Membrane potential change effects on cationic and neutral drug - induced erythrocyte shape change and cellular uptake of drugs

Abstract

The effect of membrane potential change of the human erythrocytes on cationic drugs tetracaine and chlorpromazine and neutral drug benzyl alcohol induced cell shape change and red cell uptake of drug has been quantitated using light microscopy and spectrophotometry respectively.
At the drug concentration necessary to cause cell membrane cell shape change membrane potential change from -7.1 mV to 1 6.4mV let to the reversal of the cup-forming property of chlorpromazine and tetracaine to that of a crenetor at both 20°C and 37°C. The effect of altering
the membrane potential from -7. lmV to 16.4mV also led to the decrease of cellular uptake of drug with increasing membrane diffusion potential. The membrane potential dependent drug induced cell shape change with also reversible on reversing the membrane potential. The results therefore suggest that the cellular uptake of drug and drug induced cell shape change in human erythrocytes was dependent on change in extracellular chloride concentration