Publication:
Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil.

dc.contributor.authorEspinoza, Lupe Carolina
dc.contributor.authorSilva-Abreu, Marcelle
dc.contributor.authorClares, Beatriz
dc.contributor.authorRodríguez-Lagunas, María José
dc.contributor.authorHalbaut, Lyda
dc.contributor.authorCañas, María-Alexandra
dc.contributor.authorCalpena, Ana Cristina
dc.date.accessioned2023-01-25T10:29:54Z
dc.date.available2023-01-25T10:29:54Z
dc.date.issued2019-02-01
dc.description.abstractDonepezil (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.identifier.doi10.3390/pharmaceutics11020064
dc.identifier.issn1999-4923
dc.identifier.pmcPMC6410084
dc.identifier.pmid30717264
dc.identifier.pubmedURLhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC6410084/pdf
dc.identifier.unpaywallURLhttps://www.mdpi.com/1999-4923/11/2/64/pdf?version=1550143960
dc.identifier.urihttp://hdl.handle.net/10668/13508
dc.issue.number2
dc.journal.titlePharmaceutics
dc.journal.titleabbreviationPharmaceutics
dc.language.isoen
dc.organizationHospital Universitario San Cecilio
dc.pubmedtypeJournal Article
dc.rightsAttribution 4.0 International
dc.rights.accessRightsopen access
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/
dc.subjectAlzheimer’s disease
dc.subjectDonepezil
dc.subjectPluronic F-127
dc.subjectmucoadhesion
dc.subjectnanoemulsion
dc.subjectnose-to-brain
dc.titleFormulation Strategies to Improve Nose-to-Brain Delivery of Donepezil.
dc.typeresearch article
dc.type.hasVersionVoR
dc.volume.number11
dspace.entity.typePublication
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