Micropartículas de xilana contendo mesalazina visando a liberação no cólon

Xylan is an important biopolymer that can be extracted from several agrowastes in the world and has been receiving a great attention on the production of colon drug delivery systems. This polymer could pass through the digestive tract unchanged. Its complex structure requires enzymes that are prod...

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Autor principal: Urtiga, Silvana Cartaxo da Costa
Outros Autores: Egito, Eryvaldo Socrates Tabosa do
Formato: doctoralThesis
Idioma:pt_BR
Publicado em: Universidade Federal do Rio Grande do Norte
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Endereço do item:https://repositorio.ufrn.br/handle/123456789/32219
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Resumo:Xylan is an important biopolymer that can be extracted from several agrowastes in the world and has been receiving a great attention on the production of colon drug delivery systems. This polymer could pass through the digestive tract unchanged. Its complex structure requires enzymes that are produced specifically by the human colonic microflora, which makes it an interesting raw material to produce targeted drug delivery systems. The aim of this work was to produce xylan-based delivery systems loaded of mesalamine as a drug model. Xylan was extracted from corn cobs and posteriorly used to produce mesalamine-loaded xylan microparticles (XMP5-ASA) by cross-linking polymerization using a non-hazardous cross-linking agent. The microparticles were characterized by thermal analysis (DSC/TG), X-ray diffraction (XRD), infrared spectroscopy (FTIR-ATR) and scanning electron microscopy (SEM). A comparative study of the in vitro drug release from XMP5-ASA and from gastroresistant capsules filled with XMP5-ASA (XMPCAP5-ASA) or 5-ASA was also performed. FTIR-ATR, XRD and DSC/TG studies indicated no interactions among the components of the formulation that could interfere on the drug characteristics and that the drug was molecularly dispersed into the microparticles, enhancing the drug stability. The microparticles presented a spherical shape with a mean diameter size of 12.66 m ± 1.01 and 14.64 m ± 0.5 μm for XMP and XMP5-ASA, respectively. The entrapment efficiency for XMP5-ASA was 65.41 ± 3.9 %.The release studies showed that XMPCAP5- ASA allowed more efficient drug retention in the simulated gastric fluid with a prolonged drug release lasting up to 24 h. XMPCAP5-ASA retained approximately 48 % of its drug content after 6 h on the drug release assay. Therefore, the encapsulation of 5-ASA into xylan microparticles together with gastro-resistant capsules allowed a drug-controlled release at different simulated gastrointestinal medium.