Liposomal modification with uronate, which endows liposomes with long circulation in vivo, reduces the uptake of liposomes by J774 cells in vitro

Life Sci. 1992;50(23):1773-9. doi: 10.1016/0024-3205(92)90061-s.

Abstract

For overcoming rapid removal of liposomes from the bloodstream, we developed reticuloendothelial system (RES)-avoiding liposomes modified with a uronic acid derivative, palmityl-D-glucuronide (PGlcUA). In this current study, we examined the in vitro interaction of PGlcUA-liposomes with J774 cells derived from mouse macrophages. Liposomal association with J774 cells at 37 degrees C did not increase compared with the binding at 4 degrees C when liposomes were modified with PGlcUA. RES-avoiding ability was not specifically endowed by glucuronate but by uronates in general, since palmityl-D-galacturonide showed a similar effect on liposomal clearance in vivo and liposomal uptake in vitro. These facts indicate that modification of the liposomal surface with uronic acid derivatives endows liposomes with a long circulation time in the bloodstream by reducing their uptake by macrophages.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Cells, Cultured
  • Glucuronates / blood
  • Glucuronates / pharmacokinetics*
  • Hexuronic Acids / pharmacokinetics
  • Liposomes / metabolism
  • Liposomes / pharmacokinetics*
  • Macrophages / metabolism*
  • Mice
  • Mononuclear Phagocyte System / metabolism*
  • Phosphatidylglycerols / blood
  • Phosphatidylglycerols / pharmacokinetics
  • Rats

Substances

  • Glucuronates
  • Hexuronic Acids
  • Liposomes
  • Phosphatidylglycerols
  • 1-O-palmitylglucuronic acid
  • galacturonic acid
  • 1,2-dipalmitoylphosphatidylglycerol