Labeling, characterization, and in vivo localization of a new Y-90-based phosphonate chelate 2,3-dicarboxypropane-1,1-diphosphonic acid for the treatment of bone metastases: Comparison with Tc-99m-DPD complex
Апстракт
The goal of this investigation was to examine the possibilities for yttrium-90-labeling of the 2,3-dicarboxypropane-1,1-diphosphonic acid (DPD), which is currently labeled with technetium-99m and as a Tc-99m-DPD clinically used as bone imaging agent. Analysis of the complex enclosed the radiochemical quality control methods, biodistribution studies, as well as the determination of pharmacokinetic parameters. The biological behavior of complexes Y-90-DPD, Tc-99m-DPD and Y-90-labeled DPD-kit formulation [Y-90-(Sn)-DPD] in animal model was compared. The labeling conditions were standardized to give the maximum yield, which ranged between 93% and 98%. The examined Y-90 complex could be easily prepared, with an outstanding yield and was also found to be very stable for at least 10 h after Y-90-labeling. Protein binding value was 4.6 +/- 0.7% for Y-90-DPD complex and the complex possess a hydrophilic character. The satisfactory results of Y-90- DPD biodistribution in healthy test animals wer...e obtained; the uptake in the bone was 11-13% ID/g after 24 h depending on the pH value during the preparation. With high skeletal uptake, a minimum uptake in soft tissues and rapid blood clearance the Y-90-DPD complex proved to be an excellent candidate for targeting tumor therapy. (C) 2008 Elsevier Ltd. All rights reserved.
Кључне речи:
phosphonates / DPD / Y-90-radiolabeling / targeted tumor therapyИзвор:
Bioorganic and Medicinal Chemistry, 2008, 16, 8, 4457-4465
DOI: 10.1016/j.bmc.2008.02.062
ISSN: 0968-0896
PubMed: 18331797
WoS: 000255246100024
Scopus: 2-s2.0-42349099555
Колекције
Институција/група
VinčaTY - JOUR AU - Đokić, Divna Đ. AU - Janković, Drina AU - Nikolić, Nadežda S. PY - 2008 UR - https://vinar.vin.bg.ac.rs/handle/123456789/3240 AB - The goal of this investigation was to examine the possibilities for yttrium-90-labeling of the 2,3-dicarboxypropane-1,1-diphosphonic acid (DPD), which is currently labeled with technetium-99m and as a Tc-99m-DPD clinically used as bone imaging agent. Analysis of the complex enclosed the radiochemical quality control methods, biodistribution studies, as well as the determination of pharmacokinetic parameters. The biological behavior of complexes Y-90-DPD, Tc-99m-DPD and Y-90-labeled DPD-kit formulation [Y-90-(Sn)-DPD] in animal model was compared. The labeling conditions were standardized to give the maximum yield, which ranged between 93% and 98%. The examined Y-90 complex could be easily prepared, with an outstanding yield and was also found to be very stable for at least 10 h after Y-90-labeling. Protein binding value was 4.6 +/- 0.7% for Y-90-DPD complex and the complex possess a hydrophilic character. The satisfactory results of Y-90- DPD biodistribution in healthy test animals were obtained; the uptake in the bone was 11-13% ID/g after 24 h depending on the pH value during the preparation. With high skeletal uptake, a minimum uptake in soft tissues and rapid blood clearance the Y-90-DPD complex proved to be an excellent candidate for targeting tumor therapy. (C) 2008 Elsevier Ltd. All rights reserved. T2 - Bioorganic and Medicinal Chemistry T1 - Labeling, characterization, and in vivo localization of a new Y-90-based phosphonate chelate 2,3-dicarboxypropane-1,1-diphosphonic acid for the treatment of bone metastases: Comparison with Tc-99m-DPD complex VL - 16 IS - 8 SP - 4457 EP - 4465 DO - 10.1016/j.bmc.2008.02.062 ER -
@article{ author = "Đokić, Divna Đ. and Janković, Drina and Nikolić, Nadežda S.", year = "2008", abstract = "The goal of this investigation was to examine the possibilities for yttrium-90-labeling of the 2,3-dicarboxypropane-1,1-diphosphonic acid (DPD), which is currently labeled with technetium-99m and as a Tc-99m-DPD clinically used as bone imaging agent. Analysis of the complex enclosed the radiochemical quality control methods, biodistribution studies, as well as the determination of pharmacokinetic parameters. The biological behavior of complexes Y-90-DPD, Tc-99m-DPD and Y-90-labeled DPD-kit formulation [Y-90-(Sn)-DPD] in animal model was compared. The labeling conditions were standardized to give the maximum yield, which ranged between 93% and 98%. The examined Y-90 complex could be easily prepared, with an outstanding yield and was also found to be very stable for at least 10 h after Y-90-labeling. Protein binding value was 4.6 +/- 0.7% for Y-90-DPD complex and the complex possess a hydrophilic character. The satisfactory results of Y-90- DPD biodistribution in healthy test animals were obtained; the uptake in the bone was 11-13% ID/g after 24 h depending on the pH value during the preparation. With high skeletal uptake, a minimum uptake in soft tissues and rapid blood clearance the Y-90-DPD complex proved to be an excellent candidate for targeting tumor therapy. (C) 2008 Elsevier Ltd. All rights reserved.", journal = "Bioorganic and Medicinal Chemistry", title = "Labeling, characterization, and in vivo localization of a new Y-90-based phosphonate chelate 2,3-dicarboxypropane-1,1-diphosphonic acid for the treatment of bone metastases: Comparison with Tc-99m-DPD complex", volume = "16", number = "8", pages = "4457-4465", doi = "10.1016/j.bmc.2008.02.062" }
Đokić, D. Đ., Janković, D.,& Nikolić, N. S.. (2008). Labeling, characterization, and in vivo localization of a new Y-90-based phosphonate chelate 2,3-dicarboxypropane-1,1-diphosphonic acid for the treatment of bone metastases: Comparison with Tc-99m-DPD complex. in Bioorganic and Medicinal Chemistry, 16(8), 4457-4465. https://doi.org/10.1016/j.bmc.2008.02.062
Đokić DĐ, Janković D, Nikolić NS. Labeling, characterization, and in vivo localization of a new Y-90-based phosphonate chelate 2,3-dicarboxypropane-1,1-diphosphonic acid for the treatment of bone metastases: Comparison with Tc-99m-DPD complex. in Bioorganic and Medicinal Chemistry. 2008;16(8):4457-4465. doi:10.1016/j.bmc.2008.02.062 .
Đokić, Divna Đ., Janković, Drina, Nikolić, Nadežda S., "Labeling, characterization, and in vivo localization of a new Y-90-based phosphonate chelate 2,3-dicarboxypropane-1,1-diphosphonic acid for the treatment of bone metastases: Comparison with Tc-99m-DPD complex" in Bioorganic and Medicinal Chemistry, 16, no. 8 (2008):4457-4465, https://doi.org/10.1016/j.bmc.2008.02.062 . .