Transport of aripiprazole across Caco-2 monolayer model

This study aimed to investigate the transport characteristics of aripiprazole.  A human intestinal epithelial cell model Caco-2 cell in vitro cultured had been applied to study the transport of aripiprazole.  The effects of time, concentration of donor solutions, pH, temperature and P-glycoprotein inhibitor on the transport of aripiprazole were investigated.  The determination of aripiprazole was performed by HPLC.  It is concluded that aripiprazole is transported through the intestinal mucosa via a passive diffusion mechanism primarily, coexisting with a carrier-mediated transport.  The transport of aripiprazole is positively correlated to transport time, pH, and temperature.  P_app increased with donor concentrations up to 10 μg·mL^-1, and then decreased for higher concentrations.  The P-glycoprotein inhibitor cyclosporine A significantly enhanced the transport amount of aripiprazole.