Preparation and characterization of antioxidant nanoparticles composed of chitosan and fucoidan for antibiotics delivery

Mar Drugs. 2014 Jul 31;12(8):4379-98. doi: 10.3390/md12084379.

Abstract

In this study, we developed novel chitosan/fucoidan nanoparticles (CS/F NPs) using a simple polyelectrolyte self-assembly method and evaluated their potential to be antioxidant carriers. As the CS/F weight ratio was 5/1, the CS/F NPs were spherical and exhibited diameters of approximately 230-250 nm, as demonstrated by TEM. These CS/F NPs maintained compactness and stability for 25 day in phosphate-buffered saline (pH 6.0-7.4). The CS/F NPs exhibited highly potent antioxidant effects by scavenging 1,1-diphenyl-2-picrylhydrazyl (DPPH), reducing the concentration of intracellular reactive oxygen species (ROS) and superoxide anion (O2-) in stimulated macrophages. The DPPH scavenging effect of CS/F NPs primarily derives from fucoidan. Furthermore, these CS/F NPs activated no host immune cells into inflammation-mediated cytotoxic conditions induced by IL-6 production and NO generation. The MTT cell viability assay revealed an absence of toxicity in A549 cells after exposure to the formulations containing 0.375 mg NPs/mL to 3 mg NPs/mL. Gentamicin (GM), an antibiotic, was used as a model drug for an in vitro releasing test. The CS/F NPs controlled the release of GM for up to 72 h, with 99% of release. The antioxidant CS/F NPs prepared in this study could thus be effective in delivering antibiotics to the lungs, particularly for airway inflammatory diseases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Bacterial Agents / administration & dosage*
  • Anti-Bacterial Agents / chemistry*
  • Antioxidants / administration & dosage
  • Antioxidants / chemistry*
  • Biphenyl Compounds / chemistry
  • Cell Line
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Chitosan / chemistry*
  • Drug Carriers / chemistry
  • Humans
  • Hydrogen-Ion Concentration
  • Interleukin-6 / metabolism
  • Macrophages / drug effects
  • Mice
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry*
  • Nitric Oxide / chemistry
  • Particle Size
  • Picrates / chemistry
  • Polysaccharides / administration & dosage
  • Polysaccharides / chemistry*
  • Reactive Oxygen Species / metabolism
  • Superoxides / metabolism

Substances

  • Anti-Bacterial Agents
  • Antioxidants
  • Biphenyl Compounds
  • Drug Carriers
  • Interleukin-6
  • Picrates
  • Polysaccharides
  • Reactive Oxygen Species
  • Superoxides
  • Nitric Oxide
  • Chitosan
  • fucoidan
  • 1,1-diphenyl-2-picrylhydrazyl