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Desenvolvimento de um m?todo inovador de forma??o de nanoemuls?es para libera??o modificada de praziquantel atrav?s da dilui??o de cristais l?quidosSouza, Izadora de 31 July 2015 (has links)
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Previous issue date: 2015-07-31 / Coordena??o de Aperfei?oamento de Pessoal de N?vel Superior (CAPES) / Cristais l?quidos (CL) possuem um arranjo molecular bastante estruturado que combina propriedades dos estados l?quido e s?lido, bem como o fluxo dos l?quidos e a ordena??o da estrutura cristalina dos s?lidos. Foram testadas t?cnicas de alta e baixa energia para produzir CL, utilizando oleato de s?dio, fosfatidilcolina de soja, ?leo de soja, N-metilpirrolidona (NMP) e ?gua. As intera??es entre NMP e oleato de s?dio da formula??o foram investigadas. CL obtidos por t?cnica de alta energia foram caracterizados por microscopia de luz polarizada (MLP), reologia e tamanho de part?cula. MLP exibiu estruturas que sugerem presen?a de CL lamelares. Na reologia, as amostras apresentaram viscosidade newtoniana limitante nas curvas de fluxo e uma diminui??o no grau de estrutura??o nos testes oscilat?rios, quando a concentra??o de NMP diminu?a. Uma nova t?cnica para obter sistemas lip?dicos de libera??o de f?rmacos foi desenvolvida a partir da dilui??o de CL produzidos por baixa energia. CL foram produzidos por agita??o magn?tica e, posteriormente, foram dilu?dos com ?gua e solu??o aquosa de NMP 10%, a 25 ? C e 70 ?C, em que foram avaliados tamanho de got?cula e incorpora??o de praziquantel (PRZ). Os sistemas dilu?dos com ?gua apresentaram menor faixa de tamanho (165,22 ? 381,26 nm) e maior faixa de incorpora??o de PRZ (40,96 ? 43,44 mg/mL) quando comparadas com as dilu?das com a solu??o de NMP. N?o houve contribui??o da solu??o de NMP para a forma??o de got?culas menores e para a maior incorpora??o de PRZ. Houve um aumento na solubilidade do PRZ em sistemas dilu?dos com ?gua, aumentando a fra??o sol?vel de f?rmaco em at? 200 vezes quando comparada ? sua solubilidade em ?gua. Testes utilizando Espalhamento de raios-X a baixo ?ngulo e MLP comprovaram a transi??o da mesofase lamelar para sistemas com micelas vermiformes, confirmando o sucesso da nova t?cnica em obter sistemas lip?dicos de libera??o de f?rmacos atrav?s da dilui??o de CL. / Liquid crystalline mesophase (LC) have an organized molecular arrangement and combining properties of liquid and solid state as the flow of liquids and the ordered and crystalline structure of solids. High- and low energy techniques were used to produce LC. N-methylpyrrolidone (NMP) and sodium oleate interactions with the system were investigated. LC fabricated by high-energy method were characterized by polarizing light microscopy (PLM), rheology and droplet size. PLM showed structures that indicated lamellar phases. Surface tension no important difference between the samples was observed. Rheology showed a zero shear viscosity in flow curves with a shear-thinning behavior in oscillatory tests, which with increasing of NMP, there was a decrease in degree of structure. Novel method to obtain lipid based drug delivery system (LBDDS) were developed through LC dilution and drug-loading was tested. LC fabricated with low-energy method was diluted with water and NMP 10% aqueous solution, at 25 ?C and 70 ?C, which droplet size and drug loading were evaluated. The systems diluted with water showed lower range size (165.22 nm- 381.26 nm) and higher drug-loading (40.96 mg/mL - 43.44 mg/mL) when compared with systems diluted by NMP solution. NMP aqueous solution did not contribute to form smaller particle size and higher praziquantel-loading. An increment in the apparent solubility of Praziquantel was achieved from incorporation in dilution of LC with water, increasing the soluble drug fraction approximately 200-fold when compared with water solubility. Small angle X-ray scattering (SAXS) measurements and PLM comproved the transition from lamellar mesophase to worm-like micelle systems confirming the success of new techinique for obtain LBDDS from LC dilution.
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