Gastrointestinal transition and anti-diabetic effect of Isabgol husk microparticles containing gliclazide

Int J Biol Macromol. 2014 May:66:15-25. doi: 10.1016/j.ijbiomac.2014.02.014. Epub 2014 Feb 14.

Abstract

Isabgol husk with sodium alginate was formulated into gliclazide loaded microparticles which were characterized for particle size, swelling index, entrapment efficiency, in vitro release, release kinetics, stability, hypoglycemic effect, surface morphology, and gastrointestinal transition. The particle size in different formulations varied from 752.83 ± 0.630 to 872.03 ± 0.293 μm. It was analyzed by dissolution study that up to 98% of loaded gliclazide was released in simulated intestinal fluid (SIF, pH 7.4) within 8h. The formulations containing sodium alginate and Isabgol husk-sodium alginate showed bioequivalency with marketed sustained release tablets (Glizid MR 60(®)) in terms of release pattern. The drug maintained its integrity in terms of functional groups after fabrication in formulations as observed by FTIR analysis. The hypoglycemic effect of gliclazide loaded Isabgol husk-sodium alginate microparticles was found to be 37 ± 6.356% in terms of changes of blood glucose level from base glucose level (100%) in diabetic condition after 24h of oral administration and it was more than marketed conventional tablets (95.5 ± 3.286%). The retention of microparticles was observed in small intestine up to 10h during whole body X-ray imaging. The study revealed that microparticles composing of Isabgol husk may have the potential for regulating blood glucose level in diabetic animals with controlled release of gliclazide.

Keywords: Cross-linking; In vitro release; Isabgol husk; X-ray imaging.

MeSH terms

  • Alginates / chemistry
  • Animals
  • Blood Glucose / drug effects
  • Chemistry, Pharmaceutical / methods
  • Delayed-Action Preparations / chemistry
  • Delayed-Action Preparations / pharmacology
  • Diabetes Mellitus, Experimental / drug therapy
  • Diabetes Mellitus, Experimental / metabolism
  • Drug Carriers / chemistry
  • Gliclazide / chemistry*
  • Gliclazide / pharmacology*
  • Glucose / metabolism
  • Glucuronic Acid / chemistry
  • Hexuronic Acids / chemistry
  • Hypoglycemic Agents / chemistry*
  • Hypoglycemic Agents / pharmacology*
  • Intestine, Small / metabolism*
  • Microspheres
  • Particle Size
  • Psyllium / chemistry*
  • Psyllium / pharmacology*
  • Rabbits
  • Solubility
  • Tablets / chemistry
  • Tablets / pharmacology

Substances

  • Alginates
  • Blood Glucose
  • Delayed-Action Preparations
  • Drug Carriers
  • Hexuronic Acids
  • Hypoglycemic Agents
  • Tablets
  • Psyllium
  • Glucuronic Acid
  • Gliclazide
  • Glucose