Technetium-99m labeled Ibuprofen: Development and biological evaluation using sterile inflammation induced animal models
In this study we are presenting the development of technetium-99m ( 99m Tc) labeled ibuprofen for the imaging of aseptic inflammation. 99m Tc-Ibuprofen complex was developed by optimizing the radiolabeling conditions such as reaction time, ligand and reducing agent concentration, pH, reaction time a...
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Published in | Molecular biology reports Vol. 46; no. 3; pp. 3093 - 3100 |
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Main Authors | , , , , |
Format | Journal Article |
Language | English |
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Springer Netherlands
01.06.2019
Springer Nature B.V |
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Abstract | In this study we are presenting the development of technetium-99m (
99m
Tc) labeled ibuprofen for the imaging of aseptic inflammation.
99m
Tc-Ibuprofen complex was developed by optimizing the radiolabeling conditions such as reaction time, ligand and reducing agent concentration, pH, reaction time and temperature. Following the addition of 600 µg of ibuprofen, 4 µg of stannous chloride as reducing agent and 300 MBq
99m
Tc radioactivity; the pH of reaction mixture was adjusted to 11 and allowed to react for 15 min at room temperature. Chromatography analysis revealed > 94%
99m
Tc-ibuprofen complex formation with promising stability in saline and blood serum up to 6 h. Biodistribution study using normal and sterile inflammation induced mice indicated low accumulation of labeled compound in key body organs; however, kidneys (14.76 ± 0.87% ID/g organ) and bladder (31.6 ± 3.0% ID/g organ) showed comparatively higher radioactivity due to main excretory path. Inflamed to normal tissues ratio (T/NT), at 1 h post-injection, showed promising value (4.57 ± 0.56). The SPECT imaging of artificially inflammation induced rabbit model also verified the biodistribution results. In conclusion, radiochemical purity and biological evaluation of
99m
Tc-ibuprofen complex indicates the agent can be utilized for imaging of deep seated aseptic inflammation. |
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AbstractList | In this study we are presenting the development of technetium-99m (99mTc) labeled ibuprofen for the imaging of aseptic inflammation. 99mTc-Ibuprofen complex was developed by optimizing the radiolabeling conditions such as reaction time, ligand and reducing agent concentration, pH, reaction time and temperature. Following the addition of 600 µg of ibuprofen, 4 µg of stannous chloride as reducing agent and 300 MBq 99mTc radioactivity; the pH of reaction mixture was adjusted to 11 and allowed to react for 15 min at room temperature. Chromatography analysis revealed > 94% 99mTc-ibuprofen complex formation with promising stability in saline and blood serum up to 6 h. Biodistribution study using normal and sterile inflammation induced mice indicated low accumulation of labeled compound in key body organs; however, kidneys (14.76 ± 0.87% ID/g organ) and bladder (31.6 ± 3.0% ID/g organ) showed comparatively higher radioactivity due to main excretory path. Inflamed to normal tissues ratio (T/NT), at 1 h post-injection, showed promising value (4.57 ± 0.56). The SPECT imaging of artificially inflammation induced rabbit model also verified the biodistribution results. In conclusion, radiochemical purity and biological evaluation of 99mTc-ibuprofen complex indicates the agent can be utilized for imaging of deep seated aseptic inflammation. In this study we are presenting the development of technetium-99m ( 99m Tc) labeled ibuprofen for the imaging of aseptic inflammation. 99m Tc-Ibuprofen complex was developed by optimizing the radiolabeling conditions such as reaction time, ligand and reducing agent concentration, pH, reaction time and temperature. Following the addition of 600 µg of ibuprofen, 4 µg of stannous chloride as reducing agent and 300 MBq 99m Tc radioactivity; the pH of reaction mixture was adjusted to 11 and allowed to react for 15 min at room temperature. Chromatography analysis revealed > 94% 99m Tc-ibuprofen complex formation with promising stability in saline and blood serum up to 6 h. Biodistribution study using normal and sterile inflammation induced mice indicated low accumulation of labeled compound in key body organs; however, kidneys (14.76 ± 0.87% ID/g organ) and bladder (31.6 ± 3.0% ID/g organ) showed comparatively higher radioactivity due to main excretory path. Inflamed to normal tissues ratio (T/NT), at 1 h post-injection, showed promising value (4.57 ± 0.56). The SPECT imaging of artificially inflammation induced rabbit model also verified the biodistribution results. In conclusion, radiochemical purity and biological evaluation of 99m Tc-ibuprofen complex indicates the agent can be utilized for imaging of deep seated aseptic inflammation. In this study we are presenting the development of technetium-99m ( Tc) labeled ibuprofen for the imaging of aseptic inflammation. Tc-Ibuprofen complex was developed by optimizing the radiolabeling conditions such as reaction time, ligand and reducing agent concentration, pH, reaction time and temperature. Following the addition of 600 µg of ibuprofen, 4 µg of stannous chloride as reducing agent and 300 MBq Tc radioactivity; the pH of reaction mixture was adjusted to 11 and allowed to react for 15 min at room temperature. Chromatography analysis revealed > 94% Tc-ibuprofen complex formation with promising stability in saline and blood serum up to 6 h. Biodistribution study using normal and sterile inflammation induced mice indicated low accumulation of labeled compound in key body organs; however, kidneys (14.76 ± 0.87% ID/g organ) and bladder (31.6 ± 3.0% ID/g organ) showed comparatively higher radioactivity due to main excretory path. Inflamed to normal tissues ratio (T/NT), at 1 h post-injection, showed promising value (4.57 ± 0.56). The SPECT imaging of artificially inflammation induced rabbit model also verified the biodistribution results. In conclusion, radiochemical purity and biological evaluation of Tc-ibuprofen complex indicates the agent can be utilized for imaging of deep seated aseptic inflammation. |
Author | Khan, Naeem-Ul-Haq Roohi, Samina Naqvi, Syed Ali Raza Sohail, Hamza Jamal, Muhammad Asghar |
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CitedBy_id | crossref_primary_10_1080_03639045_2020_1776316 crossref_primary_10_1016_j_apradiso_2023_110856 crossref_primary_10_1080_03639045_2023_2235009 crossref_primary_10_1177_02841851241249161 crossref_primary_10_1021_acsomega_9b04327 |
Cites_doi | 10.1097/00006231-200207000-00010 10.1016/S0969-8051(97)00118-2 10.1590/S1516-89132002000500005 10.1007/s002590050036 10.1016/j.ica.2011.01.060 10.1136/jcp.55.11.817 10.1136/gut.47.3.320 10.1097/00006231-199711000-00009 10.1039/C7DT01189J 10.2967/jnmt.110.085498 10.1097/00006231-199705000-00009 10.1007/s12149-010-0417-3 10.1002/jlcr.3380 10.1007/s11033-018-4220-x 10.1016/j.bmc.2008.09.050 10.1002/jlcr.3494 10.1093/cid/civ286 10.2174/138955712802762112 10.5001/omj.2010.49 |
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Keywords | Nuclear medicine Radiopharmaceuticals Tc-Ibuprofen Infection imaging Ibuprofen 99mTc-Ibuprofen |
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Snippet | In this study we are presenting the development of technetium-99m (
99m
Tc) labeled ibuprofen for the imaging of aseptic inflammation.
99m
Tc-Ibuprofen complex... In this study we are presenting the development of technetium-99m ( Tc) labeled ibuprofen for the imaging of aseptic inflammation. Tc-Ibuprofen complex was... In this study we are presenting the development of technetium-99m (99mTc) labeled ibuprofen for the imaging of aseptic inflammation. 99mTc-Ibuprofen complex... |
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SubjectTerms | Animal Anatomy Animal Biochemistry Animal models Animals Biomedical and Life Sciences Chromatography Drug Stability Histology Humans Hydrogen-Ion Concentration Ibuprofen Ibuprofen - administration & dosage Ibuprofen - chemistry Ibuprofen - pharmacokinetics Inflammation Isotope Labeling Kidneys Life Sciences Ligands Models, Animal Molecular Structure Morphology Nonsteroidal anti-inflammatory drugs Original Article pH effects Radioactivity Radionuclide Imaging - methods Radiopharmaceuticals - administration & dosage Radiopharmaceuticals - chemistry Radiopharmaceuticals - pharmacokinetics Rats Single photon emission computed tomography Stannous chloride Technetium Tissue Distribution Tomography, Emission-Computed, Single-Photon |
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Title | Technetium-99m labeled Ibuprofen: Development and biological evaluation using sterile inflammation induced animal models |
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