Co-encapsulated resveratrol and quercetin in chitosan and peg modified chitosan nanoparticles: For efficient intra ocular pressure reduction

Int J Biol Macromol. 2017 Nov;104(Pt B):1837-1845. doi: 10.1016/j.ijbiomac.2017.04.117. Epub 2017 May 1.

Abstract

Natural anti-oxidants resveratrol (RES) and quercetin (QUR) posses the ability to reduce intra ocular pressure efficiently. Concurrent administration of RES and QUR was able to enhance the bioavailability of RES. Present research work describes upsurge of QUR in RES loaded chitosan (CS) nanoparticles (NPs) and polyethylene glycol (PEG) modified CS NPs for improved delivery and synergic effects on reducing intra ocular pressure for the treatment of glaucoma. CS NPs and PEG modified CS NPs were prepared by ionic gelation of tripolyphosphate and CS. The synthesised NPs were spherical in shape and RES entrapment and loading efficiency in the formulation decreased with increasing PEG concentration. Particle size of the formulation increased while incorporating PEG and drugs. The crystalline nature of RES and QUR changed in the NPs and that was confirmed by XRD study. Free radical neutralising efficiency improved while incorporating QUR in the formulation. Ex-vivo corneal permeation of RES was higher from RES and QUR loaded formulation than RES alone containing NPs and free RES dispersion. RES and QUR loaded PEG modified CS NPs showed sustained and enhanced reduction of intra ocular pressure (5.5±0.5mmHg) in normotensive rabbits.

Keywords: Chitosan; Quercetin; Resveratrol.

MeSH terms

  • Animals
  • Antioxidants / chemistry
  • Antioxidants / pharmacology
  • Chickens
  • Chitosan / chemistry*
  • Drug Carriers / chemistry
  • Drug Compounding*
  • Drug Liberation
  • Hydrogen-Ion Concentration
  • Intraocular Pressure / drug effects
  • Nanoparticles / chemistry*
  • Nanoparticles / ultrastructure
  • Osmolar Concentration
  • Particle Size
  • Polyethylene Glycols / chemistry*
  • Quercetin / chemistry*
  • Quercetin / pharmacology
  • Rabbits
  • Resveratrol
  • Spectroscopy, Fourier Transform Infrared
  • Stilbenes / chemistry*
  • Stilbenes / pharmacology

Substances

  • Antioxidants
  • Drug Carriers
  • Stilbenes
  • Polyethylene Glycols
  • Chitosan
  • Quercetin
  • Resveratrol