Ajuste de liberação de fármaco a partir de dispersões sólidas utilizando blendas poliméricas processadas por extrusão a quente

• Autor(a) principal: Soares, Julia Ciarlini Junger
• Data de Publicação: 2015
• Tipo de documento: Trabalho de conclusão de curso
• Idioma: por
• Título da fonte: Repositório Institucional da UFRN
• Texto Completo: https://repositorio.ufrn.br/handle/123456789/38765
• topic: Extrusão hot-melt. Dispersões sólidas. Efavirenz. Blendas poliméricas. Liberação de fármaco.; Hot-melt extrusion. Solid dispersion. Efavirenz. Polymer blends. Drug release.

In the past decades, advances in combinatorial chemistry and high throughput screening led to the discovery of numerous new drugs. However, their solubility behavior and bioavailability are limiting factors to their development and commercialization, since most of the new drugs are poorly water-soluble. The production of amorphous solid dispersions is a promising strategy to overcome this limitation, and hot-melt extrusion represents a valuable technology to obtain such a product using polymers as carrier matrix. In addition to improvements in apparent solubility, dissolution rate and bioavailability, the possibility of achieving controlled drug release by changing the matrix properties is extremely attractive. This study aimed to control and investigate the in vitro release pattern of a poorly water soluble drug – Efavirenz – from solid dispersions processed by hot-melt extrusion using Soluplus® individually and combined with Eudragit® EPO, Eudragit® RL100 or Klucel™ JF as carrier matrices. The products were characterized through scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffractometry (XRD), dissolution studies and solubility tests. The results confirm the formation of amorphous solid dispersions and the achievement of controlled drug release to all the polymer combinations used in this work, which ensures the potential of using polymer blends and hot-melt extrusion as solid dispersion manufacturing technique to tailor drug dissolution behavior.