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Radiolabeled block copolymer micelles for image-guided drug delivery

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Summary:We aimed at exploring block copolymer micelles (BCMs) for the simultaneous delivery of radiation/chemotherapy to cancer cells. To achieve that goal, we have prepared and characterized a novel type of docetaxel (DTX) loaded and non-loaded BCMs. The micelles were decorated with pyrazolyl-diamine chelating units to stabilize the matched pair 99mTc/Re for image-guided delivery of therapeutic drugs. The in vitro studies have shown that DTX release is pH-dependent increasing at lower pH values. Anti-proliferative studies in different cancer cell lines showed that DTX-loaded BCMs present relevant anti-proliferative activity. In comparison to free DTX, the loaded-micelles exhibited higher anti-proliferative activity for the same DTX concentration, which mean that a similar therapeutic outcome may be achieved with reduced side effects. The pyrazolyl-diamine-functionalized micelles were labeled with fac-[99mTc(CO)3(H2O)3]+ in high radiochemical yield and purity. The radiolabeled micelles are stable in phosphate buffer and in cell culture media. Cellular uptake studies in different cancer cell lines indicate a cell type and time-dependent uptake, in agreement with the anti-proliferative activity. Early biodistribution studies in healthy BALB/c mice has shown prolonged circulation lifetime in the bloodstream and relevant in vivo stability, important features when considering an effective DTX delivery system and image-guided delivery agent for cancer theranostics.
Main Authors:Ribeiro, Elisabete
Other Authors:Alho, Irina; Marques, Fernanda; Gano, Lurdes; Correia, Isabel; Correia, João D. G.; Casimiro, Sandra; Costa, Luis; Santos, Isabel Cordeiro; Fernandes, Célia
Subject:(99m)Tc Block copolymer micelle Drug delivery system PEG-b-PCL Radiolabeled micelles
Year:2016
Country:Portugal
Document type:article
Access type:restricted access
Associated institution:Universidade de Lisboa
Language:English
Origin:Repositório da Universidade de Lisboa

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