In vivo evaluation of 99mTc-polymeric micelles probes loaded with 2-amino-7(8)-fluorophenazine N5,N10-dioxide as a potential target & delivery agent toward breast cancer tumors

LECOT N.; AFONSO J; FERNANDEZ LOMONACO M.; CABRERA M.; GAMBINI JP.; CERECETTO H.; GLISONI RJ.; GONZALEZ M.; CABRAL P.

Mar del Plata

Congreso; SAIC SAI SAFIS-NANOMED-ar 2018; 2018

SAIC-NANOMED-ar

Breast cancer is a solid tumor characterized by a high level of hypoxic areas which are difficult to treat. In order to these we have developed polymeric micelles (PMs) as a nanocarriers of bioreducible pro-drug 2-amino-7(8)-fluorophenazine N5,N10-dioxide (FNZ) which have the ability to detect and treat hypoxic tumoral tissues.To improve FNZ pharmaceutical properties, the encapsulation was studied using pristine polymeric micelles (PMs) and glycosylated derivatives as a strategy: (a) to increase the solubility, (b) to stabilize the aqueous formulation for intravenous application and (c) to have nanoscale sizes which are suitable for the enhanced permeability and retention (EPR) effect for cancer diagnosis and improved antitumor activity. On the other hand, in order to know the biodistribution behavior of PMs/FNZ systems we prepared different radio-probes. This work presents the physicochemical characterization and the in vivo evaluation of 99mTc-PMs/FNZ probes.The preliminary results indicate that all the systems under study (Free-FNZ, pristine PMs/FNZ and glycosylated PMs/FNZ) were stable in particle size and Z-potential after its re-suspension in ultrapure water. Finally, the in vivo studies using 99mTc-PMs/FNZ, revealed an enhanced circulation time and a good performance in models of mice bearing 4T1 tumor.