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I am working with very lipophylic substances, so I have a problem to reach high concentrations with intention to evaluate enzyme kinetics. Do you have any idea what should I use to enhance the solubility and not to disrupt microsomes, Caco-2 cells, Hep g2 cells and other biologic materials? Does the use of BSA affects the determination of Km, Vmax on microsomes and Peff on Caco-2? Which concentration should I use as donor concentration- free or total?
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The following message was posted to: PharmPK
Hello
Regarding solubility enhancers and potential effects upon metabolic
assay
outcomes this is a useful reference:
Ren 2008 European J Pharmaceutics and Biopharmaceutics
For BSA see some discussion and references here:
Skolnik et al J Pharm Sci. 2010 Feb 17. [Epub ahead of print]
Towards prediction of in vivo intestinal absorption using a 96-well
Caco-2 assay.
Hope this helps?
David Turner, PhD
Principal Scientist
Simcyp Limited
Blades Enterprise Centre, John Street, Sheffield, S2 4SU, UK
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