5-Fluorouracil loaded Eudragit fibers prepared by electrospinning

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• 作者：U. Eranka Illangakoon^a ; Deng-Guang Yu^b ; ^{ydg017@usst.edu.cn" class="auth_mail" title="E-mail the corresponding author} ; Bilal S. Ahmad^a ; Nicholas P. Chatterton^c ; ^{nicholas.chatterton@open.ac.uk" class="auth_mail" title="E-mail the corresponding author} ; Gareth R. Williams^a ; ^{g.williams@ucl.ac.uk" class="auth_mail" title="E-mail the corresponding author}
• 关键词：5-Fluoruracil (PubChem CID ; 3385)
• 刊名：International Journal of Pharmaceutics
• 出版年：2015
• 出版时间：30 November 2015
• 年：2015
• 卷：495
• 期：2
• 页码：895-902
• 全文大小：2260 K

文摘

A series of 5-fluorouracil (5-FU) loaded core/shell electrospun fibers is reported. The fibers have shells made of Eudragit S100 (ES-100), and drug-loaded cores comprising poly(vinylpyrrolidone), ethyl cellulose, ES-100, or drug alone. Monolithic 5-FU loaded ES-100 fibers were also prepared for comparison. Electron microscopy showed all the fibers to have smooth cylindrical shapes, and clear core–shell structures were visible for all samples except the monolithic fibers. 5-FU was present in the amorphous physical form in all the materials prepared. Dissolution studies showed that the ES-100 shell was not able to prevent drug release at pH 1.0, even though the polymer is completely insoluble at this pH: around 30–80% of the maximum drug release was reached after 2 h immersion at pH 1.0. These observations are ascribed to the low molecular weight of 5-FU permitting it to diffuse through pores in the ES-100 coating, and the relatively high acid solubility of the drug providing a thermodynamic impetus for this to happen. In addition, the fibers were observed to be broken or merged following 2 h at pH 1.0, giving additional escape routes for the 5-FU.