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
- Institución
- Consejo Nacional de Investigaciones Científicas y Técnicas
- OAI Identificador
- oai:ri.conicet.gov.ar:11336/156756
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oai:ri.conicet.gov.ar:11336/156756 |
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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 Técnicas2025-09-29T10:30:12Zoai: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:34982025-09-29 10:30:12.769CONICET 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 |
13.070432 |