Two arene
ruthenium porphyrin compounds showing interesting photodynamic activity in vitro, [Ru(η(6)-p-Pr(i)C(6)H(4)Me)(PMP)Cl(2)] (PMP=5-(3-pyridyl)-10,15,20-triphenylporphyrin) and [Ru(4)(η(6)-p-Pr(i)C(6)H(4)Me)(4)(PTP)Cl8] (PTP=5,10,15,20-tetra(3-pyridyl)
porphyrin) coined Rut1 and Rut4 respectively, have been evaluated in vivo.
Porphyrins alone and the arene
ruthenium porphyrin derivatives (Rut1 and Rut4) showed comparable spectroscopic and photophysical properties. The in vivo study consisted in selecting the optimal arene
ruthenium porphyrin photosensitizer by using an original experimental design approach on mice bearing an ectopic human oral
carcinoma xenograft. The model of experimental design demonstrated to be well suited to the empirical model-building of
photodynamic therapy (
PDT) response. Arene
ruthenium porphyrins concentration and fluence level demonstrated no statistically significant influence on the
tumor growth. On the contrary, the presence of
ruthenium groups improved the in vivo photodynamic efficiency. By
optical fiber fluorimetry, we demonstrated that both compounds exhibited enhanced accumulation in KB
tumors from 24h to 96 h post-
intravenous injection. These experiments were completed by inductively coupled plasma mass spectrometry quantification of
ruthenium in different organs including
tumor tissue. Despite a statistically significant in vivo photodynamic efficiency for Rut4, cellular localization in human oral
carcinoma KB cells using fluorescence microscopy demonstrated that both conjugates Rut1 and Rut4 accumulated only in cytoplasm of KB cells but not in the nucleus.