Liposome clearance.
The clearance rate of liposomal drugs from the circulation is determined by the rate and extent of both drug release and uptake of liposomes by cells of the mononuclear phagocyte system (MPS). Intravenously injected liposomes initially come into contact with serum proteins. The interaction of liposomes with serum proteins is thought to play a critical role in the liposome clearance. Therefore, in this review, we focus on the role of serum proteins, so-called opsonins, that enhance the clearance of liposomes, when bound to liposomes. In addition to opsonin-dependent liposome clearance, opsonin-independent liposome clearance is also reviewed. As opposed to the conventional (non-surface modification) liposomes, we briefly address the issue of the accelerated clearance of PEGylated-liposomes (sterically stabilized liposomes, long-circulating liposomes) on repeated injection, a process that has recently been observed.
Ishida
Tatsuhiro
T
Faculty of Pharmaceutical Sciences, Department of Pharmakokinetics and Biopharmaceutics, The University of Tokushima, Japan.
Harashima
Hideyoshi
H
Kiwada
Hiroshi
H
D000818:Animals; D002417:Cattle; D003167:Complement Activation / Q000187:drug effects; D004339:Drug Compounding; D006023:Glycoproteins / Q000378:metabolism; D006168:Guinea Pigs; D006801:Humans; D007136:Immunoglobulins / Q000378:metabolism; D007275:Injections, Intravenous; D056484:Jumonji Domain-Containing Histone Demethylases; D008081:Liposomes / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D008099:Liver / Q000378:metabolism; D008563:Membrane Lipids / Q000737:chemistry; D008565:Membrane Proteins; D008657:Metabolic Clearance Rate; D051379:Mice; D009895:Opsonin Proteins / Q000378:metabolism; D010316:Particle Size; D010587:Phagocytosis; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000493:pharmacokinetics; D011485:Protein Binding; D051381:Rats; D011956:Receptors, Cell Surface / Q000378:metabolism; D011971:Receptors, Immunologic / Q000378:metabolism; D018110:Receptors, Lipoprotein; D051116:Receptors, Scavenger; D051122:Scavenger Receptors, Class B; D013045:Species Specificity; D014018:Tissue Distribution; D053482:beta 2-Glycoprotein I
D006023:Glycoproteins; D007136:Immunoglobulins; D008081:Liposomes; D008563:Membrane Lipids; D008565:Membrane Proteins; D009895:Opsonin Proteins; C498708:Ptdsr protein, mouse; D011956:Receptors, Cell Surface; D011971:Receptors, Immunologic; D018110:Receptors, Lipoprotein; D051116:Receptors, Scavenger; C454739:Scarb1 protein, mouse; D051122:Scavenger Receptors, Class B; D053482:beta 2-Glycoprotein I; C051534:dysopsonins; C408123:phosphatidylserine receptor; D011092:Polyethylene Glycols; C498707:JMJD6 protein, human; D056484:Jumonji Domain-Containing Histone Demethylases