The Effect of Novel Surfactants and Solutol® HS 15 on Paclitaxel Aqueous Solubility and Permeability Across a Caco-2 Monolayer
The effect of novel surfactants on the aqueous solubility and the permeability of paclitaxel across a Caco-2 cell monolayer were examined in this work. The solubility and permeability of paclitaxel was evaluated in the presence of four soft surfactants (SS) KXN441, KXN424, KXN437, and KXN 337 and So...
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Published in | Journal of pharmaceutical sciences Vol. 99; no. 8; pp. 3473 - 3485 |
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Main Authors | , , , , , |
Format | Journal Article |
Language | English |
Published |
Hoboken
Elsevier Inc
01.08.2010
Wiley Subscription Services, Inc., A Wiley Company Wiley American Pharmaceutical Association |
Subjects | |
Online Access | Get full text |
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Summary: | The effect of novel surfactants on the aqueous solubility and the permeability of paclitaxel across a Caco-2 cell monolayer were examined in this work. The solubility and permeability of paclitaxel was evaluated in the presence of four soft surfactants (SS) KXN441, KXN424, KXN437, and KXN 337 and Solutol® HS15. All surfactants increased the aqueous solubility of paclitaxel. Caco-2 cell membrane integrity in the presence of SS and Solutol® HS15 was assessed by mannitol permeability and LDH release. All surfactants were tested at 0.5× CMC, 5× CMC and 1.5mM concentrations. The effect of SSs on paclitaxel permeability was concentration dependent. At all concentrations tested, KXN 441 and Solutol® HS 15 showed partially inhibition of drug efflux with no discernable change in mannitol permeability or cytotoxicity as observed with LDH release. At these concentrations, other SSs exhibited some partial efflux inhibition along with compromised membrane integrity and increasing mannitol permeability. In conclusion, all SSs were able to increase the aqueous solubility and permeability of paclitaxel across Caco-2 cells monolayer. However, KXN441 and Solutol® HS15 were able to enhance paclitaxel permeability across Caco-2 monolayer without cytotoxicity. |
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Bibliography: | istex:B9B9F1355AA20416AFB3BED97A5FA02FFEFA317C ark:/67375/WNG-Q0FNZX5Z-H ArticleID:JPS22111 ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 0022-3549 1520-6017 |
DOI: | 10.1002/jps.22111 |