Avaliação do efeito do praziquantel veiculado em dispersões lipídicas no tratamento de camundongos infectados com schistosoma mansoni
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Data
2008-01-11
Autores
Souza, Ana Luiza Ribeiro [UNESP]
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Editor
Universidade Estadual Paulista (Unesp)
Resumo
A esquistossomose é uma infecção parasitária causada pelo trematódeo do gênero Schistosoma. Afeta aproximadamente 200 milhões de pessoas, matando cerca de 280.000 pessoas por ano, com uma grande porcentagem dos indivíduos infectados residindo na África. Praziquantel (PRZ) é ativo contra todas as espécies de Schistosoma e é considerado o fármaco de escolha para o tratamento de tal doença. No entanto, sua baixa solubilidade em água e o risco de resistência ou tolerância do parasita ao PRZ justificam a importância de desenvolver uma alternativa tecnológica para obtenção de um produto farmacêutico que pode aumentar a eficácia terapêutica e melhorar a biodisponibilidade deste fármaco. Lipossomas têm sido utilizados com sucesso na área farmacêutica e vários estudos clínicos têm demonstrado sua versatilidade para compartimentalizar e modificar o comportamento de fármacos. Os lipossomas são capazes de modificar várias propriedades de fármacos, tais como sua farmacocinética e, no caso de fármacos lipofílicos, sua solubilidade e biodisponibilidade. O objetivo deste trabalho foi avaliar o efeito das dispersões lipídicas contendo PRZ e sua eficácia in vivo contra a cepa tolerante BH. O transporte do fármaco através da membrana intestinal foi avaliado empregando o modelo do saco intestinal invertido.
Schistosomiasis is a parasitic infection caused by trematode of the genus Schistosoma. It affects approximately 200 million people, killing as many as 280.000 people per year, with a large percentage of infected individuals residing in Africa. Praziquantel (PRZ) is active against all species of Schistosoma and it is considered the drug of choice for the treatment of such disease. However, its low water solubility and the risk of parasite resistance or tolerance to PRZ justify the importance to develop an alternative technology to obtain a pharmaceutical product that can increase the therapeutic efficacy and improve the bioavailability of this drug. Liposomes have been successfully used in the pharmaceutical area and some clinical studies have demonstrated its versatility to compartmentalize and to modify the drug behavior. Liposomes are able to modify several properties of a drug, such as its pharmacokinetics and, in the case of lipophilic drugs, their solubility and bioavailability. The aim of this work was to evaluate the effect of lipid dispersions containing PRZ and its in vivo efficacy against a BH tolerant strain. The transport of the drug through the intestinal membrane was evaluated by means of the everted gut sac model. In order to assess the effect of increasing both PC and PRZ concentrations during the structuration of these systems, they were characterized by means of SAXS, rheology, dynamic light scattering and polarized light microscopy.
Schistosomiasis is a parasitic infection caused by trematode of the genus Schistosoma. It affects approximately 200 million people, killing as many as 280.000 people per year, with a large percentage of infected individuals residing in Africa. Praziquantel (PRZ) is active against all species of Schistosoma and it is considered the drug of choice for the treatment of such disease. However, its low water solubility and the risk of parasite resistance or tolerance to PRZ justify the importance to develop an alternative technology to obtain a pharmaceutical product that can increase the therapeutic efficacy and improve the bioavailability of this drug. Liposomes have been successfully used in the pharmaceutical area and some clinical studies have demonstrated its versatility to compartmentalize and to modify the drug behavior. Liposomes are able to modify several properties of a drug, such as its pharmacokinetics and, in the case of lipophilic drugs, their solubility and bioavailability. The aim of this work was to evaluate the effect of lipid dispersions containing PRZ and its in vivo efficacy against a BH tolerant strain. The transport of the drug through the intestinal membrane was evaluated by means of the everted gut sac model. In order to assess the effect of increasing both PC and PRZ concentrations during the structuration of these systems, they were characterized by means of SAXS, rheology, dynamic light scattering and polarized light microscopy.
Descrição
Palavras-chave
Esquistossomose, Lipossomos, Praziquantel, Dispersões lipídicas
Como citar
SOUZA, Ana Luiza Ribeiro. Avaliação do efeito do praziquantel veiculado em dispersões lipídicas no tratamento de camundongos infectados com schistosoma mansoni. 2008. 79 f. Dissertação (mestrado) - Universidade Estadual Paulista, Faculdade de Ciências Farmacêuticas, 2008.