Chlorin and bacteriochlorin derivatives are at present the most promising compounds used in photodynamic therapy. However, the use of these photosensitizers (PSs) in clinical practice is limited because of their low solubility in biological fluids. A water-soluble dipropoxybacteriopurpurinimide (DPBI) conjugate with Pluronic F-127 was synthesized in the present work. It was shown that conjugation with the poloxamer did not affect the physicochemical and photophysical properties of the starting PS. It was found during biological tests that the resulting conjugate had photodynamic and pharmacokinetic properties similar to those of the original DPBI pigment. The advantages of the proposed PS were demonstrated in an acute toxicity study. Intravenous administration of the PS at 10 times the therapeutic dose did not cause the death of test animals, in contrast to a DPBI emulsion in water.
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Acknowledgments
The article was prepared in the framework of the project Radiopharmaceuticals during a development program at RTU MIREA for strategic academic leadership Priority-2030 and with support of the Ministry of Science and Higher Education of the RF (No. 0706-2020-0019). Equipment at the RTU MIREA Common Use Center was used during the work (Contract No. 075-15-2021-689 of Sept. 1, 2021; unique identification No. 2296.61321X0010).
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 56, No. 6, pp. 10 – 16, June, 2022.
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Suvorov, N.V., Sapel’nikov, M.D., Plotnikova, E.A. et al. New Water-Soluble IR Photosensitizer in the Bacteriochlorophyll a Series. Pharm Chem J 56, 736–741 (2022). https://doi.org/10.1007/s11094-022-02703-1
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DOI: https://doi.org/10.1007/s11094-022-02703-1