The effectiveness of penetration of erythrocyte membrane by sodium salt of 2,4-dichlorophenoxyacetic acid was analyzed. The experiment was executed in a dependence on different doses of the herbicide and at different times of incubation of red blood cells with 2,4-D-Na. It is known that the main mechanism of detoxification of the cell from xenobiotics including 2,4-D is to bind them with proteins contained in blood plasma. In the case of exposure of blood to high doses of 2,4-D-Na, the unbound part of xenobiotics may penetrate into erythrocytes and change the activity of numerous parameters of the cells. The results obtained by the use of high pressure liquid chromatography (HPLC) revealed that 2,4-D-Na is adsorbed by erythrocytes of 5% haematocrite in the amount of ~1% of the initial concentration. Moreover, it was observed that 2,4-D-Na is capable of accumulating in erythrocyte’s membrane and haemolysate in the amounts of 0.15% and 1.23% of the initial concentration, respectively. It was also stated that penetration of 2,4-dichlorophenoxyacetic acid into erythrocytes is not associated with incubation time (the similar concentrations of 2,4-D-Na were detected after different incubation times of 0.5 to 3 hours); however, it was related with concentrations of the herbicide. We suggest that 2,4-D-Na was transported with concentration gradient in human erythrocytes.