Comparison of the permeability characteristics of a human colonic epithelial (Caco-2) cell line to colon of rabbit, monkey, and dog intestine and human drug absorption

Pharm Res. 1993 Jan;10(1):113-8. doi: 10.1023/a:1018937416447.


The in vitro permeabilities of Caco-2 monolayers and permeabilities in tissue sections from colon of monkey, rabbit, and dog were compared using a series of compounds. The selected compounds differed in their physicochemical properties, such as octanol/water partition coefficient, water solubility, and molecular weight. Their structure included steroids, carboxylic acids, xanthins, alcohols, and polyethylene glycols. A linear permeability relationship was established between Caco-2 and colon tissue from both rabbit and monkey. The results suggest that Caco-2 is twice as permeable as rabbit and five times as permeable as monkey colon. However, no clear relationship could be established between Caco-2 monolayers and dog colon permeability. A relationship between permeability in Caco-2 monolayers and human absorption was found. The results suggest that within certain limits, permeability of Caco-2 monolayers may be used as a predictive tool to estimate human drug absorption.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Cell Line
  • Cell Membrane Permeability / physiology*
  • Chemical Phenomena
  • Chemistry, Physical
  • Colon / cytology
  • Colon / metabolism
  • Dogs
  • Humans
  • Intestinal Absorption / physiology*
  • Intestinal Mucosa / cytology
  • Intestinal Mucosa / metabolism
  • Intestines / cytology
  • Macaca fascicularis
  • Rabbits
  • Solubility
  • Species Specificity