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Radiosynthesis of Stable 198 Au-Nanoparticles by Neutron Activation of α v β 3 -Specific AuNPs for Therapy of Tumor Angiogenesis

Affiliation
Molecular Imaging and Radiochemistry, Clinic of Radiology and Nuclear Medicine, Medical Faculty Mannheim of Heidelberg University, 68167 Mannheim, Germany;
Davarci, Güllü;
ORCID
0000-0003-1161-8669
Affiliation
Biomedical Chemistry, Clinic of Radiology and Nuclear Medicine, Medical Faculty Mannheim of Heidelberg University, 68167 Mannheim, Germany;
Wängler, Carmen;
Affiliation
Research Reactor TRIGA Mainz, Institute for Nuclear Chemistry, Johannes-Gutenberg-Universität Mainz, 55128 Mainz, Germany;(K.E.);(C.G.)
Eberhardt, Klaus;
Affiliation
Research Reactor TRIGA Mainz, Institute for Nuclear Chemistry, Johannes-Gutenberg-Universität Mainz, 55128 Mainz, Germany;(K.E.);(C.G.)
Geppert, Christopher;
ORCID
0000-0002-7098-3036
Affiliation
Department of Oncology, Division of Oncological Imaging, University of Alberta, Edmonton, AB T6G 2R3, Canada;
Schirrmacher, Ralf;
Affiliation
Department of Nuclear Medicine, University Hospital Carl Gustav Carus, TU Dresden, 01307 Dresden, Germany;
Freudenberg, Robert;
ORCID
0000-0002-6432-5694
Affiliation
Molecular Imaging and Radiochemistry, Clinic of Radiology and Nuclear Medicine, Medical Faculty Mannheim of Heidelberg University, 68167 Mannheim, Germany;
Pretze, Marc;
ORCID
0000-0003-3877-5576
Affiliation
Molecular Imaging and Radiochemistry, Clinic of Radiology and Nuclear Medicine, Medical Faculty Mannheim of Heidelberg University, 68167 Mannheim, Germany;
Wängler, Björn

This paper reports on the development of stable tumor-specific gold nanoparticles (AuNPs) activated by neutron irradiation as a therapeutic option for the treatment of cancer with high tumor angiogenesis. The AuNPs were designed with different mono- or dithiol-ligands and decorated with different amounts of Arg-Gly-Asp (RGD) peptides as a tumor-targeting vector for α v β 3 integrin, which is overexpressed in tissues with high tumor angiogenesis. The AuNPs were evaluated for avidity in vitro and showed favorable properties with respect to tumor cell accumulation. Furthermore, the therapeutic properties of the [ 198 Au]AuNPs were evaluated in vitro on U87MG cells in terms of cell survival, suggesting that these [ 198 Au]AuNPs are a useful basis for future therapeutic concepts.

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