Abstract

The effects of a soybean-derived sterol mixture (SS) and their glucoside mixture (SG) in dipalmitoylphosphatidylcholine (DPPC) liposomes on blood circulation and hepatic distribution were investigated by measuring the leakage of calcein after intravenous administration to mice. Four kinds of liposomes were prepared: liposomes consisting only of DPPC (DPPC liposomes); and DPPC liposomes containing SS, cholesterol (Ch) or SG (molar ratio of DPPC/X = 7:2, X = SS, Ch, SG; SS, Ch and SG liposome), respectively. The area under the blood concentration-time curve (AUC) was greater in the order, SS liposomes > DPPC liposomes > SG liposomes, and the order is the same for lower membrane fluidity. Hepatic cellular distribution of SG liposomes 2 h after intravenous injection was significantly high compared with that of DPPC and SS liposomes. The results indicated that SS liposomes were stable in the blood circulation; however, SG liposomes were not stable and appeared to have an enhancing effect on hepatic uptake. This difference might indicate that hepatic accumulation is primarily governed by the glucose group of SG.

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