Optimization of labeling conditions and bioevalution of 99m Tc-Meloxicam for inflammation imaging

Sanad, M. H.; Amin, A. M.

doi:10.1134/s1066362213050123

Cited by 36 publications

(9 citation statements)

References 15 publications

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“…In previous study Meloxicam was labeled with 99m Tc via direct labeling method and the in vivo behavior of the 99m Tc‐Meloxicam has been reported in intramuscularly inflamed mice . The ratio of T/NT activity which accumulated at the site of inflamed muscle compared to normal muscle was 5.10 at 4 h post injection while the uptake values for blood, liver and intestine were relatively high (13.10 ± 0.90, 13.00 ± 1.10 and 25.00 ± 1.40 %ID/g at 4 h post injection respectively).…”

Section: Resultsmentioning

confidence: 96%

“…However in this study as the evaluation of the ratios uptakes of inflamed muscle to normal muscle (T/NT) shows, one can conclude that the above radiocomplex has a specific binding affinity for inflammation regions; nevertheless, in order to assure that the interaction with COX-2 has not been lost or reduced because of radiocomplexation further study of in vitro binding of has been reported in intramuscularly inflamed mice. 20 The ratio of T/NT activity which accumulated at the site of inflamed muscle compared to normal muscle was 5.10 at 4 h post injection while the uptake values for blood, liver and intestine were relatively high (13.10 ± 0.90, 13.00 ± 1.10 and 25.00 ± 1.40 %ID/g at 4 h post injection respectively). Tc-tricarbonyl-Meloxicam were lower than that of for 99m Tc-Diclofenac (1.21 ± 0.27, 1.01 ± 0.08 and 5.26 ± 0.83 %ID/g at 1 h versus 20.2 ± 1.20, 16.8 ± 1.30 and 16.2 ± 1.30 %ID/g at 1 h post injection respectively).…”

Section: Resultsmentioning

confidence: 97%

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

Erfani

Sharifzadeh

Doroudi

et al. 2016

Labelled Comp Radiopharmac

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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.

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Section: Resultsmentioning

confidence: 96%

Section: Resultsmentioning

confidence: 97%

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

Erfani

Sharifzadeh

Doroudi

et al. 2016

Labelled Comp Radiopharmac

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“…Radioisotope imaging has a crucial role in the identification of infection from sterile infection lesions. Therefore, different radiopharmaceutical agents have been established or examined as potential detecting agents for infection ( 15 – 18 ) or sterile inflammation ( 19 , 20 ) in both preclinical and clinical investigations. An ideal radiopharmaceutical agent has the following characteristics to distinguish infection or inflammation lesions.…”

Section: Discussionmentioning

confidence: 99%

The sensitivity and specificity of 99mTc-IgG radiotracer to differentiate infection lesions induced by Staphylococcus aureus and sterile inflammation lesions induced by carrageenan assay in rat’s foot

et al. 2018

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BackgroundDetection and identification of infection from sterile inflammation foci has a crucial role in diagnosis and therapy of patients in clinical practice.ObjectiveTo assess the efficiency of labeled human polyclonal immunoglobulin with technetium 99m in order to detect septic or aseptic lesions which were induced in a rat model.MethodsThe freeze-dried IgG kits have been reconstituted by 99mTc. The radio conjugate yield, radiochemical impurities and stability radio complex were performed by ITLC (Instant Thin Layer Chromatography) and Gel filtration assays. Twenty adult, male NMRI (Naval Medical Research Institute) rats were randomly divided into two groups equally. Infection was induced by Staphylococcus aureus and sterile inflammation created by Carrageenan test. All lesions were created in the rat’s foot. Then radioisotope investigations were undertaken.ResultsLabeling yield was approximately 98%. The radio complex showed good stability in normal saline. All affected feet could be easily visualized by imaging in qualitative study. The value of target to non-target ratio at the infection (n=10) and sterile inflammation (n=10) were 2.81±0.16 and 1.54±0.15 with p<0.007. Therefore, the radiotracer uptake at the septic lesions was significantly higher than the aseptic lesions.ConclusionImaging with 99mTc-IgG is highly sensitive to localized infection or inflammation foci. The increased accumulation of radiotracer at the infection versus inflammation foci may be helpful to interpret the image.

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“…Trials were performed for each factor to obtain the optimum value. The experiment was repeated with all the factors kept at optimum values except the factor under study, until the overall optimum conditions were achieved [14][15][16].…”

Section: Animalsmentioning

confidence: 99%

Radiodiagnosis of peptic ulcer with technetium-99m labeled rabeprazole

Sanad

Ibrahim

2015

Radiochemistry

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Rabeprazole, antiulcer drug, was labeled with 99m Tc to obtain an agent for ulcer imaging. The radiochemical yield of 99m Tc-rabeprazole reaches approximately 98.5 ± 0.4%.The optimum conditions are as follows: pH 9, 50 μg of SnCl 2 ·2H 2 O, 30 min, and 3 mg of the substrate. 99m Tc-rabeprazole was stable for 6 h. Intravenous biodistribution studies of 99m Tc-rabeprazole revealed high concentration in the stomach ulcer, reaching about 33.4% of the total injected dose at 30 min post injection. This concentration of 99m Tc-rabeprazole in stomach ulcer makes this agent promising for stomach ulcer imaging.

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Optimization of labeling conditions and bioevalution of 99m Tc-Meloxicam for inflammation imaging

Cited by 36 publications

References 15 publications

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

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

The sensitivity and specificity of 99mTc-IgG radiotracer to differentiate infection lesions induced by Staphylococcus aureus and sterile inflammation lesions induced by carrageenan assay in rat’s foot

Radiodiagnosis of peptic ulcer with technetium-99m labeled rabeprazole

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Optimization of labeling conditions and bioevalution of 99m Tc-Meloxicam for inflammation imaging

Cited by 36 publications

References 15 publications

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

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

The sensitivity and specificity of 99mTc-IgG radiotracer to differentiate infection lesions induced by Staphylococcus aureus and sterile inflammation lesions induced by carrageenan assay in rat’s foot

Radiodiagnosis of peptic ulcer with technetium-99m labeled rabeprazole

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

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