Effect of medium-chain glycerides on physiological properties of XXXX intestinal epithelium in vitro.

@entity2656 @entity3405 @entity95 @entity21212 @entity7265
Medium chain glycerides (MCGs) have been reported to enhance intestinal absorption of hydrophilic drugs. However, the mechanisms involved in absorption enhancement are not well understood. The effects of MCGs (CapMul @entity21212 ) on physiological properties of @entity95 ileum and distal colon, including active ion transport, transepithelial resistance (Rt) and passive permeability, have been investigated in vitro. CapMul @entity21212 inhibited active ion transport (measured as a decrease in short-circuit current, Isc) in both intestinal segments in a concentration-dependent manner. The inhibition of Isc was rapidly reversible (within 100 min) upon removal of CapMul @entity21212 . The data indicate that CapMul @entity21212 preferentially affected ion transport by villus cells in the ileum and surface cells in the distal colon. Ion transport in crypt cells in both segments was not significantly altered. Rt of the ileum was not significantly affected by 5% CapMul @entity21212 , while @entity2656 transport was 6 fold enhanced. Treatment of distal colon with 1% CapMul @entity21212 reduced Rt by 95%, while @entity2656 transport was 100 fold enhanced. In a parallel experiment, mucosal(m)-to-serosal(s) transport of @entity7265 , a @entity3405 antibiotic, in the ileum was about 40% reduced in the presence of 5% CapMul @entity21212 , whereas transport in the s-to-m direction was 2.5 fold enhanced. Treatment of the distal colon with 1% CapMul @entity21212 resulted in 25 fold enhancement of @entity7265 transport in either direction. These results suggest that absorption enhancement by MCGs results from an increased permeability of the intestine confined to the villus or surface epithelium.
