PHBV/PCL microparticles for controlled release of resveratrol: physicochemical characterization, antioxidant potential, and effect on hemolysis of human erythrocytes

ScientificWorldJournal. 2012:2012:542937. doi: 10.1100/2012/542937. Epub 2012 May 1.

Abstract

Microparticles of poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) and poly(ε-caprolactone) (PCL) containing resveratrol were successfully prepared by simple emulsion/solvent evaporation. All formulations showed suitable encapsulation efficiency values higher than 80%. PHBV microparticles revealed spherical shape with rough surface and presence of pores. PCL microparticles were spherically shaped with smooth surface. Fourier-transformed infrared spectra demonstrated no chemical bond between resveratrol and polymers. X-ray powder diffraction patterns and differential scanning calorimetry analyses indicated that microencapsulation led to drug amorphization. These PHBV/PCL microparticles delayed the dissolution profile of resveratrol. Release profiles were better fitted to biexponential equation. The hypochlorous-acid-scavenging activity and 2,2-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation discoloration assay confirmed that the antioxidant activity of PHBV/PCL microparticles was kept, but was dependent on the microparticle morphology and dissolution profile. Resveratrol-loaded PHBV/PCL microparticles showed no cytotoxic effect on red blood cells.

MeSH terms

  • Antioxidants / administration & dosage*
  • Antioxidants / pharmacology
  • Calorimetry, Differential Scanning
  • Drug Carriers*
  • Erythrocytes / drug effects*
  • Hemolysis / drug effects*
  • Humans
  • Microscopy, Electron, Scanning
  • Particle Size
  • Polyesters / administration & dosage*
  • Resveratrol
  • Stilbenes / administration & dosage*
  • Stilbenes / pharmacology
  • Thermogravimetry

Substances

  • Antioxidants
  • Drug Carriers
  • Polyesters
  • Stilbenes
  • poly(3-hydroxybutyrate)-co-(3-hydroxyvalerate)
  • polycaprolactone
  • Resveratrol