Evaluation of dipalmitoylphosphatidylcholine liposomes containing a soybean-derived sterylglucoside mixture for liver targeting.
We investigated multilamellar vesicle (MLV) liposomes composed of dipalmitoylphosphatidylcholine (DPPC) and a soybean-derived sterylglucoside mixture (SG) (DPPC/SG-liposomes) for targeting liver parenchymal cells after administration via the tail vein in mice, using liposome-entrapping calcein. The accumulation of DPPC/SG(7:2, mole ratio, DPPC:SG = 7:2)-liposomes in the liver was the highest among DPPC/SG-liposomes. About 80% and 40% of the dose of DPPC/SG(7:2)-liposomes accumulated in the liver at 15 min and 2 h, respectively, but about 20% of DPPC/SG(7:3.5, 7:7)-liposomes accumulated at 2 h after an intravenous administration. However, the uptake of DPPC/SG(7:2, 7:3.5, 7:7)-liposomes by liver parenchymal cells was about 7 times greater than that in non-parenchymal cells irrespective of the SG concentration in liposomes. The uptake of DPPC/SG(7:2)-liposomes in liver was almost the same level as that by liposomes containing lactocylceramide (LC) (LC-liposomes) that were already known to be taken up in liver parenchymal cells by the asialoglycoprotein receptor. DPPC/SG(7:2)-liposomes effectively targeted liver, having optimal stability and SG.
Shimizu
K
K
Department of Pharmaceutics, Hoshi University, Tokyo, Japan.
Maitani
Y
Y
Takayama
K
K
Nagai
T
T
D015060:1,2-Dipalmitoylphosphatidylcholine / Q000008:administration & dosage* / Q000493:pharmacokinetics; D000818:Animals; D004337:Drug Carriers; D005069:Evaluation Studies as Topic; D005947:Glucose / Q000494:pharmacology; D005960:Glucosides / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008081:Liposomes; D008099:Liver / Q000187:drug effects / Q000378:metabolism*; D051379:Mice; D013025:Glycine max / Q000737:chemistry*; D014018:Tissue Distribution
D004337:Drug Carriers; D005960:Glucosides; D008081:Liposomes; D015060:1,2-Dipalmitoylphosphatidylcholine; D005947:Glucose