title: Kinetic modelling of liposome degradation in peritoneal macrophages.
abstract: The objective of this study was to quantify and model the degradation process of liposomes in peritoneal macrophages (PMs). Iodinated albumin (125I-alb) was chosen to be the marker of liposome degradation. The time course of the degradation of free 125I-alb after pinocytosis by PMs followed first-order kinetics with a half-life of 23 min. The degradation of liposomally encapsulated 125I-alb was also quantified. Kinetic modelling of liposome degradation indicated the existence of two kinetically different processes, one with a half-life of 13 min and the other with a half-life of 7.5 h. Comparing the degradation of liposomal and free 125I-alb suggested that 125I-alb was delivered to lysosomes much faster through phagocytosis than pinocytosis. These results indicate that the intracellular degradation kinetics of pinosomes and phagosomes is different. This method can quantify the rate and extent of liposomal degradation in macrophages and provide kinetic information on the intracellular destiny of liposomally encapsulated compounds.
authors.affiliation: Faculty of Pharmaceutical Sciences, University of Tokushima, Japan.
authors.forename: H
authors.initials: H
authors.lastname: Harashima
authors.forename: N
authors.initials: N
authors.lastname: Hirai
authors.forename: H
authors.initials: H
authors.lastname: Kiwada
mesh_terms: D000418:Albumins / Q000008:administration & dosage / Q000493:pharmacokinetics; D000818:Animals; D006207:Half-Life; D008081:Liposomes / Q000493:pharmacokinetics*; D017737:Macrophages, Peritoneal / Q000378:metabolism*; D008297:Male; D008954:Models, Biological; D010587:Phagocytosis; D010873:Pinocytosis; D051381:Rats; D017208:Rats, Wistar
chemical_list: D000418:Albumins; D008081:Liposomes