Several studies have shown that Caco-2 cells have the capability to transpo
rt peptides and proteins from their apical to basal surfaces when these mol
ecules are linked to vitamin B-12 (VB12). In this study we have extended th
ese studies and have shown that Caco-2 cells are also able to internalize a
nd transport VB12-modifed nanoparticles from their apical to basal surfaces
. Uptake and transport of nanoparticles was found to occur in both a VB12-d
ependent intrinsic factor (IF)-independent manner as well as in a VB12-depe
ndent IF-dependent manner. Both IF-independent and IF-dependent VB12-mediat
ed uptake and transport were dependent upon the surface density of VB12 as
a reduction in surface modification of the nanoparticles with VB,, resulted
in a reduced level of both VB12-mediated and IF-mediated uptake. At lower
levels of VB,, modification there was no apparent non-IF-mediated uptake; h
owever, VB12-IF-mediated uptake was still measurable. These studies show th
at Caco-2 cell cultures are a suitable model for the study of VB12-mediated
uptake and transport of nanoparticles, and suggest that for effective oral
uptake of VB12-coated nanoparticles high surface densities of VB12 are req
uired. (C) 1999 Elsevier Science B.V. All rights reserved.