Enhancement of felodipine dissolution rate through its incorporation into Eudragit® E-PHB polymeric microparticles: in vitro characterization and investigation of absorption in rats.

Giovana C Bazzo, Daniela B Caetano, Maura L T Boch, Mileine Mosca, Luiza C Branco, Melissa Zétola, Eduardo M Pereira, Bianca R Pezzini

Department of Pharmacy, Universidade da Região de Joinville (UNIVILLE), Joinville, Santa Catarina, Brazil. gbazzo@uol.com.br

Journal of pharmaceutical sciences 2012 Apr

filter terms:

In this study, felodipine was incorporated into microparticles prepared with Eudragit® E and it blended with poly(3-hydroxybutyrate) (PHB) using the emulsion-solvent evaporation technique, with the aim of improving the dissolution rate of the drug. The formulation prepared with Eudragit® E showed irregular and fragmented microparticles, with a loading efficiency (LE) of 82.6%. When the microparticles were prepared with a blend of Eudragit® E and PHB, they had a spherical form with a LE of 103.9%. X-ray diffraction and differential thermal analysis indicated a reduction in the crystallinity of felodipine after its incorporation into the microparticles, which caused a significant increase in the felodipine dissolution rate. An investigation into the absorption in rats was carried out using high-performance liquid chromatography analysis of the blood collected 20 and 60 min after the animals were administered felodipine [30 mg/Kg, orally (p.o.)] or felodipine microparticles (30 mg/Kg, p.o.). Animals that were given felodipine showed mean plasmatic levels of 0.0125 (±0.00156) and 0.0240 (±0.0069) μg mL(-1) after 20 and 60 min, respectively, whereas animals that received microparticles containing felodipine showed respective mean plasmatic levels of 0.0651 (±0.0120) and 0.0369 (±0.0145) μg mL(-1) . Our data suggest that the incorporation into microparticles significantly enhanced the release of felodipine, improving its absorption in rats. Copyright © 2012 Wiley Periodicals, Inc.

Citation

Giovana C Bazzo, Daniela B Caetano, Maura L T Boch, Mileine Mosca, Luiza C Branco, Melissa Zétola, Eduardo M Pereira, Bianca R Pezzini. Enhancement of felodipine dissolution rate through its incorporation into Eudragit® E-PHB polymeric microparticles: in vitro characterization and investigation of absorption in rats. Journal of pharmaceutical sciences. 2012 Apr;101(4):1518-23