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Dear Group,
Often early in the lead selection process during
drug development,Caco-2 cells are employed to address
the permeability of compounds which of course has
efflux transporters like P-glycoprotein to screen the
active transport of compounds/NCEs.However the
compounds that undergo passive diffusion can be
filtered from Caco-2 screening as a part of cost
effective analysis.
Literature insight reveals that Immobilized
artificial membrane (IAM) chromatography, where IAM
stationary phases are prepared by covalently
immobilizing monolayers of cell membrane phospholipids
to the inert silica particles which would then mimic
cell membranes.The chromatographic retention factors
of an analyte was reported to correlate with the
permeability through everted gut sacs.
Can IAM chromatography replace the PAMPA assay in
passive permeability screening? How confidently IAM
chromatography can be employed in screening passive
diffusion of NCEs since IAM has merits over PAMPA in
screening low permeable compounds based on
chromatographic retention indices with ease of
operation.Thanks in advance.
Regards,
S Syed Mustafa,
Drug Metabolism & Pharmacokinetics,
Discovery Research,
Dr Reddy's Lab Ltd,
Bollaram Road, Miyapur,
Hyderabad-500 049 INDIA
mustafas.-at-.drreddys.com
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Copyright 1995-2010 David W. A. Bourne (david@boomer.org)