Jornal de Técnicas Analíticas e Bioanalíticas

Abstrato

Comparative Study of Tissue Distribution of Chlorin e6 Complexes with Amphiphilic Polymers in Mice with Cervical Carcinoma

Marina V Shirmanova, Alena I Gavrina, Nadeshda A Aksenova, Nikolay N Glagolev, Anna B Solovieva, Boris E Shakhov and Elena V Zagaynova

Many photosensitizers, including chlorins, are highly hydrophobic, which makes intravenous administration problematic and affects their delivery to the tumor and uptake in the cells. Moreover, self-aggregation of the photosensitizer in aqueous solution reduces fluorescence quantum yield, triplet state, and singlet oxygen generation, and consequently diminishes photosensitizing activity. To address these issues, it was proposed to use biocompatible water-soluble polymers. However, animal studies of the photosensitizer-polymer systems are still very limited. In this work, polyvinylpyrrolidone (PVP), polyvinyl alcohol (PVA), and pluronic F108 were used for dissolution of chlorin e6 (Ce6). Dynamics of accumulation of the formulations in a mouse cervical carcinoma and clearance from normal tissue, drug plasma concentrations and tissue distribution after intravenous injection were investigated. Ce6 alone and clinically used photosensitizer Photoditazine served as a control. The results showed that none of the polymers significantly changed fluorescence kinetics in the tumor. Concentration of the Ce6 formulated with polymers in the tumor tissue was comparable with Photoditazine, but uptake in the skin was less. At the same time, tumor-toskin ratios of the Ce6-polymer complexes were similar to free Ce6. We concluded that the use of the polymeric formulation is reasonable for fluorescence diagnosis and PDT of cancer.