Technetium-99m radiolabeled paclitaxel as an imaging probe for breast cancer in vivo

Publication date: May 2017
Source:Biomedicine & Pharmacotherapy, Volume 89
Author(s): Liziane O.F. Monteiro, Renata S. Fernandes, Luciano C. Castro, Valbert N. Cardoso, Mônica C. Oliveira, Danyelle M. Townsend, Alice Ferretti, Domenico Rubello, Elaine A. Leite, André L.B. de Barros
The high incidence and mortality of breast cancer supports efforts to develop innovative imaging probes to effectively diagnose, evaluate the extent of the tumor, and predict the efficacy of tumor treatments while concurrently and selectively delivering anticancer agents to the cancer tissue. In the present study we described the preparation of technetium–99m (^99mTc)-labeled paclitaxel (PTX) and evaluated its feasibility as a radiotracer for breast tumors (4T1) in BALB/c mice. Thin Layer Chromatography (TLC) was used to determine the radiochemical purity and in vitro stability of ^99mTc-PTX. PTX micelles showed a unimodal distribution with mean diameter of 13.46±0.06nm. High radiochemical purity (95.8±0.3%) and in vitro stability (over than 95%), up to 24h, were observed. Blood circulation time of ^99mTc-PTX was determined in healthy BALB/c mice. ^99mTc-PTX decays in a one-phase manner with a half-life of 464.3 minutes. Scintigraphic images and biodistribution were evaluated at 4, 8 and 24h after administration of ^99mTc-PTX in 4T1 tumor-bearing mice. The data showed a significant uptake in the liver, spleen and kidneys, due to the importance of these routes for excretion. Moreover, high tumor uptake was achieved, indicated by high tumor-to-muscle ratios. These findings indicate the usefulness of ^99mTc-PTX as a radiotracer to identify 4T1 tumor in animal models. In addition, ^99mTc-PTX might be used to follow-up treatment protocols in research, being able to provide information about tumor progression after therapy.



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