Effect of ibuprofen entrapment procedure on physicochemical and controlled drug release performances of chitosan/xanthan gum polyelectrolyte complexes

Int J Biol Macromol. 2021 Jan 15:167:547-558. doi: 10.1016/j.ijbiomac.2020.11.201. Epub 2020 Dec 2.

Abstract

The effect of the entrapment procedure of a poorly water soluble drug (ibuprofen) on physicochemical and drug release performances of chitosan/xanthan polyelectrolyte complexes (PECs) was investigated to achieve controlled drug release as the ultimate goal. The formation of PECs for two drug entrapment procedures (before or after the mixing of polymers) at pH 4.6 and 5.6 and three chitosan-to-xanthan mass ratios (1:1, 1:2 and 1:3) was observed by continuous decrease in conductivity during the PECs formation and increased apparent viscosity and hysteresis values. The most extensive crosslinking was observed with ibuprofen added before the PECs formation at pH 4.6 and chitosan-to-xanthan mass ratio 1:1. The PECs prepared at polymers' mass ratios 1:2 and 1:3 had higher yield and drug entrapment efficiency. DSC and FT-IR analysis confirmed ibuprofen entrapment in PECs and the partial disruption of its crystallinity. All ibuprofen release profiles were similar, with 60-70% of drug released after 12 h, mainly by diffusion, but erosion and polymer chain relaxation were also included. Potentially optimal can be considered the PEC prepared at pH 4.6, ibuprofen entrapped before the mixing of polymers at chitosan-to-xanthan mass ratio 1:2, which provided controlled drug release by zero-order kinetics, high yield, and drug entrapment efficiency.

Keywords: Chitosan; Controlled drug release; Drug entrapment; Polyelectrolyte complex; Polymer crosslinking; Xanthan gum.

MeSH terms

  • Chitosan / chemistry*
  • Delayed-Action Preparations
  • Hydrogen-Ion Concentration
  • Ibuprofen / chemistry
  • Ibuprofen / pharmacokinetics*
  • Polyelectrolytes / chemistry
  • Polysaccharides, Bacterial / chemistry*
  • Spectroscopy, Fourier Transform Infrared
  • Viscosity

Substances

  • Delayed-Action Preparations
  • Polyelectrolytes
  • Polysaccharides, Bacterial
  • Chitosan
  • xanthan gum
  • Ibuprofen