TrisOxine abiotic siderophores for technetium complexation: radiolabeling and biodistribution studies
Background Despite the development of positron emission tomography (PET), single photon emission computed tomography (SPECT) still accounts for around 80% of all examinations performed in nuclear medicine departments. The search for new radiotracers or chelating agents for Technetium-99m is therefor...
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Published in | EJNMMI radiopharmacy and chemistry Vol. 8; no. 1; p. 32 |
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Main Authors | , , , , , , , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
Cham
Springer International Publishing
19.10.2023
Springer Nature B.V London : Springer Open SpringerOpen |
Subjects | |
Online Access | Get full text |
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Summary: | Background
Despite the development of positron emission tomography (PET), single photon emission computed tomography (SPECT) still accounts for around 80% of all examinations performed in nuclear medicine departments. The search for new radiotracers or chelating agents for Technetium-99m is therefore still ongoing.
O-
TRENSOX and
O-
TRENOX two synthetic siderophores would be good candidates for this purpose as they are hexadentate ligands based on the very versatile and efficient 8-hydroxyquinoline chelating subunit. First, the radiolabeling of
O-
TRENOX and
O
-TRENSOX with
99m
Tc was investigated. Different parameters such as the quantity of chelating agent, type of reducing agent, pH and temperature of the reaction mixture were adjusted in order to find the best radiolabeling conditions. Then an assessment of the partition coefficient by measuring the distribution of each radiosynthesized complex between octanol and phosphate-buffered saline was realized. The complex’s charge was evaluated on three different celluloses (neutral, negatively charged P81 and positively charged DE81), and finally in vivo studies with biodistribution and SPECT imaging of [
99m
Tc]Tc-
O-
TRENOX and [
99m
Tc]Tc-
O-
TRENSOX were performed.
Results
The radiolabeling studies showed a rapid and efficient complexation of
99m
Tc with both chelating agents. Using tin pyrophosphate as the reducing agent and a minimum of 100 nmol of ligand, we obtained the [
99m
Tc]Tc-
O-
TRENOX complex with a radiochemical purity of more than 98% and the [
99m
Tc]Tc-
O-
TRENSOX complex with one above 97% at room temperature within 5 min. [
99m
Tc]Tc-
O-
TRENOX complex was lipophilic and neutral, leading to a hepatobiliary elimination in mice. On the contrary, the [
99m
Tc]Tc-
O-
TRENSOX complex was found to be hydrophilic and negatively charged. This was confirmed by a predominantly renal elimination in mice.
Conclusions
These encouraging results allow us to consider the
O-
TRENOX/
99m
Tc and
O-
TRENSOX/
99m
Tc complexes as serious candidates for SPECT imaging chelators. This study should be continued by conjugating these tris-oxine ligands to peptides or antibodies and comparing them with the other bifunctional agents used with Tc. |
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Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 2365-421X 2365-421X |
DOI: | 10.1186/s41181-023-00214-2 |