An Ex-Vivo Study on the Stereoselective Accumulation of Mefloquine Enantiomers in Human Blood Fractions

Mefloquine (mfq), as a racemic mixture is used for the prophylaxis andtreatment of malaria. stereoselective pharmacodynamic and pharmacokineticdifferences have been observed for mfq. in the present study, the human blood wasspiked with racemic mfq. the concentration of mfq enantiomers in variousblood fractions including packed erythrocyte layer, platelet rich plasma and plateletpoor plasma was determined. the results showed that the ratio of (+)-mfq was about1.5 time higher than (-)-mfq in packed erythrocyte layer. results obtained fromthe separated erythrocytes spiked with racemic mfq showed no significantdifference between the enantiomer concentrations. it can be concluded that the stereoselectiveaccumulation of mfq enantiomers in erythrocytes might be in relationto protein binding or the presence of other blood cells.