Evaluation of the praziquantel in liposome effect in Schistosoma mansoni in vivo / Avaliação do efeito do praziquantel associado a lipossomas em Schistosoma mansoni in vivo

AUTOR(ES)
DATA DE PUBLICAÇÃO

2007

RESUMO

For the treatment of schistosomiasis mansoni in Brazil, the drugs of choice are Oxamniquina (OXA) and the Praziquantel (PRZ). OXA has its production reduced by its collateral, carcinogenic and mutagenic effects that it presents. PRZ has wide action spectrum and low toxicity, when compared to OXA. However, it has the disadvantage of being eliminated very fast by the organism. Besides, it has its action depending on the age of the parasite and its extensive use leads to a resistance of the Schistosoma mansoni to the drug. It?s necessary the research of new alternatives to make PRZ more available in the organism, with more adequate liberation rate. One of these alternatives is its incorporation to the liposome (LPZ). The current work had as a target to analyze the effect of the PRZ incorporated to LPZ (PRZ+LPZ) by its action in the survival of adult worms of Schistosoma mansoni, BH strain, and alteration in the laying of eggs beyond its action in the formation of granulomas in the liver. Five doses were tested of PRZ e PRZ+LPZ (40; 47; 60; 250 and 300 mg/kg) in Swiss mice, administered by the intragastric route in only one dose. The liposomes of phosphatidilcoline were prepared by the method of sonication. The mice were divided in two big groups (one of them was treated after 30 days of infection and the other group treated after 45 days) and in each group ten animals received a determined dose of PRZ to be tested, to the other ten the same dose, this time with PRZ+LPZ and to the last ten, Busser Tris HCl pH 7,5. After 15 days of the administration of the treatment, the animals were sacrificed and necropsies. The treatment done with PRZ+LPZ in the dose of 300 mg/kg, administered of the 45th day of the infection, showed itself superior to the majority of the analyzed parameters (higher quantity of worms outside the porta-hepatic system which indicates a response of the worm to the action of the drug -, big reduction in the number of worms and eggs in the fezzes and big reduction of the viable eggs in the intestines mainly of immature eggs). Probably this treatment altered the oviposition of the worm. The organs of mice treated with PRZ+LPZ in dose of 300 mg/kg, administered in the 30est day of infection, presented fewer injuries. Besides, they don t show granulomas in the livers observed histological, which can be explained by the low oviposition that occurs in this period, with the fact that this treatment perhaps having the capacity of minimize the formation of granulomas. The treatment done with PRZ+LPZ was superior probably because the availability increased of the drug in the organism as well its solubility in water environment. Besides, the drug, when incorporated, probably was more easily absorbed by the worm, making the harm provoqued by PRZ deeper .

ASSUNTO(S)

liposome schistosoma mansoni praziquantel praziquantel schistosoma mansoni lipossomos

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