99mTc‐tricarbonyl labeling of paclitaxel as an antimicrotubule agent and its evaluation in B16‐F10 melanoma tumor‐bearing mice. (26th October 2016)

• Record Type: Journal Article
• Authors: Erfani, Mostafa; Shabani, Zahra; Shamsaei, Mojtaba; Shirmardi, Seyed Pezhman; Shafiei, Mohammad
• Is Part Of: Journal of labelled compounds & radiopharmaceuticals. Volume 59:Number 13(2016)
• Page Start: 582
• Page End: 588
• Publication Date: 2016-10-26
• Subjects: 99mTc(CO)3 core -- imaging -- labeling -- melanoma tumor -- paclitaxel; Tracers (Chemistry) -- Periodicals; Radiopharmaceuticals -- Periodicals; 615.8424
• DOI: 10.1002/jlcr.3468
• Languages: English
• ISSNs: 0362-4803

Abstract

Abstract : In the present study paclitaxel (taxol) was labeled with [ 99m Tc(CO)3 (H2 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 (H2 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. Abstract : Paclitaxel (taxol) was labeled with [ 99m Tc(CO)3 (H2 O)3 ] + core. [ 99m Tc(CO)3 (H2 O)3 ] + ‐paclitaxel complex with high specific activity (0.77 GBq/µmol), and labeling yield (96.8 ± 1.3) was obtained. Our main achievement was high accumulation of radiolabeled paclitaxel in tumor (4.51 ± 0.65 percentage injected dose per gram (% ID/g) at 2‐hour postinjection) followed by significant reduction (1.86 ± 0.27% ID/g) at 4‐hour postinjection.