Effect of Tween-80 on the permeability of rhodamine 123, a P-gp substrate across rat intestinal membranes in vitro.
- Author:
Guo-feng LI
1
;
Ya-fei TAN
;
Dan GUO
;
Lin WANG
Author Information
- Publication Type:Journal Article
- MeSH: ATP-Binding Cassette, Sub-Family B, Member 1; metabolism; Animals; Colon; metabolism; Ileum; metabolism; In Vitro Techniques; Intestinal Absorption; drug effects; Intestinal Mucosa; metabolism; Jejunum; metabolism; Male; Permeability; drug effects; Polysorbates; pharmacology; Rats; Rats, Wistar; Rhodamine 123; metabolism; pharmacokinetics
- From: Journal of Southern Medical University 2008;28(4):579-581
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVETo investigate the effect of Tween-80 in modulating rhodamine123 (R123) permeability across the intestinal membranes.
METHODSThe permeability of R123 or fluorescein sodium (CF) across isolated rat intestinal membranes at the concentration of 5 microg/ml was evaluated using an in vitro diffusion chamber system, in the presence or absence of Tween-80 at different low concentrations. The concentration of R123 or CF in the receptor chamber was determined using fluorospectrophotometry.
RESULTSThe intestinal membrane permeability of R123 gradually decreased from the jejunum to the ileum and then to the colon. The serosal-to-mucosal transport of R123 was much greater than its mucosal-to-serosal transport. In the presence of low concentrations of Tween-80, the absorptive transport of R123 was significantly increased while its secretory transport decreased depending on the concentration of Tween-80. However, Tween-80 at the experimental concentrations was found to obviously affect the CF transport across the intestinal membranes.
CONCLUSIONLow concentrations of Tween-80 may promote the absorption of P-gp-mediated drugs and therefore improve the oral bioavailability of these drugs.
