Preparation and evaluation of chitosan-based nanogels/gels for oral delivery of myricetin

Eur J Pharm Sci. 2016 Aug 25:91:144-53. doi: 10.1016/j.ejps.2016.06.014. Epub 2016 Jun 18.

Abstract

A novel nanogel/gel based on chitosan (CS) for the oral delivery of myricetin (Myr) was developed and evaluated comprehensively. The particle size of the obtained Myr-loaded CS/β-glycerol phosphate (β-GP) nanogels was in the range of 100-300nm. The rheological tests showed that the sol-gel transition happened when the nanogels were exposed to physiological temperatures, and 3D network structures of the gelatinized nanogels (gels) were confirmed by Scanning Electron Microscopy. Myr was released from CS/β-GP nanogel/gel in acidic buffers via a Fickian mechanism, and this release was simultaneously accompanied by swelling and erosion. Moreover, the nanogel/gel exhibited no cytotoxicity by MTT assay, and the oral bioavailability of Myr in rats was improved with an accelerated absorption rate after Myr was loaded into CS/β-GP nanogel/gel. In summary, all of the above showed that CS/β-GP nanogel/gel was an excellent system for orally delivering Myr.

Keywords: Chitosan; In vitro release; Myricetin; Nanogels; Pharmacokinetics; β-glycerol phosphate.

MeSH terms

  • Administration, Oral
  • Animals
  • Biological Availability
  • Caco-2 Cells
  • Cell Survival / drug effects
  • Chitosan / administration & dosage*
  • Chitosan / chemistry
  • Chitosan / pharmacokinetics
  • Drug Compounding
  • Drug Liberation
  • Flavonoids / administration & dosage*
  • Flavonoids / chemistry
  • Flavonoids / pharmacokinetics
  • Gels
  • Glycerophosphates / administration & dosage*
  • Glycerophosphates / chemistry
  • Glycerophosphates / pharmacokinetics
  • Humans
  • Microscopy, Electron, Scanning
  • Nanoparticles / administration & dosage*
  • Nanoparticles / chemistry
  • Nanoparticles / ultrastructure
  • Particle Size
  • Rats, Sprague-Dawley
  • Rheology

Substances

  • Flavonoids
  • Gels
  • Glycerophosphates
  • myricetin
  • Chitosan
  • beta-glycerophosphoric acid