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...
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Language: | English |
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2014-01-01
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Series: | The Scientific World Journal |
Online Access: | http://dx.doi.org/10.1155/2014/268107 |
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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 |
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