Comparative Assessment of Pharmacokinetic Parameters of Mexidol after Intravenous Administration of Liposomal Emulsion and Aqueous Solution to Rats.

Abstract

We compared the pharmacokinetic parameters of liposomal emulsion and aqueous solution of Mexidol after intravenous injection to rats at a dose of 50 mg/kg. The concentrations of Mexidol in blood plasma and homogenates of the lungs, liver, kidneys, testes, and ovaries were measured 30, 60, 120, 240 min, 24 and 48 h after administration by HPLC. The liposomal Mexidol in contrast to its aqueous solution quickly disappeared from systemic circulation (a 5-fold decrease in plasma concentration was noted as soon as 4 h after administration) and was predominantly absorbed and retained for a longer period by the liver and lungs: after 24 h, the concentration of liposomal Mexidol exceeded that of its water-soluble form by 14.2 times in the liver and by 63% in the lungs. In the testes, the concentration of liposomal Mexidol exceeded that of its water-soluble form during the first 4 h postinjection: by 4 times after 1 h and by 2 times after 4 h, whereas in the ovarian tissues, the same concentrations were observed after administration of liposomal and water-soluble forms. In the gonadal tissues, the water-soluble form of Mexidol was retained longer than its liposomal form.