Permeability, Caco-2 for BCS classification
Apparent permeability of the test compound through Caco-2 cell monolayers in two directions is investigated using transwell plates in accordance to ICH M9 guideline to classify compounds according to BCS system. Passive transport is assessed prior to the actual permeability assay. Cell monolayer integrity is controlled with transepithelial electrical resistance (TEER) measurement prior to and after the incubations. Intracellular test compound concentrations at the end of the experiment can also be quantified for mass balance evaluation.
Test concentrations: 1
Time points: 0, 2h
Replicates: 3
Control compounds
UPLC-MS/MS analysis
Background
The Biopharmaceutics Classification System (BCS) provides a robust framework for categorizing compounds based on their in vitro solubility and permeability, enabling accurate prediction of oral drug absorption in vivo and supporting formulation strategies. To facilitate BCS classification, we offer Caco-2 permeability assessments, which are fully aligned with the ICH M9 guidance. This assay has been rigorously validated using a set of control compounds that represent diverse permeability characteristics. The ICH M9 guidance aims to streamline drug development by allowing biopharmaceutics classification of system-based biowaivers, reducing the need for in vivo bioequivalence studies. Such waivers apply to certain orally administered systemic dosage forms if the compound qualifies as BCS Class I (high solubility, high permeability) or Class III (high solubility, low permeability). If you are working on a compound that you plan to apply for a biowaiver, we can assist with solubility and in vitro dissolution studies within the Symeres family.
