Cell-based in vitro models for predicting drug permeability

Expert Opin Drug Metab Toxicol. 2012 May;8(5):607-21. doi: 10.1517/17425255.2012.673586. Epub 2012 Mar 18.

Abstract

Introduction: 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 cost-benefit 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 vitro-in vivo correlation compared with human data are required to further use in order to consider a future drug discovery optimization and clinical development.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Caco-2 Cells
  • Cell Line
  • Cell Membrane Permeability / drug effects*
  • Eye / cytology
  • Eye / drug effects
  • Eye / metabolism
  • Humans
  • Intestinal Absorption / drug effects
  • Intestinal Mucosa / metabolism
  • Intestines / cytology
  • Intestines / drug effects
  • Lung / cytology
  • Lung / drug effects
  • Lung / metabolism
  • Models, Biological
  • Permeability
  • Pharmaceutical Preparations / metabolism*
  • Skin / cytology
  • Skin / drug effects
  • Skin / metabolism

Substances

  • Pharmaceutical Preparations