-energy UV and visible light by multiphotonic processes. Owing to such unique feature, UCNPs have found application in optical imaging and have been investigated for the NIR light activation of prodrugs, including transition metal complexes of interest in photochemotherapy. Besides, UCNPs also function as magnetic resonance imaging (MRI) contrast agents and positron emission tomography (PET) probes when labelled with radionuclides such as 18F. In this contribution, we report on a new series of phosphonate-functionalized NaGdF4:Yb,Er UCNPs that show affinity for hydroxyapatite (inorganic constituent of bones), and we discuss their potential as bone targeting multimodal (MRI/PET) imaging agents. In vivo biodistribution studies of 18F-labelled NaGdF4:Yb,Er UCNPs in rats indicate that surface functionalization with phosphonates favours the accumulation of nanoparticles in bones over time. PET results reveal leakage of 18F for phosphonate-functionalized NaGdF4:Yb,Er and control nanomaterials. However, Gd was detected in the femur for phosphonate-capped UCNPs by ex vivo analysis using ICP-MS, corresponding to 6–7% of the injected dose. View Full-Text
Keywords: upconverting nanoparticles; phosphonates; bones; imaging; MRI; PET upconverting nanoparticles; phosphonates; bones; imaging; MRI; PET
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Alonso-de Castro, S.; Ruggiero, E.; Lekuona Fernández, A.; Cossío, U.; Baz, Z.; Otaegui, D.; Gómez-Vallejo, V.; Padro, D.; Llop, J.; Salassa, L. Functionalizing NaGdF4:Yb,Er Upconverting Nanoparticles with Bone-Targeting Phosphonate Ligands: Imaging and In Vivo Biodistribution. Inorganics 2019, 7, 60.

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