PCL/PHBV Microparticles as Innovative Carriers for Oral Controlled Release of Manidipine Dihydrochloride

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 efficie...

Full description

Saved in:
Bibliographic Details
Main Authors: Fernanda Malaquias Barboza, Willian Moreira Machado, Luiz Renato Olchanheski Junior, Josiane Padilha de Paula, Sônia Faria Zawadzki, Daniel Fernandes, Paulo Vitor Farago
Format: Article
Language:English
Published: Wiley 2014-01-01
Series:The Scientific World Journal
Online Access:http://dx.doi.org/10.1155/2014/268107
Tags: Add Tag
No Tags, Be the first to tag this record!
_version_ 1832551840136298496
author Fernanda Malaquias Barboza
Willian Moreira Machado
Luiz Renato Olchanheski Junior
Josiane Padilha de Paula
Sônia Faria Zawadzki
Daniel Fernandes
Paulo Vitor Farago
author_facet Fernanda Malaquias Barboza
Willian Moreira Machado
Luiz Renato Olchanheski Junior
Josiane Padilha de Paula
Sônia Faria Zawadzki
Daniel Fernandes
Paulo Vitor Farago
author_sort Fernanda Malaquias Barboza
collection DOAJ
description 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.
format Article
id doaj-art-dfc95a30ec6545b880a60697c5088c27
institution Kabale University
issn 2356-6140
1537-744X
language English
publishDate 2014-01-01
publisher Wiley
record_format Article
series The Scientific World Journal
spelling doaj-art-dfc95a30ec6545b880a60697c5088c272025-02-03T06:00:29ZengWileyThe Scientific World Journal2356-61401537-744X2014-01-01201410.1155/2014/268107268107PCL/PHBV Microparticles as Innovative Carriers for Oral Controlled Release of Manidipine DihydrochlorideFernanda Malaquias Barboza0Willian Moreira Machado1Luiz Renato Olchanheski Junior2Josiane Padilha de Paula3Sônia Faria Zawadzki4Daniel Fernandes5Paulo Vitor Farago6Laboratory 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, BrazilLaboratory 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, BrazilLaboratory 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, BrazilLaboratory 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, BrazilLaboratory 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, BrazilLaboratory 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, BrazilLaboratory 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, BrazilMicroparticles 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.http://dx.doi.org/10.1155/2014/268107
spellingShingle Fernanda Malaquias Barboza
Willian Moreira Machado
Luiz Renato Olchanheski Junior
Josiane Padilha de Paula
Sônia Faria Zawadzki
Daniel Fernandes
Paulo Vitor Farago
PCL/PHBV Microparticles as Innovative Carriers for Oral Controlled Release of Manidipine Dihydrochloride
The Scientific World Journal
title PCL/PHBV Microparticles as Innovative Carriers for Oral Controlled Release of Manidipine Dihydrochloride
title_full PCL/PHBV Microparticles as Innovative Carriers for Oral Controlled Release of Manidipine Dihydrochloride
title_fullStr PCL/PHBV Microparticles as Innovative Carriers for Oral Controlled Release of Manidipine Dihydrochloride
title_full_unstemmed PCL/PHBV Microparticles as Innovative Carriers for Oral Controlled Release of Manidipine Dihydrochloride
title_short PCL/PHBV Microparticles as Innovative Carriers for Oral Controlled Release of Manidipine Dihydrochloride
title_sort pcl phbv microparticles as innovative carriers for oral controlled release of manidipine dihydrochloride
url http://dx.doi.org/10.1155/2014/268107
work_keys_str_mv AT fernandamalaquiasbarboza pclphbvmicroparticlesasinnovativecarriersfororalcontrolledreleaseofmanidipinedihydrochloride
AT willianmoreiramachado pclphbvmicroparticlesasinnovativecarriersfororalcontrolledreleaseofmanidipinedihydrochloride
AT luizrenatoolchanheskijunior pclphbvmicroparticlesasinnovativecarriersfororalcontrolledreleaseofmanidipinedihydrochloride
AT josianepadilhadepaula pclphbvmicroparticlesasinnovativecarriersfororalcontrolledreleaseofmanidipinedihydrochloride
AT soniafariazawadzki pclphbvmicroparticlesasinnovativecarriersfororalcontrolledreleaseofmanidipinedihydrochloride
AT danielfernandes pclphbvmicroparticlesasinnovativecarriersfororalcontrolledreleaseofmanidipinedihydrochloride
AT paulovitorfarago pclphbvmicroparticlesasinnovativecarriersfororalcontrolledreleaseofmanidipinedihydrochloride