Abstract

Considering the importance of lipophilicity of contraceptive β-estradiol (ES) a significant contributor to its mechanism of action, interactions of the drug with total lipids of goat whole blood have been investigated using phospholipid binding, fatty acid composition and peroxidation phenomena as the parameters under investigation. The objective was to derive an insight into the pharmacodynamic behavior of the drug. Significant loss in phospholipid along with changes in fatty acid composition was observed after incubation of whole blood with ES at 150 pg/ml (effective contraceptive concentration in blood) in varying periods of time. This may be ascribed to binding affinity of ES with lipid constituents in blood. Lipid binding potential of the drug may have a role in its therapeutic effect. The effect of ES on lipid peroxidation phenomenon has been quantitatively measured and the results reveal that ES caused significant inhibition of lipid peroxidation which is in good agreement with its cardioprotectant action.