Micropartículas poliméricas obtidas por spray-drying para liberação de um derivado tiofeno

2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile (6CN) is a thiophene derivative with antiproliferative activity against cancer cell lines. However, presents low aqueous solubility which interferes its clinical use. This work aims to evaluate the influence of microencapsulation technique t...

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Autor principal: Menezes, Danielle Lima Bezerra de
Outros Autores: Lima, Adley Antonini Neves de
Formato: Dissertação
Idioma:pt_BR
Publicado em: Universidade Federal do Rio Grande do Norte
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Endereço do item:https://repositorio.ufrn.br/handle/123456789/44816
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Resumo:2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile (6CN) is a thiophene derivative with antiproliferative activity against cancer cell lines. However, presents low aqueous solubility which interferes its clinical use. This work aims to evaluate the influence of microencapsulation technique to developed a new system capable of modulate its release. 6CN-loaded hydroxypropyl methylcellulose (HPMC) microspheres employing the spray-drying method were developed with different drug-polymer ratios. These systems were characterized for drug content (%), infrared, scanning electron microscopy (SEM), X-ray diffraction (XRD), granulometric and differential scanning calorimetry (DSC) analysis. The systems showed a drug content (%) between 70-80%, although losses during the developing process. Infrared results evidenced interactions between the components of the formulation. The granulometric analysis showed microparticles with an average size between 31-47 µm and SEM analysis showed particles with a well-defined and smooth spherical surface morphology. XRD and DSC analysis confirmed the 6CN crystalline nature. In contrast, in the systems it showed an amorphous state. The kinetics study with the dialysis method showed that after 10 hours almost 100% of 6CN was released in both medium (pH 1.2 and pH 7.4). The systems MP2 and MP3 were capable of promote a controlled release for 56 hours fitted the mono and biexponential model.