Improvement of antischistosomal activity of praziquantel by incorporation into phosphatidylcholine-containing liposomes.
Praziquantel (PZQ) is effective against all known species of Schistosomes that infect humans. The failure of mass treatment of schistosomiasis has been attributed to the fact that therapy is not sufficiently long-lasting. This effect may be due to the low bioavailability of PZQ that has a low hydrosolubility and fast metabolism. Liposomes have been used to prolong drug levels, reduce the side effects, direct drugs to specific sites and increase bioavailability after administration. The aim of this work was to study the effect of phosphatidylcholine (PC)-containing liposomes to vehiculate PZQ to improve the treatment of schistosomiasis. The in vitro study was carried out using Schistosoma mansoni parasites recovered by perfusion from the hepatic portal system of infected mice. Suspensions of liposomes with PZQ and free PZQ were administered p.o. in mice after 14 days of infection. The effect of both preparations in vitro on S. mansoni culture was similar. In the in vivo test, PZQ-liposomes caused a decrease in amounts of eggs and parasites. Liposomes improve the antischistosomal activity of praziquantel. This can be used as a starting point to investigate alternative administration routes or dosage forms and to examine the mechanism of intestinal absorption of PRZ.
Mourão
Samanta C
SC
Programa de Pós-graduação em Ciências Farmacêuticas, Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista, Rua Rodovia Araraquara, Jaú km 01, CEP 14801-902, Araraquara, SP, Brazil.
Costa
Paulo I
PI
Salgado
Hérida R N
HR
Gremião
Maria Palmira D
MP
D000818:Animals; D008081:Liposomes; D051379:Mice; D008807:Mice, Inbred BALB C; D010713:Phosphatidylcholines / Q000008:administration & dosage*; D011223:Praziquantel / Q000008:administration & dosage* / Q000737:chemistry; D012556:Schistosomicides / Q000008:administration & dosage*; D012995:Solubility
D008081:Liposomes; D010713:Phosphatidylcholines; D012556:Schistosomicides; D011223:Praziquantel