Novel carvedilol paediatric nanomicelle formulation:in-vitro characterization and in-vivo evaluation

Autores
Wegmann, Marcel; Parola, Luciano; Bertera, Facundo Martin; Taira, Carlos Alberto; Cagel, Carlos Maximiliano; Buontempo, Fabián; Bernabeu, Ezequiel Adrian; Höcht, Christian; Chiappetta, Diego Andrés; Moretton, Marcela Analía
Año de publicación
2017
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Objectives Carvedilol (CAR) is a poorly water-soluble beta-blocker. Its encapsu-lation within nanomicelles (NMs) could improve drug solubility and its oralbioavailability, allowing the development of a paediatric liquid CAR formulationwith commercially available copolymers: D-a-tocopheryl polyethylene glycol1000 succinate (TPGS) and poly(vinyl caprolactam)-poly(vinyl acetate)-poly(ethylene glycol) (Soluplusâ).Methods Drug-loaded NMs were prepared by copolymer and CAR dispersion indistilled water. Micellar size and morphology were characterized by dynamic lightscattering and transmission electron microscopy, respectively. In-vitro drug per-meation studies were evaluated by conventional gut sac method. In-vivo CARoral bioavailability from NMs dispersions and drug control solution was evalu-ated in Wistar rats.Key findings Carvedilol apparent aqueous solubility was increased (up to 60.4-folds) after its encapsulation within NMs. The micellar size was ranged between10.9 and 81.9 nm with a monomodal size distribution. There was a significantenhancement of CAR relative oral bioavailability for both copolymers vs amicelle-free drug solution (P < 0.05). This improvement was higher for TPGS-based micelles (4.95-fold) in accordance with the in-vitro CAR permeationresults.Conclusions The present investigation demonstrates the development of highlyconcentrated CAR liquid micellar formulation. The improvement on drug oralbioavailability contributes to the potential of this NMs formulation to enhanceCAR paediatric treatment.
Fil: Wegmann, Marcel. Hochschule Furtwangen University; Alemania
Fil: Parola, Luciano. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina
Fil: Bertera, Facundo Martin. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina
Fil: Taira, Carlos Alberto. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina
Fil: Cagel, Carlos Maximiliano. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina
Fil: Buontempo, Fabián. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica; Argentina
Fil: Bernabeu, Ezequiel Adrian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina
Fil: Höcht, Christian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina
Fil: Chiappetta, Diego Andrés. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina
Fil: Moretton, Marcela Analía. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica; Argentina
Materia
CARVEDILOL
NANOMICELLES
NANOTECHNOLOGY
ORAL BIOAVAILABILITY
PAEDIATRIC PHARMACOTHERAPY
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/156756
Acceder
id CONICETDig_9e86f97c70903bb45777316ebfd09ec7
oai_identifier_str oai:ri.conicet.gov.ar:11336/156756
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Novel carvedilol paediatric nanomicelle formulation:in-vitro characterization and in-vivo evaluationWegmann, MarcelParola, LucianoBertera, Facundo MartinTaira, Carlos AlbertoCagel, Carlos MaximilianoBuontempo, FabiánBernabeu, Ezequiel AdrianHöcht, ChristianChiappetta, Diego AndrésMoretton, Marcela AnalíaCARVEDILOLNANOMICELLESNANOTECHNOLOGYORAL BIOAVAILABILITYPAEDIATRIC PHARMACOTHERAPYhttps://purl.org/becyt/ford/3.1https://purl.org/becyt/ford/3Objectives Carvedilol (CAR) is a poorly water-soluble beta-blocker. Its encapsu-lation within nanomicelles (NMs) could improve drug solubility and its oralbioavailability, allowing the development of a paediatric liquid CAR formulationwith commercially available copolymers: D-a-tocopheryl polyethylene glycol1000 succinate (TPGS) and poly(vinyl caprolactam)-poly(vinyl acetate)-poly(ethylene glycol) (Soluplusâ).Methods Drug-loaded NMs were prepared by copolymer and CAR dispersion indistilled water. Micellar size and morphology were characterized by dynamic lightscattering and transmission electron microscopy, respectively. In-vitro drug per-meation studies were evaluated by conventional gut sac method. In-vivo CARoral bioavailability from NMs dispersions and drug control solution was evalu-ated in Wistar rats.Key findings Carvedilol apparent aqueous solubility was increased (up to 60.4-folds) after its encapsulation within NMs. The micellar size was ranged between10.9 and 81.9 nm with a monomodal size distribution. There was a significantenhancement of CAR relative oral bioavailability for both copolymers vs amicelle-free drug solution (P < 0.05). This improvement was higher for TPGS-based micelles (4.95-fold) in accordance with the in-vitro CAR permeationresults.Conclusions The present investigation demonstrates the development of highlyconcentrated CAR liquid micellar formulation. The improvement on drug oralbioavailability contributes to the potential of this NMs formulation to enhanceCAR paediatric treatment.Fil: Wegmann, Marcel. Hochschule Furtwangen University; AlemaniaFil: Parola, Luciano. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; ArgentinaFil: Bertera, Facundo Martin. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; ArgentinaFil: Taira, Carlos Alberto. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; ArgentinaFil: Cagel, Carlos Maximiliano. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; ArgentinaFil: Buontempo, Fabián. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica; ArgentinaFil: Bernabeu, Ezequiel Adrian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; ArgentinaFil: Höcht, Christian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; ArgentinaFil: Chiappetta, Diego Andrés. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; ArgentinaFil: Moretton, Marcela Analía. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica; ArgentinaPharmaceutical Press-Royal Pharmaceutical Society Great Britian2017-06info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/156756Wegmann, Marcel; Parola, Luciano; Bertera, Facundo Martin; Taira, Carlos Alberto; Cagel, Carlos Maximiliano; et al.; Novel carvedilol paediatric nanomicelle formulation:in-vitro characterization and in-vivo evaluation; Pharmaceutical Press-Royal Pharmaceutical Society Great Britian; Journal of Pharmacy and Pharmacology; 69; 6-2017; 544-5530022-3573CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/https://academic.oup.com/jpp/article/69/5/544/6128976info:eu-repo/semantics/altIdentifier/doi/10.1111/jphp.12605info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-10-22T12:02:44Zoai:ri.conicet.gov.ar:11336/156756instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-10-22 12:02:45.002CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Novel carvedilol paediatric nanomicelle formulation:in-vitro characterization and in-vivo evaluation
title Novel carvedilol paediatric nanomicelle formulation:in-vitro characterization and in-vivo evaluation
spellingShingle Novel carvedilol paediatric nanomicelle formulation:in-vitro characterization and in-vivo evaluation
Wegmann, Marcel
CARVEDILOL
NANOMICELLES
NANOTECHNOLOGY
ORAL BIOAVAILABILITY
PAEDIATRIC PHARMACOTHERAPY
title_short Novel carvedilol paediatric nanomicelle formulation:in-vitro characterization and in-vivo evaluation
title_full Novel carvedilol paediatric nanomicelle formulation:in-vitro characterization and in-vivo evaluation
title_fullStr Novel carvedilol paediatric nanomicelle formulation:in-vitro characterization and in-vivo evaluation
title_full_unstemmed Novel carvedilol paediatric nanomicelle formulation:in-vitro characterization and in-vivo evaluation
title_sort Novel carvedilol paediatric nanomicelle formulation:in-vitro characterization and in-vivo evaluation
dc.creator.none.fl_str_mv Wegmann, Marcel
Parola, Luciano
Bertera, Facundo Martin
Taira, Carlos Alberto
Cagel, Carlos Maximiliano
Buontempo, Fabián
Bernabeu, Ezequiel Adrian
Höcht, Christian
Chiappetta, Diego Andrés
Moretton, Marcela Analía
author Wegmann, Marcel
author_facet Wegmann, Marcel
Parola, Luciano
Bertera, Facundo Martin
Taira, Carlos Alberto
Cagel, Carlos Maximiliano
Buontempo, Fabián
Bernabeu, Ezequiel Adrian
Höcht, Christian
Chiappetta, Diego Andrés
Moretton, Marcela Analía
author_role author
author2 Parola, Luciano
Bertera, Facundo Martin
Taira, Carlos Alberto
Cagel, Carlos Maximiliano
Buontempo, Fabián
Bernabeu, Ezequiel Adrian
Höcht, Christian
Chiappetta, Diego Andrés
Moretton, Marcela Analía
author2_role author
author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv CARVEDILOL
NANOMICELLES
NANOTECHNOLOGY
ORAL BIOAVAILABILITY
PAEDIATRIC PHARMACOTHERAPY
topic CARVEDILOL
NANOMICELLES
NANOTECHNOLOGY
ORAL BIOAVAILABILITY
PAEDIATRIC PHARMACOTHERAPY
purl_subject.fl_str_mv https://purl.org/becyt/ford/3.1
https://purl.org/becyt/ford/3
dc.description.none.fl_txt_mv Objectives Carvedilol (CAR) is a poorly water-soluble beta-blocker. Its encapsu-lation within nanomicelles (NMs) could improve drug solubility and its oralbioavailability, allowing the development of a paediatric liquid CAR formulationwith commercially available copolymers: D-a-tocopheryl polyethylene glycol1000 succinate (TPGS) and poly(vinyl caprolactam)-poly(vinyl acetate)-poly(ethylene glycol) (Soluplusâ).Methods Drug-loaded NMs were prepared by copolymer and CAR dispersion indistilled water. Micellar size and morphology were characterized by dynamic lightscattering and transmission electron microscopy, respectively. In-vitro drug per-meation studies were evaluated by conventional gut sac method. In-vivo CARoral bioavailability from NMs dispersions and drug control solution was evalu-ated in Wistar rats.Key findings Carvedilol apparent aqueous solubility was increased (up to 60.4-folds) after its encapsulation within NMs. The micellar size was ranged between10.9 and 81.9 nm with a monomodal size distribution. There was a significantenhancement of CAR relative oral bioavailability for both copolymers vs amicelle-free drug solution (P < 0.05). This improvement was higher for TPGS-based micelles (4.95-fold) in accordance with the in-vitro CAR permeationresults.Conclusions The present investigation demonstrates the development of highlyconcentrated CAR liquid micellar formulation. The improvement on drug oralbioavailability contributes to the potential of this NMs formulation to enhanceCAR paediatric treatment.
Fil: Wegmann, Marcel. Hochschule Furtwangen University; Alemania
Fil: Parola, Luciano. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina
Fil: Bertera, Facundo Martin. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina
Fil: Taira, Carlos Alberto. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina
Fil: Cagel, Carlos Maximiliano. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina
Fil: Buontempo, Fabián. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica; Argentina
Fil: Bernabeu, Ezequiel Adrian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina
Fil: Höcht, Christian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina
Fil: Chiappetta, Diego Andrés. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina
Fil: Moretton, Marcela Analía. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica; Argentina
description Objectives Carvedilol (CAR) is a poorly water-soluble beta-blocker. Its encapsu-lation within nanomicelles (NMs) could improve drug solubility and its oralbioavailability, allowing the development of a paediatric liquid CAR formulationwith commercially available copolymers: D-a-tocopheryl polyethylene glycol1000 succinate (TPGS) and poly(vinyl caprolactam)-poly(vinyl acetate)-poly(ethylene glycol) (Soluplusâ).Methods Drug-loaded NMs were prepared by copolymer and CAR dispersion indistilled water. Micellar size and morphology were characterized by dynamic lightscattering and transmission electron microscopy, respectively. In-vitro drug per-meation studies were evaluated by conventional gut sac method. In-vivo CARoral bioavailability from NMs dispersions and drug control solution was evalu-ated in Wistar rats.Key findings Carvedilol apparent aqueous solubility was increased (up to 60.4-folds) after its encapsulation within NMs. The micellar size was ranged between10.9 and 81.9 nm with a monomodal size distribution. There was a significantenhancement of CAR relative oral bioavailability for both copolymers vs amicelle-free drug solution (P < 0.05). This improvement was higher for TPGS-based micelles (4.95-fold) in accordance with the in-vitro CAR permeationresults.Conclusions The present investigation demonstrates the development of highlyconcentrated CAR liquid micellar formulation. The improvement on drug oralbioavailability contributes to the potential of this NMs formulation to enhanceCAR paediatric treatment.
publishDate 2017
dc.date.none.fl_str_mv 2017-06
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/156756
Wegmann, Marcel; Parola, Luciano; Bertera, Facundo Martin; Taira, Carlos Alberto; Cagel, Carlos Maximiliano; et al.; Novel carvedilol paediatric nanomicelle formulation:in-vitro characterization and in-vivo evaluation; Pharmaceutical Press-Royal Pharmaceutical Society Great Britian; Journal of Pharmacy and Pharmacology; 69; 6-2017; 544-553
0022-3573
CONICET Digital
CONICET
url http://hdl.handle.net/11336/156756
identifier_str_mv Wegmann, Marcel; Parola, Luciano; Bertera, Facundo Martin; Taira, Carlos Alberto; Cagel, Carlos Maximiliano; et al.; Novel carvedilol paediatric nanomicelle formulation:in-vitro characterization and in-vivo evaluation; Pharmaceutical Press-Royal Pharmaceutical Society Great Britian; Journal of Pharmacy and Pharmacology; 69; 6-2017; 544-553
0022-3573
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/https://academic.oup.com/jpp/article/69/5/544/6128976
info:eu-repo/semantics/altIdentifier/doi/10.1111/jphp.12605
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
application/pdf
application/pdf
application/pdf
application/pdf
dc.publisher.none.fl_str_mv Pharmaceutical Press-Royal Pharmaceutical Society Great Britian
publisher.none.fl_str_mv Pharmaceutical Press-Royal Pharmaceutical Society Great Britian
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
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score 12.982451

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