Labeling and evaluation of 99mTc-tricarbonyl-meloxicam as a preferential COX-2 inhibitor for inflammation imaging

• Published in: Journal of labelled compounds & radiopharmaceuticals Vol. 59; no. 7; pp. 284 - 290
• Main Authors: Erfani, Mostafa, Sharifzadeh, Somayeh, Doroudi, Alireza, Shafiei, Mohammad
• Format: Journal Article
• Language: English
• Published: Bognor Regis Blackwell Publishing Ltd 15.06.2016; Wiley Subscription Services, Inc
• Subjects: 99mTc-tricarbonyl; imaging; inflammation; Meloxicam
• ISSN: 0362-4803; 1099-1344
• DOI: 10.1002/jlcr.3396

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 ([99mTc (CO)3 (H2O)3]+) in order to evaluate its feasibility as an inflammation imaging agent for in vivo use. 99mTc‐tricabonyl labeling of meloxicam was performed by its incubation with prepared precursor 99mTc‐tricabonyl and heating in a boiling water bath for 30 min while various range of pH (1–9) was adjusted. The stability of 99mTc‐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 99mTc‐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. Meloxican as a nonsteroidal anti‐inflammatory drug (NSAID) has been labeled with thechnetium‐99m‐tricarbonyl core ([99mTc (CO)3 (H2O)3]+) in order to evaluate its feasibility as an inflammation imaging agent for in vivo use. High accumulation of 99mTc‐tricarbonyl‐Meloxicam in the inflamated muscle in mice (T/NT = 3.90 at 4 h post injection) was observed which may diagnostically be beneficial for distinguish sites of inflammation.