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In the present work the following silicon (IV) - phthalocyanines and -naphthalocyanines bearing methoxyethylene glycol or methoxypolyethylene glycol covalently bound at the silicon are investigated: SiPc[OCH2CH2OCH3]2 (SiPc1), SiNc[OCH2CH2OCH3]2 (SiNc), SiPc[(OCH2CH2)nOCH3] with n approximately 115 (SiPc2). The phototherapeutic effect was shown at Lewis lung carcinoma implanted in mice. SiPc2 is monomeric soluble in water whereas the other two compounds aggregated in this solvent. Therefore these compounds were dissolved monomer in in aqueous Cremophor solution before in vivo administration. Laser irradiation was applied 7 days after implantation and 24 h after drug administration at the following wavelength (eta) ext: 672 nm for SiPc1 and SiPc2, 782 nm for SiNc. In all cases a fluence rate of 370 mW/cm2 at fluence of 360 J/cm2 was used. The assessment criteria for the tumor response were the changes in the mean tumor diameter with time, regrowth delay and average survival time (AST). According to the first parameter the most promising result was obtained after treatment with SiPc1. For example the mean tumor diameter increases as follows: SiPc1 less than SiPc2 less than SiNc very much less than control group without photosensitizer. The regrowth delay showed the same trend. however, for AST another dependence was observed. AST was the longest for SiPc2 (26 days) and shortest for SiNc (22 days). Compared to the control group (without sensitizer and irradiation) the AST was 9 days longer after SiPc2 treatment. Comparing SiPc1 and SiPc2 the chain length of the substituents does not influence the phototherapeutic properties. The detected therapeutic results probably are connected with the long wavelength absorption of the photosensitizers. The relatively lower affectivity of SiNc may be due to a lower degree of tumor accumulation as it was observed in our preliminary pharmacokinetic studies. It is also possible that the shorter AST after treatment with SiNc is connected with a greater dark toxicity.
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