Near Infrared Activation of Pt(IV) Anticancer Agents by Upconverting Nanoparticles
Luca Salassa a, Emmanuel Ruggiero a, Juan C. Mareque-Rivas a b
a CIC biomaGUNE, Paseo Miramon 182, Donostia, 20009, Spain
b IKERBASQUE, Basque Foundation for Science, Bilbao, 48011, Spain
Poster, Emmanuel Ruggiero, 004
Publication date: 10th April 2014

Photodynamic therapy (PDT) is emerging in the clinics as an alternative therapeutic protocol to traditional cancer treatments. PDT kills cancer cells by generating reactive species upon light excitation of a prodrug (i.e. photosensitizer). Light activation allows to control spatially and temporally the effects of the treatment, decreasing systemic toxicity of anticancer agents and limiting unwanted side effects [1].

On the bases of the success of Pt(II) and Pt(IV) anticancer agents, several photoactivatable Pt(IV) anticancer agents have been developed for PDT in the last few years. However, such photoactive systems all suffer from the need of high-energy UV or visible light for activation [2], which is not ideal for in vivo applications since low tissue penetration is achieved at such wavelengths and cellular damage can be induced.

Coupling photoactivatable anticancer complexes with upconverting nanoparticles (UCNPs) is a promising strategy to overcome such challenging limitation. UCNPs can convert NIR light into UV-visible light, meeting metal complexes' demand for high-energy light excitation. Recently, we have demonstrated the photoactivation of Ru polypyridyls by UCNPs [3] and we are currently extending the strategy to light-sensitive Pt(IV) anticancer complexes.

In this contribution we will discuss our advances in the design of hybrid systems which combine biocompatible UCNPs with Pt(IV) prodrugs. Our efforts are ultimately aimed at developping theranostic nanoplatforms that are capable of releasing cytotoxic platinum species under NIR activation and that allow visualization via multimodal imaging methods.

[1] Garaikoetxea Arguinzoniz, A.; Ruggiero, E.; Habtemarian, A.; Hernández-Gil, J.; Salassa, L.; Mareque-Rivas, J. C. Part. Part. Syst. Charact., 2014, 1, 46.

[2] Farrer, N. J.; Salassa, L.; Sadler, P. J. Dalton Trans., 2009, 10690.

[3] Ruggiero, E.; Habtemariam, A.; Yate, L.; Mareque-Rivas, J. C.; Salassa, L. Chem. Commun., 2014, 50, 1715.

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