Effect of nonsteroidal anti-inflammatory drugs on the permeability of the rectal mucosa.

Publisher Website
Google Scholar
Abstract
Recently, rectal administration was studied as a delivery route to overcome the problem of mucosal irritation. The effect of nonsteroidal anti-inflammatory drugs (NSAID) on the permeability to marker drugs, sulfanilic acid and creatinine, was investigated in the rat rectum using the in situ perfusion technique: Indomethacin (IM), phenylbutazone (PB), diclofenac sodium (DF) and aspirin (ASA) were used as NSAID. The permeability of rectal mucosa to the marker drugs was increased by NSAID. The permeability-enhancing effect increased in the following order: ASA < PB < DF < IM. The effects were reversible. No marked histological changes were observed and protein release from the rectal mucosa was not increased. There was a good correlation between the permeability-enhancing effect and the NSAID amount accumulated in the rectum. The accumulation of NSAID in the rectum apparently plays an important role in the enhancement of the rectal permeability to drugs.