Resveratrol cross-linked chitosan loaded with phospholipid for controlled release and antioxidant activity

Int J Biol Macromol. 2016 Dec;93(Pt A):757-766. doi: 10.1016/j.ijbiomac.2016.09.018. Epub 2016 Sep 7.

Abstract

Despite the therapeutic effects of resveratrol, its clinical application is restricted by its poor oral bioavailability and low water solubility. To overcome these physicochemical and pharmacokinetic limitations, encapsulation of resveratrol (RV) into nanodevices has been explored. Resveratrol cross-linked chitosan nanoparticles modified with phospholipids (RVC-lipid) were synthesized using a double emulsion technique. The surface morphology of RVC-lipid nanoparticles was evaluated with field emission scanning electron microscopy (FESEM) and transmission electron microscopy (TEM). Particle size was measured using dynamic light scattering technique (DLS), X-ray diffraction (XRD) was performed to identify the crystallographic nature and Fourier transform infrared spectroscopy (FTIR) was used to measure changes in the chemical structures of the resveratrol and RVC-lipid nanoparticles. Results showed RVC-lipid nanoparticle had a characteristic amorphous structure, a mean particle sizes of 570nm in DI water and 950nm in ethanol, and an encapsulation efficiency of 63.82% in aqueous medium and 85.59% in ethanol medium. In-vitro release studies demonstrated a slow and sustained release of resveratrol governed by diffusion. Based on assays of antioxidant activity the scavenging activity of RVC-lipid nanoparticles was inferior to that of resveratrol due to its prolonged release. We concluded that phospholipids are the potential carriers for resveratrol.

Keywords: Antioxidant activity; Control release; Nanoparticles; Phospholipid; Resveratrol.

MeSH terms

  • Animals
  • Antioxidants* / chemistry
  • Antioxidants* / pharmacokinetics
  • Antioxidants* / pharmacology
  • Chitosan* / chemistry
  • Chitosan* / pharmacokinetics
  • Chitosan* / pharmacology
  • Delayed-Action Preparations / chemistry
  • Delayed-Action Preparations / pharmacokinetics
  • Delayed-Action Preparations / pharmacology
  • Mice
  • NIH 3T3 Cells
  • Phospholipids* / chemistry
  • Phospholipids* / pharmacokinetics
  • Phospholipids* / pharmacology
  • Resveratrol
  • Stilbenes* / chemistry
  • Stilbenes* / pharmacokinetics
  • Stilbenes* / pharmacology

Substances

  • Antioxidants
  • Delayed-Action Preparations
  • Phospholipids
  • Stilbenes
  • Chitosan
  • Resveratrol