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

dc.contributor.author
Espinoza, Lupe Carolina
dc.contributor.author
Silva Abreu, Marcelle
dc.contributor.author
Clares Naveros, Beatriz
dc.contributor.author
Rodríguez Lagunas, María José
dc.contributor.author
Halbaut, Lyda
dc.contributor.author
Cañas, María Alexandra
dc.contributor.author
Calpena Campmany, Ana Cristina
dc.date.issued
2020-04-15T12:11:29Z
dc.date.issued
2020-04-15T12:11:29Z
dc.date.issued
2019-02-01
dc.date.issued
2020-04-15T12:11:29Z
dc.identifier
1999-4923
dc.identifier
https://hdl.handle.net/2445/155359
dc.identifier
691103
dc.identifier
30717264
dc.description.abstract
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.
dc.format
16 p.
dc.format
application/pdf
dc.language
eng
dc.publisher
MDPI
dc.relation
Reproducció del document publicat a: https://doi.org/10.3390/pharmaceutics11020064
dc.relation
Pharmaceutics, 2019, vol. 11, num. 2, p. 64
dc.relation
https://doi.org/10.3390/pharmaceutics11020064
dc.rights
cc-by (c) Espinoza, Lupe Carolina et al., 2019
dc.rights
http://creativecommons.org/licenses/by/3.0/es
dc.rights
info:eu-repo/semantics/openAccess
dc.source
Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)
dc.subject
Malaltia d'Alzheimer
dc.subject
Barrera hematoencefàlica
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Neurofarmacologia
dc.subject
Cervell
dc.subject
Alzheimer's disease
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Blood-brain barrier
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Neuropharmacology
dc.subject
Brain
dc.title
Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil
dc.type
info:eu-repo/semantics/article
dc.type
info:eu-repo/semantics/publishedVersion


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