PHBV/PCL microparticles for controlled release of resveratrol: physicochemical characterization, antioxidant potential, and effect on hemolysis of human erythrocytes.
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.
Postgraduate Program in Pharmaceutical Sciences, Department of Pharmaceutical Sciences, State University of Ponta Grossa, 4748 Carlos Cavalcanti Avenue, 84030-900 Ponta Grossa, Brazil.
Jessica Bitencourt Emilio
JB
Mendes
Manoela Klüppel
MK
Riekes
Viviane Matoso
VM
de Oliveira
Milton Domingos
MD
Michel
Hellen Karine
HK
Stulzer
Najeh Maissar
NM
Khalil
Sônia Faria
SF
Zawadzki
Rubiana Mara
RM
Mainardes
Paulo Vitor
PV
Farago
D000975:Antioxidants / Q000008:administration & dosage* / Q000494:pharmacology; D002152:Calorimetry, Differential Scanning; D004337:Drug Carriers; D004912:Erythrocytes / Q000187:drug effects*; D006461:Hemolysis / Q000187:drug effects*; D006801:Humans; D008855:Microscopy, Electron, Scanning; D010316:Particle Size; D011091:Polyesters / Q000008:administration & dosage*; D000077185:Resveratrol; D013267:Stilbenes / Q000008:administration & dosage* / Q000494:pharmacology; D013818:Thermogravimetry; D000094122:Polyhydroxybutyrates
D000975:Antioxidants; D004337:Drug Carriers; D011091:Polyesters; D000077185:Resveratrol; D013267:Stilbenes; C052620:poly(3-hydroxybutyrate)-co-(3-hydroxyvalerate); D000094122:Polyhydroxybutyrates; C016240:polycaprolactone