Chloroquine containing liposomes in the chemotherapy of murine malaria.
In this study, the advantage of the use of chloroquine (CQ) containing liposomes (lipCQ) over free CQ in the chemotherapy of murine malaria (Plasmodium berghei) was demonstrated. The maximum permissible dose per intraperitoneal injection was 0.8 and 10 mg for CQ and lipCQ, respectively. An increase in therapeutic and prophylactic efficacy of lipCQ in comparison with free CQ at a 0.8 mg CQ dose level was found. It was possible to obtain 100% efficacy (injection at day 5 after infection; parasitaemia 4-8%) with one single intraperitoneal injection of 6 mg lipCQ. Moreover, the ability to increase the doses of CQ per injection after liposome encapsulation allowed successful treatment of infections with CQ-resistant Plasmodium berghei which could not be cured by a 7-day course with the maximum tolerable dose of free CQ of 0.8 mg/mouse/day.
Peeters
P A
PA
Department of Pharmaceutics, Faculty of Pharmacy, University of Utrecht, The Netherlands.
Huiskamp
C W
CW
Eling
W M
WM
Crommelin
D J
DJ
D000818:Animals; D002738:Chloroquine / Q000008:administration & dosage / Q000627:therapeutic use* / Q000633:toxicity; D004337:Drug Carriers; D007274:Injections, Intraperitoneal; D008081:Liposomes; D008288:Malaria / Q000188:drug therapy*; D008297:Male; D051379:Mice; D010962:Plasmodium berghei
D004337:Drug Carriers; D008081:Liposomes; D002738:Chloroquine