Labeling and evaluation of (99m) Tc-tricarbonyl-meloxicam as a preferential COX-2 inhibitor for inflammation imaging.

Abstract

Imaging of inflammation has an important role in dissolving problems in diagnosis and therapy of patients with inflammatory disorders. In this study meloxican as a nonsteroidal anti-inflammatory drug (NSAID) has been labeled with thechnetium-99m-tricarbonyl core ([(99m) Tc (CO)3 (H2 O)3 ](+) ) in order to evaluate its feasibility as an inflammation imaging agent for in vivo use. (99m) Tc-tricabonyl labeling of meloxicam was performed by its incubation with prepared precursor (99m) Tc-tricabonyl and heating in a boiling water bath for 30 min while various range of pH (1-9) was adjusted. The stability of (99m) Tc-tricarbonyl-Meloxicam was checked in human serum at 37 °C, and biodistribution was studied in mice. Labeling yield of 98.1 ± 0.4% was obtained corresponding to a specific activity of 0.14 GBq/µmol. The radioconjugate showed good stability in human serum. Our main achievement was high accumulation of (99m) Tc-tricarbonyl-Meloxicam in the inflammated muscle in mice (T/NT = 3.90 at 4 h post injection) which may diagnostically be beneficial for distinguish sites of inflammation.

• Authors: Mostafa Erfani, Somayeh Sharifzadeh, Alireza Doroudi, Mohammad Shafiei
• Journal: Journal of labelled compounds & radiopharmaceuticals (J Labelled Comp Radiopharm) Vol. 59 Issue 7 Pg. 284-90 (06 15 2016) ISSN: 1099-1344 [Electronic] England
• PMID: 27061432 (Publication Type: Journal Article)
• Copyright: Copyright © 2016 John Wiley & Sons, Ltd.

Chemical References

• Cyclooxygenase 2 Inhibitors
• Organotechnetium Compounds
• Thiazines
• Thiazoles
• technetium 99m tricarbonyl-meloxicam
• Meloxicam

Topics

• Animals
• Biological Transport
• Cyclooxygenase 2 Inhibitors (chemistry, metabolism, pharmacokinetics)
• Humans
• Inflammation (diagnostic imaging)
• Isotope Labeling
• Meloxicam
• Mice
• Muscles (diagnostic imaging)
• Organotechnetium Compounds (chemistry)
• Radionuclide Imaging (methods)
• Thiazines (chemistry, metabolism, pharmacokinetics)
• Thiazoles (chemistry, metabolism, pharmacokinetics)
• Tissue Distribution