The parenteral controlled release of liposome encapsulated chloroquine in mice.
Free (0.6 mg), and liposome encapsulated chloroquine (0.6, 3 mg), were injected intraperitoneally, intramuscularly and subcutaneously in mice. Intraperitoneal administration of liposome-encapsulated chloroquine resulted in high and long lasting concentrations of chloroquine in the blood compared with intraperitoneal administration of free chloroquine. After administration of the liposome-encapsulated chloroquine the concentrations in the spleen were also higher, indicating that chloroquine liposomes reached the blood compartment intact after intraperitoneal administration. After intramuscular and subcutaneous administration the chloroquine liposomes acted as a local depot, giving a slower release from the subcutaneous fat layer than from the muscle depot. After the 0.6 mg dose a burst effect was found at about 7 h in most of the animals; this was not found after the 3 mg dose. This finding and the slower release after the 3 mg dose than after the 0.6 mg dose could be explained by the formation of aggregates after the injection.
Titulaer
H A
HA
Department of Pharmaceutics, University of Utrecht, The Netherlands.
Eling
W M
WM
Crommelin
D J
DJ
Peeters
P A
PA
Zuidema
J
J
D000818:Animals; D002738:Chloroquine / Q000008:administration & dosage / Q000097:blood / Q000378:metabolism*; D003692:Delayed-Action Preparations; D007273:Injections, Intramuscular; D007274:Injections, Intraperitoneal; D007279:Injections, Subcutaneous; D008081:Liposomes; D051379:Mice; D013154:Spleen / Q000378:metabolism*
D003692:Delayed-Action Preparations; D008081:Liposomes; D002738:Chloroquine