Labeling and evaluation of 99mTc‐tricarbonyl‐meloxicam as a preferential COX‐2 inhibitor for inflammation imaging. (8th April 2016)

• Record Type: Journal Article
• Authors: Erfani, Mostafa; Sharifzadeh, Somayeh; Doroudi, Alireza; Shafiei, Mohammad
• Is Part Of: Journal of labelled compounds & radiopharmaceuticals. Volume 59:Number 7(2016)
• Page Start: 284
• Page End: 290
• Publication Date: 2016-04-08
• Subjects: inflammation -- 99mTc‐tricarbonyl -- Meloxicam -- imaging; Tracers (Chemistry) -- Periodicals; Radiopharmaceuticals -- Periodicals; 615.8424
• DOI: 10.1002/jlcr.3396
• Languages: English
• ISSNs: 0362-4803

Abstract

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 anonsteroidal 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. Abstract : 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. High accumulation of 99m Tc‐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.