Ecology & Safety, Volume 8, 2014

Abstract: Liposomal absorption and subcellular distribution in the rat liver in normal conditions and in chronic hepatic insufficiency (CHI) due to venous congestion were compared. The rats were intravenously administered with empty liposomes (EL) and α-tocopherol containing liposomes (TL). Both liposomal types contained 3Н-lecithin as a radioactive label. Liposomal absorption and distribution were assessed by the tritium activity in the liver sample and its subcellular fractions. It was found that either type of liposomes is absorbed both by the normal and diseased liver. Intact rats showed around 70% of the label in the liver 1h after EL or TL administration. CHI rats had around 75% and 60% of the label within 1h after TL and EL administration, respectively, which demonstrated the preserved ability of the affected liver to absorb liposomes. During the first 6 hours the slow-down of the liposomal label activity was slower in CHI rats. Liposomal membrane modification by incorporating α-tocopherol had an impact both on liposomal absorption and cellular distribution. In particular, both groups showed higher affinity of TL to mitochondria as compared to EL. Thus, the results suggest that liposomal compositions can be used for targeted delivery of biologically active substances both in normal and diseased liver and can be the basis for the development of highly effective pharmaceuticals for intracellular therapy.