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99m Tc‐tricarbonyl labeling of paclitaxel as an antimicrotubule agent and its evaluation in B16‐F10 melanoma tumor‐bearing mice
Author(s) -
Erfani Mostafa,
Shabani Zahra,
Shamsaei Mojtaba,
Shirmardi Seyed Pezhman,
Shafiei Mohammad
Publication year - 2016
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3468
Subject(s) - paclitaxel , chemistry , melanoma , high performance liquid chromatography , technetium , thin layer chromatography , radiochemistry , chromatography , cancer research , nuclear chemistry , chemotherapy , medicine , biology
In the present study paclitaxel (taxol) was labeled with [ 99m Tc(CO) 3 (H 2 O) 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 [ 99m Tc(CO) 3 (H 2 O) 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, 99m Tc‐tricarbonyl‐paclitaxel imaging would be useful for tumor characterization rather than tumor detection.