This is the peer-reviewed version of the following article: van de Winckel, E., Mascaraque, M., Zamarrón, A., Juarranz de la Fuente, Á., Torres, T., & de la Escosura, A. (2018).
Dual role of subphthalocyanine dyes for optical imaging and therapy of cancer. Advanced Functional Materials, 28(24), 1705938., which has been published in final form at https://doi.org/10.1002/adfm.201705938. This article may be used for non-commercial purposes in accordance with Wiley-VCH Terms and Conditions for Self-ArchivingThe family of subphthalocyanine (SubPc) macrocycles represents an interesting class of nonplanar aromatic dyes with promising features for energy conversion and optoelectronics. The use of SubPcs in biomedical research is, on the contrary, clearly underexplored, despite their documented high fluorescence and singlet oxygen quantum yields. Herein, for the first time it is shown that the interaction of these chromophores with light can also be useful for theranostic applications, which in the case of SubPcs comprise optical imaging and photodynamic therapy (PDT). In particular, the article evaluates, through a complete in vitro study, the dual-role capacity of a novel series of SubPcs as fluorescent probes and PDT agents, where the macrocycle axial substitution determines their biological activity. The 2D and 3D imaging of various cancer cell lines (i.e., HeLa, SCC-13, and A431) has revealed, for example, different subcellular localization of the studied photosensitizers (PS), depending on the axial substituent they bear. These results also show excellent photocytotoxicities, which are affected by the PS localization. With the best dual-role PS, preliminary in vivo studies have demonstrated their therapeutic potential. Overall, the present paper sets the bases for an unprecedented biomedical use of these well-known optoelectronic materials.E.v.d.W. and M.M. contributed equally to this work. The research leading to these results has received funding from the People Programme (Marie Curie Actions) of the European Union's Seventh Framework Program FP7‐PEOPLE‐2012‐ITN under REA grant agreement No. GA 316975. AdlE holds a Ramón y Cajal contract from the Spanish Ministry of Economy (MINECO). This work was supported by EU (CosmoPHOS‐nano, FP7‐NMP‐2012‐6, 310337‐2; GLOBASOL, FP7‐ENERGY‐2012‐J, 309194‐2), the Spanish MINECO (CTQ‐2014‐52869‐P (TT) and CTQ‐2014‐53673‐P (AdlE)), CAM (FOTOCARBON, S2013/MIT‐2841), grants from Instituto de Salud Carlos III, MINECO and Feder Funds (PI15/00974) and by S2010/BMD‐2359 from Comunidad de Madrid
