Cyclodextrin-induced hemolysis and shape changes of human erythrocytes in vitro.

Abstract

Cyclodextrins (CyD), cyclic oligosaccharides, are successfully applied pharmaceutically, to improve the physical and chemical properties of the drug molecules through inclusion complex formation. CyD at higher concentrations caused hemolysis of human erythrocytes in the order of .beta.- > .alpha.- > .gamma.-CyD in isotonic solution. Biphasic effects of CyD were observed for the osmotic and heat-induced hemolysis, i.e., the protection at relatively low CyD concentrations and stimulation at higher CyD concentrations. From the scanning EM observations, CyD induced shape changes of membrane internalization type on erythrocytes. CyD caused the release of cholesterol from erythrocyte membrane in the order of .beta.- > .gamma.- > .alpha.-CyD. CyD-induced hemolysis is probably a secondary event resulting from the membrane disruption which elicited the removal of membrane components from erythrocytes.