Properties of the Novel Photosensitizer β,β,β′,β′-Tetramethyltribenzotetraazachlorin
The abilities of solubilizers Cremophor EL, Tween 80, Emuxol 3, and Pluronic F-68 to deliver the novel promising photosensitizer β,β,β′,β′-tetramethyltribenzotetraazachlorin (H 2 TBTAC) into A549 human lung adenocarcinoma cells in vitro were compared. It was found that the number of H 2 TBTAC monome...
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Published in | Pharmaceutical chemistry journal Vol. 48; no. 2; pp. 77 - 81 |
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Main Authors | , , , , |
Format | Journal Article |
Language | English |
Published |
Boston
Springer US
01.05.2014
Springer |
Subjects | |
Online Access | Get full text |
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Summary: | The abilities of solubilizers Cremophor EL, Tween 80, Emuxol 3, and Pluronic F-68 to deliver the novel promising photosensitizer β,β,β′,β′-tetramethyltribenzotetraazachlorin (H
2
TBTAC) into A549 human lung adenocarcinoma cells
in vitro
were compared. It was found that the number of H
2
TBTAC monomers in the solubilizer solutions correlated with the amount of fluorescent monomer accumulated in the cells. The H
2
TBTAC monomer showed significantly higher ability to generate singlet oxygen than H
2
TBTAC aggregates. It was established that Cremophor EL provided the maximum amount of H
2
TBTAC monomers in solution and the best stability during storage of the composition. Cremophor EL improved the accumulation of H
2
TBTAC monomer in A549 cell cytoplasm (reaching saturation after incubation for 2 h) and gave the maximum H
2
TBTAC accumulation coefficient (0.7 ± 0.1). Experiments
in vivo
showed therapeutically significant antineoplastic activity for photodynamic therapy with H
2
TBTAC stabilized in Cremophor EL solution (10%). |
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ISSN: | 0091-150X 1573-9031 |
DOI: | 10.1007/s11094-014-1051-5 |