Chitosan-sodium lauryl sulfate/Eudragit S100 beads loaded with 5-fluorouracil: Influence of solvent and duration of crosslinking the crosslinking on physicochemical properties

Abstract

Chitosan beads loaded with 5-fluorouracil (5-FU) were prepared by ionotropic gelation using sodium lauryl sulfate (SLS) as a crosslinking agent in presences of Eudragit S100. The objective was to improve the loading and sustained release of 5-FU. The influence of the solvent system, counter ion concentration, crosslinking time, and addition of Eudragit on particle size, drug loading, entrapment efficiency (E.E.), and in vitro release was investigated. The beads were also characterized by scanning electron microscopy, Fourier transform infrared (FTIR), and thermogravimetric analysis (TGA). Spherical beads were produced with at least 2% SLS, and the resultant particle size was smaller with higher SLS concentration. FTIR has confirmed the incorporation of 5-FU and the electrostatic interaction involved in the formation of chitosan/SLS/Eudragit beads. TGA graph has shown a sharp weight loss between 225 °C and 250 °C in beads prepared with an alcoholic crosslinking solution. The amorphous nature of the entrapped drug was also revealed in the TGA. All batches exhibited 5-FU burst release within 30 min, and beads prepared with 2% SLS/Eudragit has displayed a sustained release up to 4 h in a dissolution medium of increasing pH. Further, the E.E. of 5-FU was increased with hydroalcoholic solvent, lower SLS concentration, and shorter crosslinking time.

Keywords

• Chitosan
• sodium lauryl sulfate
• Eudragit S100
• 5-fluorouracil
• ionotropic gelation
• drug loading