Thiolation of arabinoxylan and its application in the fabrication of pH-sensitive thiolated arabinoxylan grafted acrylic acid copolymer

Drug Dev Ind Pharm. 2019 May;45(5):754-766. doi: 10.1080/03639045.2019.1569041. Epub 2019 Feb 11.

Abstract

Current research work was conducted to synthesize Thiol modified arabinoxylan and its application in fabrication of hydrogel. Thioglycolic acid was esterified with arabinoxylan to prepare Thiolatedarabinoxylan. Appearance of peak at 2533.34 cm-1 in FTIR and thiol content showed successful thiolation. The pH-dependent Thiolatedarabinoxylan/acrylic acid (TAX/AA) hydrogels of perindopril erbumine were prepared via free-radical co-polymerization. Perindopril erbumine (PE) was employed as model drug. Different batches with different feed ratio of TAX, AA, and MBA were prepared and their influence on swelling, solvent penetration, and consequent drug release was investigated. Swelling coefficients increased with increase in pH. TAX/AA hydrogels were characterized by Fourier-transform infrared spectroscopy (FT-IR), Thermal Analysis (TA), X-Ray diffraction (XRD), and scanning electron microscope (SEM). Dissolution studies were performed at pH 1.2 and 7.4 in which drug release showed direct correlation with TAX and AA ratio. In vivo studies showed that Cmax of TAX-co-AA based hydrogel was 81.57 ± 0.35 ng/ml which was maintained for a longer time after its administration. All the results of in vivo studies were significant and TAX-co-AA based hydrogel enhances the bioavailability of perindopril erbumine.

Keywords: Hydrogel; perindopril erbumine (PE); thiolatedarabinoxylan (TAX).

MeSH terms

  • Acrylates / chemistry*
  • Animals
  • Biological Availability
  • Drug Carriers / chemistry*
  • Drug Liberation
  • Hydrogels / chemistry
  • Hydrogen-Ion Concentration
  • Perindopril / administration & dosage
  • Perindopril / pharmacokinetics*
  • Plantago / chemistry
  • Rabbits
  • Thioglycolates / chemistry
  • Xylans / chemistry*
  • Xylans / isolation & purification

Substances

  • Acrylates
  • Drug Carriers
  • Hydrogels
  • Thioglycolates
  • Xylans
  • 2-mercaptoacetate
  • arabinoxylan
  • acrylic acid
  • Perindopril