Targeted multifunctional tannic acid nanoparticles

Tannic acid (TA) has multiple effects against cancer, being especially promising in those types that overexpress the epidermal growth factor receptor (EGFR), as TA modulates its activation and downstream signaling pathways, triggering apoptosis. Nonetheless, despite the important role of this receptor in the pathogenesis and progression of a wide variety of tumors, no TA systems targeted to this receptor have been described yet. In this work, we synthesize, characterize by physico-chemical techniques and study the cytotoxic effect and cell uptake of TA nanoparticles targeted to EGFR in both tumoral and normal human skin cells. Our nanoparticles exhibited an extremely high entrapment efficiency, and were only toxic for the tumoral cells. The uptake assay demonstrated that nanoparticles are able to enter the cells through a receptor-mediated mechanism. Furthermore, we have included fluorescent markers in these nanoparticles to combine imaging and therapeutic applications, thus building effectively a multifunctional tool for biomedicine.This work was supported by Junta de Andalucía (Proyecto de Investigación de Excelencia P10-FQM-6615 and PAIDI FQM319), Fondo Europeo de Desarrollo Regional (FEDER-Unión Europea) and Ministerio de Economía y Competitividad, Gobierno de España (Proyecto de Excelencia CTQ2013-48396-P). José M. Oliva-Montero is grateful to the Junta de Andalucía (P10-FQM-06615) for his pre-doctoral fellowship.Peer Reviewe