Biodistribution, pharmacokinetic, and in-vivo fluorescence spectroscopic studies of photosensitizers

Johan Moan; Qian Peng; Vladimir Iani; Li Wei Ma; Richard W. Horobin; Kristian Berg; Magne Kongshaug; Jahn M. Nesland

doi:10.1117/12.231008

31 January 1996 Biodistribution, pharmacokinetic, and in-vivo fluorescence spectroscopic studies of photosensitizers

Johan Moan, Qian Peng, Vladimir Iani, Li Wei Ma, Richard W. Horobin, Kristian Berg, Magne Kongshaug, Jahn M. Nesland

Proceedings Volume 2625, Photochemotherapy: Photodynamic Therapy and Other Modalities; (1996) https://doi.org/10.1117/12.231008
Event: BiOS Europe '95, 1995, Barcelona, Spain

Abstract

Some key data concerning the pharmacokinetics of PCT photosensitizers are reviewed. The following topics are discussed: The binding of photosensitizers to serum proteins, and the significance of LDL binding for tumor localization, the distribution of sensitizers among different tissue compartments and the significance of extracellular proteins and other stromal elements, such as macrophages, low tumor pH, leaky vasculature and poor lymphatic drainage for tumor selectivity of drugs, the retention and excretion of sensitizers, and intracellular pharmacokinetics. Furthermore, the usefulness of fluorescence measurements in the study of sensitizer pharmacokinetics is briefly discussed. A key observation is that ¹O₂ has a short radius of action. Since practically all PCT sensitizers act via the ¹O₂ pathway, only targets with significant sensitizer concentrations can be damaged. A given number of ¹O₂ entities generated in different organelles (mitochondria, lysosomes, plasma membrane, etc.) may lead to widely different effects with respect to cell inactivation. Similarly, sensitizers localizing in different compartments of tissues may have different photosensitizing efficiencies even under conditions of a similar ¹O₂ yield.

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Johan Moan, Qian Peng, Vladimir Iani, Li Wei Ma, Richard W. Horobin, Kristian Berg, Magne Kongshaug, and Jahn M. Nesland "Biodistribution, pharmacokinetic, and in-vivo fluorescence spectroscopic studies of photosensitizers", Proc. SPIE 2625, Photochemotherapy: Photodynamic Therapy and Other Modalities, (31 January 1996); https://doi.org/10.1117/12.231008

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