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Title: Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil
Author: Espinoza, Lupe Carolina
Silva Abreu, Marcelle
Clares Naveros, Beatriz
Rodríguez Lagunas, María José
Halbaut, Lyda
Cañas, María-Alexandra
Calpena Campmany, Ana Cristina
Keywords: Malaltia d'Alzheimer
Barrera hematoencefàlica
Alzheimer's disease
Blood-brain barrier
Issue Date: 1-Feb-2019
Publisher: MDPI
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.
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It is part of: Pharmaceutics, 2019, vol. 11, num. 2, p. 64
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ISSN: 1999-4923
Appears in Collections:Articles publicats en revistes (Bioquímica i Fisiologia)
Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)

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