Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil

Donepezil (DPZ) is widely used in the treatment of Alzheimer's disease in tablet form for oral administration. The pharmacological efficacy of this drug can be enhanced by the use of intranasal administration because this route makes bypassing the blood-brain barrier (BBB) possible. The aim of...

Descripción completa

Detalles Bibliográficos
Autores: Espinoza, Lupe Carolina, Silva Abreu, Marcelle, Clares Naveros, Beatriz, Rodríguez Lagunas, María José, Halbaut, Lyda, Cañas, María Alexandra, Calpena Campmany, Ana Cristina
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2019
País:España
Institución:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
Repositorio:Recercat. Dipósit de la Recerca de Catalunya
OAI Identifier:oai:recercat.cat:2445/155359
Acceso en línea:https://hdl.handle.net/2445/155359
Access Level:acceso abierto
Palabra clave:Malaltia d'Alzheimer
Barrera hematoencefàlica
Neurofarmacologia
Cervell
Alzheimer's disease
Blood-brain barrier
Neuropharmacology
Brain
id ES_bc2aeb09bbb2948a97668a5230d8e376
oai_identifier_str oai:recercat.cat:2445/155359
network_acronym_str ES
network_name_str España
repository_id_str
spelling Formulation Strategies to Improve Nose-to-Brain Delivery of DonepezilEspinoza, Lupe CarolinaSilva Abreu, MarcelleClares Naveros, BeatrizRodríguez Lagunas, María JoséHalbaut, LydaCañas, María AlexandraCalpena Campmany, Ana CristinaMalaltia d'AlzheimerBarrera hematoencefàlicaNeurofarmacologiaCervellAlzheimer's diseaseBlood-brain barrierNeuropharmacologyBrainDonepezil (DPZ) is widely used in the treatment of Alzheimer's disease in tablet form for oral administration. The pharmacological efficacy of this drug can be enhanced by the use of intranasal administration because this route makes bypassing the blood-brain barrier (BBB) possible. The aim of this study was to develop a nanoemulsion (NE) as well as a nanoemulsion with a combination of bioadhesion and penetration enhancing properties (PNE) in order to facilitate the transport of DPZ from nose-to-brain. Composition of NE was established using three pseudo-ternary diagrams and PNE was developed by incorporating Pluronic F-127 to the aqueous phase. Parameters such as physical properties, stability, in vitro release profile, and ex vivo permeation were determined for both formulations. The tolerability was evaluated by in vitro and in vivo models. DPZ-NE and DPZ-PNE were transparent, monophasic, homogeneous, and physically stable with droplets of nanometric size and spherical shape. DPZ-NE showed Newtonian behavior whereas a shear thinning (pseudoplastic) behavior was observed for DPZ-PNE. The release profile of both formulations followed a hyperbolic kinetic. The permeation and prediction parameters were significantly higher for DPZ-PNE, suggesting the use of polymers to be an effective strategy to improve the bioadhesion and penetration of the drug through nasal mucosa, which consequently increase its bioavailability.MDPI2020202020192020info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersion16 p.application/pdfhttps://hdl.handle.net/2445/155359Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)reponame:Recercat. Dipósit de la Recerca de Catalunyainstname:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)InglésReproducció del document publicat a: https://doi.org/10.3390/pharmaceutics11020064Pharmaceutics, 2019, vol. 11, num. 2, p. 64https://doi.org/10.3390/pharmaceutics11020064cc-by (c) Espinoza, Lupe Carolina et al., 2019http://creativecommons.org/licenses/by/3.0/esinfo:eu-repo/semantics/openAccessoai:recercat.cat:2445/1553592026-05-29T05:05:01Z
dc.title.none.fl_str_mv Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil
title Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil
spellingShingle Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil
Espinoza, Lupe Carolina
Malaltia d'Alzheimer
Barrera hematoencefàlica
Neurofarmacologia
Cervell
Alzheimer's disease
Blood-brain barrier
Neuropharmacology
Brain
title_short Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil
title_full Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil
title_fullStr Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil
title_full_unstemmed Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil
title_sort Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil
dc.creator.none.fl_str_mv Espinoza, Lupe Carolina
Silva Abreu, Marcelle
Clares Naveros, Beatriz
Rodríguez Lagunas, María José
Halbaut, Lyda
Cañas, María Alexandra
Calpena Campmany, Ana Cristina
author Espinoza, Lupe Carolina
author_facet Espinoza, Lupe Carolina
Silva Abreu, Marcelle
Clares Naveros, Beatriz
Rodríguez Lagunas, María José
Halbaut, Lyda
Cañas, María Alexandra
Calpena Campmany, Ana Cristina
author_role author
author2 Silva Abreu, Marcelle
Clares Naveros, Beatriz
Rodríguez Lagunas, María José
Halbaut, Lyda
Cañas, María Alexandra
Calpena Campmany, Ana Cristina
author2_role author
author
author
author
author
author
dc.subject.none.fl_str_mv Malaltia d'Alzheimer
Barrera hematoencefàlica
Neurofarmacologia
Cervell
Alzheimer's disease
Blood-brain barrier
Neuropharmacology
Brain
topic Malaltia d'Alzheimer
Barrera hematoencefàlica
Neurofarmacologia
Cervell
Alzheimer's disease
Blood-brain barrier
Neuropharmacology
Brain
description Donepezil (DPZ) is widely used in the treatment of Alzheimer's disease in tablet form for oral administration. The pharmacological efficacy of this drug can be enhanced by the use of intranasal administration because this route makes bypassing the blood-brain barrier (BBB) possible. The aim of this study was to develop a nanoemulsion (NE) as well as a nanoemulsion with a combination of bioadhesion and penetration enhancing properties (PNE) in order to facilitate the transport of DPZ from nose-to-brain. Composition of NE was established using three pseudo-ternary diagrams and PNE was developed by incorporating Pluronic F-127 to the aqueous phase. Parameters such as physical properties, stability, in vitro release profile, and ex vivo permeation were determined for both formulations. The tolerability was evaluated by in vitro and in vivo models. DPZ-NE and DPZ-PNE were transparent, monophasic, homogeneous, and physically stable with droplets of nanometric size and spherical shape. DPZ-NE showed Newtonian behavior whereas a shear thinning (pseudoplastic) behavior was observed for DPZ-PNE. The release profile of both formulations followed a hyperbolic kinetic. The permeation and prediction parameters were significantly higher for DPZ-PNE, suggesting the use of polymers to be an effective strategy to improve the bioadhesion and penetration of the drug through nasal mucosa, which consequently increase its bioavailability.
publishDate 2019
dc.date.none.fl_str_mv 2019
2020
2020
2020
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/2445/155359
url https://hdl.handle.net/2445/155359
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Reproducció del document publicat a: https://doi.org/10.3390/pharmaceutics11020064
Pharmaceutics, 2019, vol. 11, num. 2, p. 64
https://doi.org/10.3390/pharmaceutics11020064
dc.rights.none.fl_str_mv cc-by (c) Espinoza, Lupe Carolina et al., 2019
http://creativecommons.org/licenses/by/3.0/es
info:eu-repo/semantics/openAccess
rights_invalid_str_mv cc-by (c) Espinoza, Lupe Carolina et al., 2019
http://creativecommons.org/licenses/by/3.0/es
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv 16 p.
application/pdf
dc.publisher.none.fl_str_mv MDPI
publisher.none.fl_str_mv MDPI
dc.source.none.fl_str_mv Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)
reponame:Recercat. Dipósit de la Recerca de Catalunya
instname:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
instname_str Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
reponame_str Recercat. Dipósit de la Recerca de Catalunya
collection Recercat. Dipósit de la Recerca de Catalunya
repository.name.fl_str_mv
repository.mail.fl_str_mv
_version_ 1869418089987178496
score 15,811543

Similares en LA Referencia