title: Liposomal modification with uronate, which endows liposomes with long circulation in vivo, reduces the uptake of liposomes by J774 cells in vitro.
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.
authors.affiliation: Research Laboratories, Nippon Fine Chemical Co. Ltd., Hyogo, Japan.
authors.forename: Y
authors.initials: Y
authors.lastname: Namba
authors.forename: N
authors.initials: N
authors.lastname: Oku
authors.forename: F
authors.initials: F
authors.lastname: Ito
authors.forename: T
authors.initials: T
authors.lastname: Sakakibara
authors.forename: S
authors.initials: S
authors.lastname: Okada
mesh_terms: D000818:Animals; D002478:Cells, Cultured; D005965:Glucuronates / Q000097:blood / Q000493:pharmacokinetics*; D006603:Hexuronic Acids / Q000493:pharmacokinetics; D008081:Liposomes / Q000378:metabolism / Q000493:pharmacokinetics*; D008264:Macrophages / Q000378:metabolism*; D051379:Mice; D012157:Mononuclear Phagocyte System / Q000378:metabolism*; D010715:Phosphatidylglycerols / Q000097:blood / Q000493:pharmacokinetics; D051381:Rats
chemical_list: D005965:Glucuronates; D006603:Hexuronic Acids; D008081:Liposomes; D010715:Phosphatidylglycerols; C065782:1-O-palmitylglucuronic acid; C007819:galacturonic acid; C030345:1,2-dipalmitoylphosphatidylglycerol