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Technetium-99m labeled Ibuprofen: Development and biological evaluation using sterile inflammation induced animal models

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Abstract

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.

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Acknowledgements

The study is a part of HEC funded Project No. 5612/Punjab/NRPU/R&D/HEC/2016, thanks to HEC, GCU Faisalabad, and PINSTECH Islamabad for providing resources and platform to conduct this research.

Funding

This study was funded by Higher Education Commission (HEC), Islamabad, Pakistan under Grant No. 5612/Punjab/NRPU/R&D/HEC/2016.

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Authors and Affiliations

  1. Department of Chemistry, Government College University Faisalabad, Faisalabad, 38000, Pakistan

    Naeem-Ul-Haq Khan, Syed Ali Raza Naqvi & Muhammad Asghar Jamal

  2. Islamabad Medical and Dental College, Murree Road, Islamabad, Pakistan

    Hamza Sohail

  3. Isotope Production Devision (IPD), Pakistan Institute of Nuclear Science and Technology (PINSTECH), Nilore, Islamabad, Pakistan

    Samina Roohi

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  1. Naeem-Ul-Haq Khan
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  2. Syed Ali Raza Naqvi
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  5. Muhammad Asghar Jamal
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Correspondence to Syed Ali Raza Naqvi or Samina Roohi.

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Khan, NUH., Naqvi, S.A.R., Sohail, H. et al. Technetium-99m labeled Ibuprofen: Development and biological evaluation using sterile inflammation induced animal models. Mol Biol Rep 46, 3093–3100 (2019). https://doi.org/10.1007/s11033-019-04762-2

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  • DOI: https://doi.org/10.1007/s11033-019-04762-2

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