PHBV/PCL Microparticles for Controlled Release of Resveratrol: Physicochemical Characterization, Antioxidant Potential, and Effect on Hemolysis of Human Erythrocytes

• Published in: TheScientificWorld Vol. 2012; no. 2012; pp. 1 - 13
• Main Authors: Farago, Paulo Vitor, Mainardes, Rubiana Mara, Khalil, Najeh Maissar, Stulzer, Hellen Karine, Michel, Milton Domingos, de Oliveira, Viviane Matoso, Riekes, Manoela Klüppel, Mendes, Jessica Bitencourt Emilio, Zawadzki, Sônia Faria
• Format: Journal Article
• Language: English
• Published: Cairo, Egypt Hindawi Publishing Corporation 01.01.2012; The Scientific World Journal; Hindawi Limited; Wiley
• Subjects: Amorphization; Antioxidants; Antioxidants - administration & dosage; Antioxidants - pharmacology; Bioavailability; Calorimetry; Calorimetry, Differential Scanning; Cell research; Chemical bonds; Controlled release; Cytotoxicity; Differential scanning calorimetry; Diffraction patterns; Discoloration; Dissolution; Drug Carriers; Engineering; Erythrocytes; Erythrocytes - drug effects; Evaporation; Formulations; Fourier transforms; Free radicals; Health aspects; Hemolysis - drug effects; Hemolysis and hemolysins; Humans; Infrared spectra; Lipids; Metabolism; Microencapsulation; Microparticles; Microscopy, Electron, Scanning; Nanoparticles; Oxidation; Oxidative stress; Particle Size; Pharmaceutical sciences; Pharmacy; Polyesters; Polyesters - administration & dosage; Polymers; Resveratrol; Rodents; Stilbenes - administration & dosage; Stilbenes - pharmacology; Sulfonic acid; Temperature; Thermogravimetry; X ray powder diffraction; Brazil; Rio de Janeiro Brazil
• ISSN: 2356-6140; 1537-744X; 1537-744X
• DOI: 10.1100/2012/542937

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.