article · Acta Medica (Hradec Kralove Czech Republic) · 2011

Caco-2 Cells, Biopharmaceutics Classification System (BCS) and Biowaiter

Libuše Smetanová, V. Štětinová, Zbyněk Svoboda, J Kvĕtina

Cited by 66Open access

Abstract

Almost all orally administered drugs are absorbed across the intestinal mucosa. The Caco-2 monolayers are used as an in vitro model to predict drug absorption in humans and to explore mechanism of drug absorption. The Caco-2 cells are derived from a human colon adenocarcinoma and spontaneously differentiate to form confluent monolayer of polarized cells structurally and functionally resembling the small intestinal epithelium. For studying drug permeability, Caco-2 cells are seeded onto the Transwell inserts with semipermeable membrane and grown to late confluence (21 days). After determination of cell viability, the integrity of monolayer is checked by phenol red permeability and by 14C-mannitol permeability. The transport from apical to basolateral (AP-BL) and basolateral to apical (BL-AP) is studied by adding the diluted drug on the apical or basolateral side and withdrawing the samples from the opposite compartment, respectively, for HPLC analysis or liquid scintillation spectrometry. Ca2+ -free transport medium is used to determine paracellular component of the drug transport. On the basis of permeability and solubility, drugs can be categorized into four classes of Biopharmaceutics Classification System (BCS). For certain drugs, the BCS-based biowaiver approach can be used which enables to reduce in vivo bioequivalence studies.

Cite this paper

APA 7

Smetanová, L., Štětinová, V., Svoboda, Z., & Kvĕtina, J. (2011). Caco-2 Cells, Biopharmaceutics Classification System (BCS) and Biowaiter. Acta Medica (Hradec Kralove Czech Republic), 54(1), 3–8. https://doi.org/10.14712/18059694.2016.9

MLA 9

Smetanová, Libuše, et al. “Caco-2 Cells, Biopharmaceutics Classification System (BCS) and Biowaiter.” Acta Medica (Hradec Kralove Czech Republic), vol. 54, no. 1, 2011, pp. 3–8, https://doi.org/10.14712/18059694.2016.9.

Chicago

Smetanová, Libuše, V. Štětinová, Zbyněk Svoboda, and J Kvĕtina. 2011. “Caco-2 Cells, Biopharmaceutics Classification System (BCS) and Biowaiter.” Acta Medica (Hradec Kralove Czech Republic) 54 (1): 3–8. https://doi.org/10.14712/18059694.2016.9.

Harvard

Smetanová, L. et al. (2011) ‘Caco-2 Cells, Biopharmaceutics Classification System (BCS) and Biowaiter’, Acta Medica (Hradec Kralove Czech Republic), 54(1), pp. 3–8. Available at: https://doi.org/10.14712/18059694.2016.9.

BibTeX

@article{smetanova2011caco,
  title = {{Caco-2 Cells, Biopharmaceutics Classification System (BCS) and Biowaiter}},
  author = {Smetanová, Libuše and Štětinová, V. and Svoboda, Zbyněk and Kvĕtina, J},
  journal = {Acta Medica (Hradec Kralove Czech Republic)},
  volume = {54},
  number = {1},
  pages = {3--8},
  year = {2011},
  doi = {10.14712/18059694.2016.9}
}

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