Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 495, Issue 2, Pages 895-902Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2015.09.044
Keywords
Coaxial electrospinning; Eudragit; 5-Fluorouracil; Colon-targeted drug delivery
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Funding
- National Science Foundation of China [51373101]
- China NSFC/UK Royal Society [51411130128/IE131748]
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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. (C) 2015 Elsevier B.V. All rights reserved.
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