Application of pH-Responsive Fucoidan/Chitosan Nanoparticles to Improve Oral Quercetin Delivery

Molecules. 2019 Jan 18;24(2):346. doi: 10.3390/molecules24020346.

Abstract

Polymeric nanoparticles based on fucoidan and chitosan were developed to deliver quercetin as a novel functional food. Through the polyelectrolyte self-assembly method, fucoidan/chitosan (F/C) nanoparticles were obtained with three different weight ratios (1/1, 3/1, and 5/1). The content of quercetin in the fucoidan/chitosan nanoparticles was in the range 110 ± 3 to 335 ± 4 mg·mL-1, with the increase of weight ratio of fucoidan to chitosan in the nanoparticle. Physicochemically stable nanoparticles were obtained with a particle size within the 300⁻400 nm range and surface potential higher than +30 mV for the 1F/1C ratio nanoparticle and around -30 mV for the 3F/1C and 5F/1C ratios nanoparticles. The 1F/1C ratio nanoparticle became larger and more unstable as the pH increased from 2.5 to 7.4, while the 3F/1C and 5F/1C nanoparticles retained their initial characteristics. This result indicates that the latter nanoparticles were stable along the gastrointestinal tract. The quercetin-loaded fucoidan/chitosan nanoparticles showed strong antioxidant activity and controlled release under simulated gastrointestinal environments (in particular for the 3F/1C and 5F/1C ratios), preventing quercetin degradation and increasing its oral bioavailability.

Keywords: antioxidant activity; in vitro release; marine polysaccharides; pH-sensitive nanoparticles.

MeSH terms

  • Antioxidants / administration & dosage
  • Antioxidants / pharmacokinetics
  • Chemical Phenomena
  • Chitosan / chemistry*
  • Drug Carriers / chemistry*
  • Drug Delivery Systems
  • Drug Liberation
  • Hydrogen-Ion Concentration
  • Nanoparticles / chemistry*
  • Nanoparticles / ultrastructure
  • Particle Size
  • Polysaccharides / chemistry*
  • Quercetin / administration & dosage*
  • Quercetin / pharmacokinetics*
  • Spectroscopy, Fourier Transform Infrared

Substances

  • Antioxidants
  • Drug Carriers
  • Polysaccharides
  • Chitosan
  • fucoidan
  • Quercetin