title: 99mTc-tricarbonyl labeling of paclitaxel as an antimicrotubule agent and its evaluation in B16-F10 melanoma tumor-bearing mice.
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.
authors: Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran.
authors: Mostafa
authors: M
authors: Erfani
authors: Faculty of Nuclear engineering and Physics, Amirkabir University of Technology, Tehran, Iran.
authors: Zahra
authors: Z
authors: Shabani
authors: Faculty of Nuclear engineering and Physics, Amirkabir University of Technology, Tehran, Iran.
authors: Mojtaba
authors: M
authors: Shamsaei
authors: Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran.
authors: Seyed Pezhman
authors: SP
authors: Shirmardi
authors: Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran.
authors: Mohammad
authors: M
authors: Shafiei
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D004355:Drug Stability; D006801:Humans; D007553:Isotope Labeling; D008546:Melanoma, Experimental / Q000188:drug therapy* / Q000473:pathology*; D051379:Mice; D008870:Microtubules / Q000187:drug effects* / Q000378:metabolism; D015609:Organotechnetium Compounds / Q000737:chemistry*; D017239:Paclitaxel / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D011854:Radiochemistry; D014018:Tissue Distribution
chemical_list: D015609:Organotechnetium Compounds; D017239:Paclitaxel
keywords: 99mTc(CO)3 core; imaging; labeling; melanoma tumor; paclitaxel