Study on the uptake of levofloxacin by gastric epithelial system cells

Objective To investigate the uptake mechanisms of levofloxacin by gastric epithelial system(GES- 1) cells. Methods The uptake of levofloxacin in GES- 1 cells were determined by HPLC and coomassie brilliant blue. The influences of incubated time,extracellular levofloxacin concentrations,pH,temperature,inhibitors of transporters on the uptake of levofloxacin by GES- 1 cells were tested. Results The uptake of levofloxacin by GES- 1 cells was increased sharply at 1- 5 minutes then was increased moderately at 7. 5- 15. 0 minutes and reached a steady state after the start of the incubation. The accumulation of levofloxacin increased with the extracellar levels,but which was not linearly. The uptake of levofloxacin reached a maximum when temperature was 37 ℃ and pH was 7. 4. The increase in levofloxacin accumulation by cyclosporin A and verapamil in GES- 1 cells was by 2. 81%- 13. 23%,2. 07%-10. 28%,respectively( P 0. 05). Effect of the cimetidine was not same that the two drugs. Conclusion Levofloxacin enters into GES- 1cells in carrier- mediated transport manner. P- gp might be involved in the process of uptake of levofloxacin in GES- 1 cells.