Specific incorporation of asialofetuin‐labeled liposomes into hepatocytes through the action of galactose‐binding protein

Abstract

Asialofetuin-labelled liposomes (AF-liposomes) having mean diameters of 0.13 micron ([S]) and 0.35 micron ([L]) were obtained by the subsequent extrusion method in combination with dialysis. Intravenously administered AF-liposomes [S] were rapidly cleared from the systemic circulation. By pre- and post-treatment of the rats with free asialofetuin (AF), the rate of elimination decreased to that of non-labelled liposomes (N-liposomes) [S]. The liver uptake of AF-liposomes [S] (60 per cent of dose in 30 min) was about twice that of N-liposomes [S]. Forty-seven per cent of the AF-liposomes [S] incorporated into the liver were found in the parenchymal cell fraction as against 20 per cent in the non-parenchymal cell fraction. In contrast, N-liposomes [S] were taken up primarily by non-parenchymal cells as was also the case for AF- or N-liposomes [L]. Both the lipid and aqueous markers of AF-liposomes [S] were detected in subcellular fractions of the liver, but their distribution was noted to change differently with the lapse of time. Intravenously administered AF-liposomes [S] were specifically recognized by galactose-binding protein and underwent disruption in the cell after being taken up by hepatocytes. AF-liposomes [S] may possibly be utilized to deliver drugs into hepatocytes.