Evaluation of dipalmitoylphosphatidylcholine liposomes containing a soybean-derived sterylglucoside mixture for liver targeting

J Drug Target. 1996;4(4):245-53. doi: 10.3109/10611869608995626.

Abstract

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.

MeSH terms

  • 1,2-Dipalmitoylphosphatidylcholine / administration & dosage*
  • 1,2-Dipalmitoylphosphatidylcholine / pharmacokinetics
  • Animals
  • Drug Carriers*
  • Evaluation Studies as Topic
  • Glucose / pharmacology
  • Glucosides / administration & dosage*
  • Glucosides / pharmacokinetics
  • Liposomes
  • Liver / drug effects
  • Liver / metabolism*
  • Mice
  • Soybeans / chemistry*
  • Tissue Distribution

Substances

  • Drug Carriers
  • Glucosides
  • Liposomes
  • 1,2-Dipalmitoylphosphatidylcholine
  • Glucose