Functional modulation of drug efflux system by drug interaction and development of oral drug delivery system

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The effects of various surfactants and polyethylene glycol on the intestinal transport of rhodamine123, a P-gp substrate, were examined by an in vitro diffusion chamber system. The jejunal serosal-to mucosal transport (Jsm) of rhodamine123 was greater than its mucosal-to serosal transport (Jms). Nonionic surfactants (Cremophor EL, Tween80 and LM) reduced the Jsm/Jms ratio of rhodamine123, whereas its ratio was not influenced in the presence of cationic surfactant (C_<16>TAB) and anionic surfactant (SDS). Therefore, these findings suggested that charge of surfactants is possibly related to the action of these surfactants on the intestinal absorption of P-gp substrates. Polyethylene glycols with various molecular weights inhibited the Jsm flux of rhodamine123 across the rat jejunum membrane.