Abstract
The effects of glycophorin (GP) and ganglioside GM 3 (GM 3) on the blood circulation and tissue distribution of liposomes were investigated in rats. Liposomes composed of dipalmitoylphosphatidylcholine (DPPC)/cholesterol (Chol) or sphingomyelin (SM)/Chol, which contained additionally GP and/or GM 3, were prepared and the blood concentration and tissue (liver, kidney, lung and spleen) distribution after intravenous administration were compared with the control liposomes which contained neither GP nor GM 3. The blood concentration of DPPC liposomes containing GP and GM 3 (GP-GM 3-Lip[DPPC]) was significantly higher than those of the other DPPC liposomes for up to 6 h after administration, and about 3.3-fold higher than that of control liposomes (Con-Lip[DPPC]) at 6 h. The liver uptake of GP-GM 3-Lip[DPPC] at 6 h was significantly reduced compared with that of Con-Lip[DPPC], while the spleen uptake was increased significantly. Similarly, in the case of SM liposomes, the liposomes containing GP and GM 3 (GP-GM 3-Lip[SM]) prolonged the blood circulation time of liposomes and reduced their uptake by the liver, and the blood concentration was about 3.7-fold higher than that of control liposomes (Con-Lip[SM]) at 6 h. It was found that GP and GM 3 were useful and valuable for prolonging the blood circulation time of liposomes and reducing the uptake of liposomes by the liver.
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