In vitro evaluation of 5-fluorouracil release by microspheres based on chitosan / montmorillonite/ avaliação in vitro da libertação de 5-fluorouracil por microesferas à base de quitosano / montmorilonite

Hanniman Denizard Cosme Barbosa, Bárbara Fernanda Figueiredo dos Santos,Albaniza Alves Tavares, Magno Duran Silva de Andrade, Raony de Melo Ferreira, João Marçal Medeiros de Sousa,Clayton Leite de Moura,Suédina Maria de Lima Silva

Brazilian Journal of Development(2020)

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摘要
5-fluorouracil (5-FU) is one of the most widely used chemotherapeutic compounds for cancer treatment and its rapid metabolization and non-uniform oral absorption are the limitations for its use as an oral chemotherapy. Therefore, this study was performed to evaluate the influence of a 5-fluorouracil (5-FU) nanocomposite microspheres with different diameters to test on a controlled release system in the gastrointestinal environment. 5-FU was incorporated into the chitosan/montmorillonite nanocomposite microspheres through the intercalation method. The microspheres containing the 5-FU were characterized by X-ray diffraction (XRD), scanning electron microscopy (SEM) and optical microscopy (OM). In vitro release fractions at different pHs (1.2, 7.4 and 10.0) were investigated by UV-vis spectroscopy. The release profile of 5-FU for the systems studied was adjusted through the Korsmeyer-Peppas kinetic model, and the results suggested that the mechanism of controlled release at pH 7.4 and 10 occurs by diffusion. In addition, the 5-FU microspheres diameter and roughness directly interfere with the release rate and the released fraction, since the F1 / F2 systems showed a difference in the released fraction of 5-FU of 7.97% and for the systems F3 / F4 the difference was 2.86%. The prepared F1, F2, F3 and F4 systems are suitable for delivery of 5-FU to the gastrointestinal environment in a controlled manner.
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microspheres based evaluation chitosan,vitro
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