Cell-based in vitro models for predicting drug permeability

Bruno Sarmento*, Fernanda Andrade, Sara Baptista da Silva, Francisca Rodrigues, José Das Neves, Domingos Ferreira

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

133 Citations (Scopus)

Abstract

In vitro cell models have been used to predict drug permeation in early stages of drug development, since they represent an easy and reproducible method, allowing the tracking of drug absorption rate and mechanism, with an advantageous costbenefit ratio. Such cell-based models are mainly composed of immortalized cells with an intrinsic ability to grow in a monolayer when seeded in permeable supports, maintaining their physiologic characteristics regarding epithelium cell physiology and functionality. Areas covered: This review summarizes the most important intestinal, pulmonary, nasal, vaginal, rectal, ocular and skin cell-based in vitro models for predicting the permeability of drugs. Moreover, the similitude between in vitro cell models and in vivo conditions are discussed, providing evidence that each model may provisionally resemble different drug absorption route. Expert opinion: Despite the widespread use of in vitro cell models for drug permeability and absorption evaluation purposes, a detailed study on the properties of these models and their in vitroin vivo correlation compared with human data are required to further use in order to consider a future drug discovery optimization and clinical development.

Original languageEnglish
Pages (from-to)607-621
Number of pages15
JournalExpert Opinion on Drug Metabolism and Toxicology
Volume8
Issue number5
DOIs
Publication statusPublished - May 2012
Externally publishedYes

Keywords

  • Cell models
  • In vitro models
  • In vitro-in vivo correlation
  • Intestinal mucosa
  • Permeability

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