Desenvolvimento e caracterização de carreadores lipídicos nanoestruturados contendo praziquantel
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Data
2011-01-20
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Universidade Estadual Paulista (Unesp)
Resumo
A esquistossomose é uma doença que atinge cerca de 200 milhões de pessoas no mundo todo. A alta incidência desta doença está ligada à falta de condições sanitárias, ao diagnóstico tardio e, principalmente, à falta de tratamento medicamentoso eficiente. O praziquantel é o fármaco de primeira escolha para o tratamento da esquistossomose. No entanto, falhas no tratamento com este fármaco e relatos de isolamento de S. mansoni tolerantes podem comprometer a eficiência do PZQ. Assim, o PZQ representa um fármaco em que pesquisas para melhorar as suas propriedades biofarmacêuticas são necessárias, pois apresenta baixa solubilidade em meio aquoso e biodisponibilidade baixa ou errática. O presente trabalho vê como finalidade desenvolver carreadores lipídicos nanoestruturados (NLC) contendo praziquantel empregando como sistema lipídico o monoestearato de glicerila (GMS) e o ácido oléico (AO) e como sistema tensoativo a associações de monoestearato de polioxietileno sorbitano 60 (TWEEN60), fosfatidilcolina, Poloxamer (Pluronic F-127 PLU). Os NLCs foram preparados através de dois diferentes métodos, de sonicação e alta velocidade de cisalhamento a quente. Os sistemas foram caracterizados através da avaliação dos parâmetros de distribuição de tamanho, potencial zeta, índice de polidispersidade e eficiência de encapsulação. O transporte intestinal do fármaco foi avaliado através do modelo do saco intestinal invertido. Ambos os métodos de obtenção empregados mostraram-se eficazes para o preparo dos NLCs em escala nanometrica, com índice de polidispersidade homogeneo e um...
The Schistosomiasis is a debilitating disease with high misfit in the quality of people life reached about 200 million people worldwide. The high incidence of this disease is linked to poor sanitary conditions, late diagnosis, and especially the lack of effective drug treatment. Praziquantel is the drug of first choice for treatment of schistosomiasis. However, treatment failures with this drug and reports of isolation of S. mansoni tolerance may compromise the efficiency of PZQ. Thus, the PZQ represents an example in which surveys to improve the biopharmaceutical properties are needed, since it has low solubility in aqueous and low or erratic bioavailability. This work aims to develop nanostructured lipid carriers (NLC) containing praziquantel employing as lipid system the glycerin monostearate (GMS) and oleic acid (OA) as a surfactant system and some combination of polyoxyethylene sorbitan monostearate 60 (TWEEN60), phosphatidylcholine and Poloxamer (Pluronic F-127 PLU) as a surfactant system. NLCs were prepared by two different methodologies, the sonication and high shear rates to warm. The systems were characterized by determination of size distribution, zeta potential, polydispersity index and encapsulation efficiency. The intestinal transport of the drug was evaluate by using the model of inverted intestinal sac. Both methods were effective for the preparation of NLCs with an average diameter in the nanometer range, the polydispersity index indicating homogeneity of particle size and a zeta... (Complete abstract click electronic access below)
The Schistosomiasis is a debilitating disease with high misfit in the quality of people life reached about 200 million people worldwide. The high incidence of this disease is linked to poor sanitary conditions, late diagnosis, and especially the lack of effective drug treatment. Praziquantel is the drug of first choice for treatment of schistosomiasis. However, treatment failures with this drug and reports of isolation of S. mansoni tolerance may compromise the efficiency of PZQ. Thus, the PZQ represents an example in which surveys to improve the biopharmaceutical properties are needed, since it has low solubility in aqueous and low or erratic bioavailability. This work aims to develop nanostructured lipid carriers (NLC) containing praziquantel employing as lipid system the glycerin monostearate (GMS) and oleic acid (OA) as a surfactant system and some combination of polyoxyethylene sorbitan monostearate 60 (TWEEN60), phosphatidylcholine and Poloxamer (Pluronic F-127 PLU) as a surfactant system. NLCs were prepared by two different methodologies, the sonication and high shear rates to warm. The systems were characterized by determination of size distribution, zeta potential, polydispersity index and encapsulation efficiency. The intestinal transport of the drug was evaluate by using the model of inverted intestinal sac. Both methods were effective for the preparation of NLCs with an average diameter in the nanometer range, the polydispersity index indicating homogeneity of particle size and a zeta... (Complete abstract click electronic access below)
Descrição
Palavras-chave
Esquistossomose, Schistosoma mansoni, Carreadores lipídicos nanoestruturados, Praziquantel, Nanostructured lipid carriers
Como citar
SANTOS, Fernanda Kolenyak dos. Desenvolvimento e caracterização de carreadores lipídicos nanoestruturados contendo praziquantel. 2011. 81 f. Dissertação (mestrado) - Universidade Estadual Paulista, Faculdade de Ciências Farmacêuticas, 2011.