Transport of bovine milk-derived opioid peptides across a Caco-2 monolayer

The transepithelial transport of μ-opioid (MOP) receptor agonists, i.e., bovine β-casomorphin-5 and -7 (derived from β-casein) and an antagonist, i.e., casoxin-6 (derived from κ-casein) were investigated using a human intestinal cell (Caco-2) monolayer. To determine the transport pathway of the peptides across Caco-2 monolayers, two directions of the transport (apical-to-basolateral and basolateral-to-apical) were studied. All investigated peptides were transported across Caco-2. The cumulative fractions of transported peptides were increased linearly in time in each case. The permeability coefficients (Paap) calculated for all peptides in two transport directions ranged between 0.57 and 9.21 × 10−6 cm min−1. These data suggest the possibility of transport of opioid peptides derived from food across human intestinal mucosa.