title: PCL/PHBV microparticles as innovative carriers for oral controlled release of manidipine dihydrochloride.
abstract: Microparticles of poly(ε-caprolactone) (PCL) and poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) containing manidipine dihydrochloride (MAN) were successfully prepared by the simple emulsion/solvent evaporation method. All formulations showed loading efficiency rates greater than 80% and average particle size less than 8 μm. Formulations had spherical shape with smooth and porous surface for PCL and PHBV, respectively. According to Fourier-transform infrared spectroscopy, initial components were not chemically modified during microencapsulation. X-ray diffraction patterns and differential scanning calorimetry demonstrated that this process led to drug amorphization. In vitro dissolution studies showed that all microparticles prolonged MAN release, mainly which one obtained using PCL that contained 5% of drug loaded (PCL-M5). Animal studies demonstrated that formulation PCL-M5 was able to keep the variation of mean arterial pressure after phenylephrine administration up to 24 hours. These data confirmed the sustained antihypertensive effect of the investigated microparticles. Results provided an experimental basis for using formulation PCL-M5 as a feasible carrier for oral controlled release of MAN intended for treating high blood pressure.
authors.affiliation: Laboratory of Pharmaceutical Products, Postgraduate Program in Pharmaceutical Science, Department of Pharmaceutical Sciences, State University of Ponta Grossa, 4748 Carlos Cavalcanti Avenue, 84030-900 Ponta Grossa, PR, Brazil.
authors.forename: Fernanda Malaquias
authors.initials: FM
authors.lastname: Barboza
authors.affiliation: Laboratory of Cardiovascular Pharmacology, Postgraduate Program in Pharmaceutical Science, Department of Pharmaceutical Sciences, State University of Ponta Grossa, 4748 Carlos Cavalcanti Avenue, 84030-900 Ponta Grossa, PR, Brazil.
authors.forename: Willian Moreira
authors.initials: WM
authors.lastname: Machado
authors.affiliation: Laboratory of Cardiovascular Pharmacology, Postgraduate Program in Pharmaceutical Science, Department of Pharmaceutical Sciences, State University of Ponta Grossa, 4748 Carlos Cavalcanti Avenue, 84030-900 Ponta Grossa, PR, Brazil.
authors.forename: Luiz Renato
authors.identifier: 0000-0002-4931-2414
authors.initials: LR
authors.lastname: Olchanheski Junior
authors.affiliation: Laboratory of Pharmaceutical Products, Postgraduate Program in Pharmaceutical Science, Department of Pharmaceutical Sciences, State University of Ponta Grossa, 4748 Carlos Cavalcanti Avenue, 84030-900 Ponta Grossa, PR, Brazil.
authors.forename: Josiane
authors.initials: J
authors.lastname: Padilha de Paula
authors.affiliation: Laboratory of Synthetic Polymers, Postgraduate Program in Chemistry, Department of Chemistry, Federal University of Paraná, Centro Politécnico Jardim das Américas, P.O. Box 19081, 81531-990 Curitiba, PR, Brazil.
authors.forename: Sônia Faria
authors.initials: SF
authors.lastname: Zawadzki
authors.affiliation: Laboratory of Cardiovascular Pharmacology, Postgraduate Program in Pharmaceutical Science, Department of Pharmaceutical Sciences, State University of Ponta Grossa, 4748 Carlos Cavalcanti Avenue, 84030-900 Ponta Grossa, PR, Brazil.
authors.forename: Daniel
authors.identifier: 0000-0002-8935-4176
authors.initials: D
authors.lastname: Fernandes
authors.affiliation: Laboratory of Pharmaceutical Products, Postgraduate Program in Pharmaceutical Science, Department of Pharmaceutical Sciences, State University of Ponta Grossa, 4748 Carlos Cavalcanti Avenue, 84030-900 Ponta Grossa, PR, Brazil.
authors.forename: Paulo Vitor
authors.identifier: 0000-0002-9934-4027
authors.initials: PV
authors.lastname: Farago
mesh_terms: D000818:Animals; D000959:Antihypertensive Agents / Q000008:administration & dosage / Q000493:pharmacokinetics; D003692:Delayed-Action Preparations; D004095:Dihydropyridines / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D004337:Drug Carriers / Q000737:chemistry*; D005260:Female; D009578:Nitrobenzenes; D010316:Particle Size; D010879:Piperazines; D011091:Polyesters / Q000737:chemistry*; D051381:Rats; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties; D013816:Thermodynamics; D014961:X-Ray Diffraction; D000094122:Polyhydroxybutyrates
chemical_list: D000959:Antihypertensive Agents; D003692:Delayed-Action Preparations; D004095:Dihydropyridines; D004337:Drug Carriers; D009578:Nitrobenzenes; D010879:Piperazines; D011091:Polyesters; C052620:poly(3-hydroxybutyrate)-co-(3-hydroxyvalerate); D000094122:Polyhydroxybutyrates; C016240:polycaprolactone; C054218:manidipine