| Summary: | Michelle Alvares Sarcinelli,1,2 Marta de Souza Albernaz,3 Marzena Szwed,4 Alexandre Iscaife,2 Kátia Ramos Moreira Leite,2 Mara de Souza Junqueira,5 Emerson Soares Bernardes,6 Emerson Oliveira da Silva,1 Maria Ines Bruno Tavares,1 Ralph Santos-Oliveira7 1Instituto de Macromoléculas Professora Eloisa Mano Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil; 2Laboratory of Medical Investigation, Faculty of Medicine, São Paulo University, São Paulo, Brazil; 3Radiopharmacy Sector, University Hospital Clementino Fraga Filho, Rio de Janeiro, Brazil; 4Department of Thermobiology, Faculty of Biology and Environmental Protection, University of Lodz, Lodz, Poland; 5Laboratory of Experimental Oncology, Faculty of Medicine, São Paulo University, São Paulo, Brazil; 6Radiopharmacy Center, Instituto de Pesquisas Energéticas e Nucleares (IPEN), São Paulo, Brazil; 7Laboratory of Nanoradiopharmaceuticals, Zona Oeste State University, Rio de Janeiro, Brazil Abstract: Monoclonal antibodies as polymeric nanoparticles are quite interesting and endow this new drug category with many advantages, especially by reducing the number of adverse reactions and, in the case of radiopharmaceuticals, also reducing the amount of radiation (dose) administered to the patient. In this study, a nanoradiopharmaceutical was developed using polylactic acid (PLA)/polyvinyl alcohol (PVA)/montmorillonite (MMT)/trastuzumab nanoparticles labeled with technetium-99m (99mTc) for breast cancer imaging. In order to confirm the nanoparticle formation, atomic force microscopy and dynamic light scattering were performed. Cytotoxicity of the nanoparticle and biodistribution with 99mTc in healthy and inducted animals were also measured. The results from atomic force microscopy showed that the nanoparticles were spherical, with a size range of ~200–500 nm. The dynamic light scattering analysis demonstrated that over 90% of the nanoparticles produced had a size of 287 nm with a zeta potential of -14,6 mV. The cytotoxicity results demonstrated that the nanoparticles were capable of reaching breast cancer cells. The biodistribution data demonstrated that the PLA/PVA/MMT/trastuzumab nanoparticles labeled with 99mTc have great renal clearance and also a high uptake by the lesion, as ~45% of the PLA/PVA/MMT/trastuzumab nanoparticles injected were taken up by the lesion. The data support PLA/PVA/MMT/trastuzumab labeled with 99mTc nanoparticles as nanoradiopharmaceuticals for breast cancer imaging. Keywords: radiopharmaceuticals, nanotechnology, oncology, breast cancer, molecular imaging, nanomedicine, nuclear pharmacy
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