99mTc‐tricarbonyl labeling of paclitaxel as an antimicrotubule agent and its evaluation in B16‐F10 melanoma tumor‐bearing mice |
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| Authors: | Mostafa Erfani Zahra Shabani Mojtaba Shamsaei Seyed Pezhman Shirmardi Mohammad Shafiei |
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| Affiliation: | 1. Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran;2. Faculty of Nuclear engineering and Physics, Amirkabir University of Technology, Tehran, Iran |
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| Abstract: | In the present study paclitaxel (taxol) was labeled with [99mTc(CO)3(H2O)3]+ core. Labeling was optimized, and radiochemical analysis was determined by thin layer chromatography and high performance liquid chromatography. Radiocomplex was evaluated and verified further as a tumor characterization agent in B16‐F10 melanoma tumor‐bearing mice. The [99mTc(CO)3(H2O)3]+‐paclitaxel complex with high specific activity (0.77 GBq/μmol) and labeling yield (96.8 ± 1.3) was obtained. No decrease in labeling was observed up to 6 hours, and the stability of the radiocomplex was found adequate. Our main achievement was high accumulation of radiolabeled paclitaxel in tumor (4.51 ± 0.65 percentage injected dose per gram [%ID/g] at 2‐h postinjection) followed by significant reduction (1.86 ± 0.27%ID/g) at 4‐hour postinjection. Because paclitaxel is a substrate for multidrug resistance, 99mTc‐tricarbonyl‐paclitaxel imaging would be useful for tumor characterization rather than tumor detection. |
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| Keywords: | 99mTc(CO)3 core imaging labeling melanoma tumor paclitaxel |
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