The effect of various liposome formulations on insulin penetration across Caco-2 cell monolayer

Degim Z., Unal N., Essiz D., Abbasoglu U.

LIFE SCIENCES, vol.75, no.23, pp.2819-2827, 2004 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 75 Issue: 23
  • Publication Date: 2004
  • Doi Number: 10.1016/j.lfs.2004.05.027
  • Journal Name: LIFE SCIENCES
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.2819-2827
  • Keywords: Caco-2, insulin, liposome, sodium taurocholate, COATED LIPOSOMES, ABSORPTION, DELIVERY, MECHANISMS, MODELS, RATS
  • Gazi University Affiliated: No


The aim of the study was to determine the penetration properties of various insulin containing liposome formulations through Caco-2 cell monolayer and to compare the in vitro test results with in vivo tests. The effect of sodium taurocholate as a penetration enhancer when it was added to the liposome formulation was also investigated. In vitro permeation experiments were performed in diffusion cells with the Caco-2 cell monolayer used as the membrane. Permeability values of various insulin containing liposome formulations through Caco-2 cells were determined (log k(insulin-solution) = -2.217 +/- 0.0723 cm.h(-1), log k(insulin-liposome) = -2.141 +/- 0.0625 cm.h(-1), log k(insulin-sodium taurohalate liposome) = -1.952 +/- 0.0623 cm.h(-1)). In vivo tests were performed in mice. Formulations were administered orally and blood glucose levels were determined and penetrations were compared with the Caco-2 cell experiment results. In conclusion, the permeability of insulin was increased across Caco-2 cell monolayer when the liposome sodium taurocholate (NaTC) formulation was used. The oral administration of insulin and NaTC incorporated liposomes significantly decreased blood glucose levels. Furthermore, it was shown that a high in vitro/in vivo correlation was observed using the Caco-2 cell monolayer model. (C) 2004 Elsevier Inc. All rights reserved.