Desenvolvimento de blendas de dextranos de pesos moleculares 70 e 148 KDA para a obtenção de hidrogéis contendo praziquantel

• Autor(a) principal: Campos, Flávio dos Santos [UNESP]
• Data de Publicação: 2013
• Tipo de documento: Tese
• Idioma: por
• Título da fonte: Repositório Institucional da UNESP
• Texto Completo: http://hdl.handle.net/11449/108793
• topic: Dextrano; Farmacotécnica; Esquistossomose; Biofarmacêutica; Schistosoma mansoni

Schistosomiasis is a major parasitic diseases in the tropics and subtropics, caused by Schistosoma mansoni. An alternative treatment for this condition is chemotherapy, especially with praziquantel (PZQ), which is highly permeable, but has a very low solubility in water, which interferes with its bioavailability. Many strategies have been use polymers in the development of systems for controlled drug release in order to modify pharmacotechnical and biopharmaceutical properties. Amongst them, highlight the dextran hydrogels, which present various advantageous properties, some of them are: low toxicity, biocompatibility and biodegradability. In previous studies, dextran 70 (DEX-70) and 148kDa (DEX-148) hydrogels containing praziquantel had been developed by a simple, economical, of easy execution, without the use of chemical crosslinking, which generated different release profiles of drug incorporated, due swelling capacity of the hydrogels formed from each one of polymers. Based on observed in this study, the utilization of blends, which can present a major technological advantage by developing new materials with different properties, without losing its characteristics and adding their advantageous properties that can be used in the development of delivery systems, was evaluated, to provide a modulation of its pharmacotechnical and biopharmaceutical propertiesin order to develop a new technological platform in terms of systems for drug delivery. Hidrogels were characterized, employing 1H-NMR, which found an interaction between dextran and praziquantel into 1:1:1 (PZQ:DEX-70:DEX-148) hydrogel. The X-ray diffraction along with DSC showed that part of drug is dispersed in the polymer matrix in the form of crystallites, helping to improve its solubility, as evidenced by solubility studies. In in vivo studies, the sample 1:2:1 and 1:2:2, were the ones that were more effective. Finally, it was found that preparation of dextran blends containing ...