The objective of this study was to quantify and model the degradation
process of liposomes in peritoneal macrophages (PMs). Iodinated albumi
n (I-125-alb) was chosen to be the marker of liposome degradation. The
time course of the degradation of free I-125- alb after pinocytosis b
y PMs followed first-order kinetics with a half-life of 23 min. The de
gradation of liposomally encapsulated I-125-alb was also quantified. K
inetic modelling of liposome degradation indicated the existence of tw
o 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 lipo
somal and free I-125-alb suggested that I-125-alb was delivered to lys
osomes much faster through phagocytosis than pinocytosis. These result
s indicate that the intracellular degradation kinetics of pinosomes an
d phagosomes is different. This method can quantify the rate and exten
t of liposomal degradation in macrophages and provide kinetic informat
ion on the intracellular destiny of liposomally encapsulated compounds
.