Technetium in Medicine

Mazzi, Ulderico; Schibli, Roger; Pietzsch, Hans‐Juergen; Kunstler, Jens-Uwe; Spies, Hartmut

doi:10.1007/978-3-540-33990-8_2

Cited by 10 publications

(13 citation statements)

References 44 publications

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“…In the neutralized [ 89 Zr]Zr-oxalate preparation, Zr 4+ is probably octachelated by four oxalates, resulting in an overall charge of −4 [18]. This hypothesis matches the anion displayed on electrophoresis results (Fig.…”

Section: Discussionsupporting

confidence: 78%

“…In the present case, when Zr is chelated, the radioactivity is significantly cleared from the mice body. The clearance of [ 89 Zr]Zr-oxalate (bidentate chelator [18]) is relevant as it resembles an unstable complex at physiological pH, in comparison to [ 89 Zr]Zr-citrate (tridentate chelator, moderately stable [19]) or [ 89 Zr]Zr-DFO (hexadentate chelator, stable complexes [20]). In addition, the biodistribution of [ 89 Zr]Zr-oxalate is characteristic of Zr itself with a strong affinity for the bones and the joints (see PET image, Fig.…”

Section: Discussionmentioning

confidence: 99%

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In vivo biodistribution and accumulation of 89Zr in mice

Abou

Smith‐Jones

2011

Nuclear Medicine and Biology

234

233

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Introduction The present investigation focuses on the chemical and biological fate of 89Zr in mice. Electrophoreses of 89Zr solvated or chelated in different conditions are here presented. The biological fate of mice injected with [89Zr]Zr-oxalate, [89Zr]Zr-chloride, [89Zr]Zr-phosphate, [89Zr]Zr-desferrioxamine and [89Zr]Zr-citrate is studied with the biodistribution, the clearances and PET images. A special focus is also given regarding the quality of 89Zr bone accumulation. Methods Electrophoreses were carried out on chromatography paper and read by gamma counting. Then, the solutions were intravenously injected in mice, imaged at different time points and sacrificed. The bones, the epiphysis and the marrow substance were separated and evaluated with gamma counts. Results The clearances of [89Zr]Zr-chloride and [89Zr]Zr-oxalate reached 20% of ID after 6 days whereas [89Zr]Zr-phosphate was only 5% of ID. [89Zr]Zr-citrate and [89Zr]Zr-DFO were noticeably excreted after the first day p.i.. [89Zr]Zr-chloride and [89Zr]Zr-oxalate resulted in a respective bone uptake of ~15% ID/g and~20% ID/g at 8 h p.i. with minor losses after 6 days. [89Zr]Zr-citrate bone uptake was also observed, but [89Zr]Zr-phosphate was absorbed in high amounts in the liver and the spleen. The marrow cells were insignificantly radioactive in comparison to the calcified tissues. Conclusion Despite the complexity of Zr coordination, the electrophoretic analyses provided detailed evidences of Zr charges either as salts or as complexes. This study also shows that weakly chelated, 89Zr is a bone seeker and has a strong affinity for phosphate.

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Section: Discussionsupporting

confidence: 78%

Section: Discussionmentioning

confidence: 99%

In vivo biodistribution and accumulation of 89Zr in mice

Abou

Smith‐Jones

2011

Nuclear Medicine and Biology

234

233

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“…They all exhibited good hypoxia selectivity in cell culture (S180 cells). Biodistribution in mice bearing induced tumour showed moderate uptake, superior to other 2-nitroimidazolic complexes bearing an isocyanide group as electron donors for Tc [21] and adequate tumour/muscle ratios. When pertechnetate is reduced in the presence of adequate ligands it frequently loses only part of the oxygen atoms leading to monoxo ([TcO] +3 ) or dioxo species ([TcO 2 ] +1 ) of Tc(V) [22].…”

Section: Labelling Strategies Of Nitroimidazoles With [ 99m Tc]tcmentioning

confidence: 88%

99mTc Labelling Strategies for the Development of Potential Nitroimidazolic Hypoxia Imaging Agents

Giglio

Rey

2019

Inorganics

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Technetium-99m has a rich coordination chemistry that offers many possibilities in terms of oxidation states and donor atom sets. Modifications in the structure of the technetium complexes could be very useful for fine tuning the physicochemical and biological properties of potential 99m Tc radiopharmaceuticals. However, systematic study of the influence of the labelling strategy on the "in vitro" and "in vivo" behaviour is necessary for a rational design of radiopharmaceuticals. Herein we present a review of the influence of the Tc complexes' molecular structure on the biodistribution and the interaction with the biological target of potential nitroimidazolic hypoxia imaging radiopharmaceuticals presented in the literature from 2010 to the present. Comparison with the gold standard [ 18 F]Fluoromisonidazole (FMISO) is also presented.

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“…For diagnosis, short-lived gamma- or positron-emitting radionuclides, including technetium-99m ( 99m Tc), gallium-68 ( 68 Ga), iodine-123 ( 123 I), indium-111 ( 111 In), fluorine-18 ( 18 F), and copper-64 ( 64 Cu), are extensively used for radiolabeling AuNPs [ 9 , 10 , 11 , 12 , 13 , 14 , 15 , 16 , 17 , 18 ]. 99m Tc is the most commonly used radionuclide in diagnostic imaging, due to its ideal nuclear characteristics, such as emission of low-energy γ-rays (140 keV) and suitable half-life (6.02 h), as well as its convenient availability from 99 Mo/ 99m Tc generators [ 19 , 20 ]. Labeling via the [ 99m Tc][Tc(H 2 O) 3 (CO) 3 ] + carbonyl core is a very efficient way of radiolabeling with 99m Tc and was first introduced by Alberto et al in 1998 [ 21 ].…”

Section: Introductionmentioning

confidence: 99%

“…[ 99m Tc]Tc(H 2 O) 3 (CO) 3 + is an ion with three coordination sites. Its water molecules can be substituted, which means that a huge variety of mono-, bi-, and tridentate ligands can be used and radiolabeled with the tricarbonyl core [ 18 , 20 ]. In this study, the two tridentate thiol ligands L 1 H and L 2 H (shown in Figure 1 ) were used: (i) to stabilize the AuNPs by forming strong Au-S bonds [ 12 ] and (ii) to form a complex with the [ 99m Tc][Tc(CO) 3 ] + core via the three nitrogen atoms that acted as donor atoms [ 19 , 20 ].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and In Vitro Evaluation of Gold Nanoparticles Functionalized with Thiol Ligands for Robust Radiolabeling with 99mTc

et al. 2021

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Radiolabeled gold nanoparticles (AuNPs) have been widely used for cancer diagnosis and therapy over recent decades. In this study, we focused on the development and in vitro evaluation of four new Au nanoconjugates radiolabeled with technetium-99m (99mTc) via thiol-bearing ligands attached to the NP surface. More specifically, AuNPs of two different sizes (2 nm and 20 nm, referred to as Au(2) and Au(20), respectively) were functionalized with two bifunctional thiol ligands (referred to as L1H and L2H). The shape, size, and morphology of both bare and ligand-bearing AuNPs were characterized by transmission electron microscopy (TEM) and dynamic light scattering (DLS) techniques. In vitro cytotoxicity was assessed in 4T1 murine mammary cancer cells. The AuNPs were successfully radiolabeled with 99mTc-carbonyls at high radiochemical purity (>95%) and showed excellent in vitro stability in competition studies with cysteine and histidine. Moreover, lipophilicity studies were performed in order to determine the lipophilicity of the radiolabeled conjugates, while a hemolysis assay was performed to investigate the biocompatibility of the bare and functionalized AuNPs. We have shown that the functionalized AuNPs developed in this study lead to stable radiolabeled nanoconstructs with the potential to be applied in multimodality imaging or for in vivo tracking of drug-carrying AuNPs.

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Technetium in Medicine

Cited by 10 publications

References 44 publications

In vivo biodistribution and accumulation of 89Zr in mice

In vivo biodistribution and accumulation of 89Zr in mice

99mTc Labelling Strategies for the Development of Potential Nitroimidazolic Hypoxia Imaging Agents

Synthesis and In Vitro Evaluation of Gold Nanoparticles Functionalized with Thiol Ligands for Robust Radiolabeling with 99mTc

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