The effect of various liposome formulations on insulin penetration across Caco-2 cell monolayer.
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 tauroholate 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.
Department of Pharmaceutical Technology, Faculty of Pharmacy, Gazi University, 06330-Etiler, Ankara, Turkey. tunc@tr.net, sdegim@gazi.edu.tr
Zelihagül
Z
Degim
Nilay
N
Unal
Dinç
D
Eşsiz
Ufuk
U
Abbasoglu
D000284:Administration, Oral; D000818:Animals; D001692:Biological Transport / Q000502:physiology; D001786:Blood Glucose; D018938:Caco-2 Cells; D002463:Cell Membrane Permeability; D002851:Chromatography, High Pressure Liquid; D005260:Female; D006801:Humans; D007328:Insulin / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D007413:Intestinal Mucosa / Q000378:metabolism*; D008081:Liposomes; D051379:Mice; D010316:Particle Size; D013656:Taurocholic Acid / Q000008:administration & dosage / Q000378:metabolism
D001786:Blood Glucose; D007328:Insulin; D008081:Liposomes; D013656:Taurocholic Acid