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Quantitative analysis of lab-to-lab variability in Caco-2 permeability assays

Lee, Jong Bong; Zgair, Atheer; Taha, Dhiaa A.; Zang, Xiaowei; Kagan, Leonid; Kim, Tae Hwan; Kim, Min Gi; Yun, Hwi-yeol; Fischer, Peter M.; Gershkovich, Pavel

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Jong Bong Lee

Atheer Zgair

Dhiaa A. Taha

Xiaowei Zang

Leonid Kagan

Tae Hwan Kim

Min Gi Kim

Hwi-yeol Yun

Peter M. Fischer


In this study, Caco-2 permeability results from different laboratories were compared. Six different sets of apparent permeability coefficient (Papp) values reported in the literature were compared to experimental Papp obtained in our laboratory. The differences were assessed by determining the root mean square error (RMSE) values between the datasets, which reached levels as high as 0.581 for the training set compounds, i.e. ten compounds with known effective human permeability (Peff). The consequences of these differences in Papp for prediction of oral drug absorption were demonstrated by introducing the Papp into the absorption and pharmacokinetics simulation software application GastroPlus™ for prediction of the fraction absorbed (Fa) in humans using calibrated “user-defined permeability models”. The RMSE were calculated to assess the differences between the simulated Fa and experimental values reported in the literature. The RMSE for Fa simulated with the permeability model calibrated using experimental Papp from our laboratory was 0.128. When the calibration was performed using Papp from literature datasets, the RMSE values for Fa were higher in all cases except one. This study shows quantitative lab-to-lab variability of Caco-2 permeability results and the potential consequences this can have in the use of these results for predicting intestinal absorption of drugs.


Lee, J. B., Zgair, A., Taha, D. A., Zang, X., Kagan, L., Kim, T. H., …Gershkovich, P. (2017). Quantitative analysis of lab-to-lab variability in Caco-2 permeability assays. European Journal of Pharmaceutics and Biopharmaceutics, 114, 38-42.

Journal Article Type Article
Acceptance Date Dec 14, 2016
Online Publication Date Jan 12, 2017
Publication Date 2017-05
Deposit Date Jan 17, 2017
Publicly Available Date Jan 17, 2017
Journal European Journal of Pharmaceutics and Biopharmaceutics
Print ISSN 0939-6411
Electronic ISSN 1873-3441
Publisher Elsevier
Peer Reviewed Peer Reviewed
Volume 114
Pages 38-42
Keywords Drug permeability; Caco-2 permeability assay; Lab-to-lab variability; Prediction of oral absorption; GastroPlus
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