5-Fluorouracil loaded Eudragit fibers prepared by electrospinning

Area of Science:

• Materials Science
• Pharmaceutical Sciences
• Drug Delivery

Background:

• Core/shell electrospun fibers offer potential for controlled drug release.
• Eudragit S100 (ES-100) is an enteric polymer insoluble at low pH.
• 5-fluorouracil (5-FU) is a widely used chemotherapeutic agent.

Purpose of the Study:

• To investigate the drug release profile of 5-fluorouracil (5-FU) from core/shell electrospun fibers with Eudragit S100 (ES-100) shells.
• To evaluate the integrity and drug release behavior of these fibers in acidic conditions (pH 1.0).

Main Methods:

• Fabrication of 5-FU loaded core/shell electrospun fibers using various core materials (poly(vinylpyrrolidone), ethyl cellulose, ES-100, or drug alone).
• Preparation of monolithic ES-100 fibers for comparison.
• Characterization using electron microscopy to assess fiber morphology and core-shell structure.
• Dissolution studies conducted at pH 1.0 to quantify drug release over time.

Main Results:

• Electron microscopy confirmed smooth cylindrical fibers with visible core-shell structures, except for monolithic fibers.
• All materials contained 5-FU in an amorphous physical form.
• Significant 5-FU release (30-80% of maximum) occurred within 2 hours at pH 1.0, despite ES-100 insolubility.
• Fiber degradation (breaking/merging) was observed at pH 1.0, facilitating additional drug release.

Conclusions:

• The Eudragit S100 shell did not effectively prevent 5-FU release at pH 1.0.
• Low molecular weight and high acid solubility of 5-FU, coupled with fiber degradation, contributed to premature drug release.
• These findings highlight limitations in using ES-100 for immediate-release formulations at low pH.