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Nasal biocompatible powder of Geraniol oil complexed with cyclodextrins for neurodegenerative diseases: physicochemical characterization and in vivo evidences of nose to brain delivery.

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Title: Nasal biocompatible powder of Geraniol oil complexed with cyclodextrins for neurodegenerative diseases: physicochemical characterization and in vivo evidences of nose to brain delivery.
Authors: Truzzi, Eleonora1 (AUTHOR) eleonora.truzzi@unimore.it, Rustichelli, Cecilia1 (AUTHOR) cecilia.rustichelli@unimore.it, de Oliveira Junior, Edilson Ribeiro2 (AUTHOR), Ferraro, Luca3 (AUTHOR) frl@unife.it, Maretti, Eleonora1 (AUTHOR) eleonora.maretti@unimore.it, Graziani, Daniel4 (AUTHOR), Botti, Giada5 (AUTHOR) giada.botti@unife.it, Beggiato, Sarah6 (AUTHOR) bggsrh@unife.it, Iannuccelli, Valentina1 (AUTHOR) valentina.iannuccelli@unimore.it, Lima, Eliana Martins2 (AUTHOR) emlima@ufg.br, Dalpiaz, Alessandro1,5 (AUTHOR) dla@unife.it, Leo, Eliana1 (AUTHOR) eliana.leo@unimore.it
Source: Journal of Controlled Release. Jul2021, Vol. 335, p191-202. 12p.
Subjects: Neurodegeneration, Cyclodextrin derivatives, Nasal mucosa, Cyclodextrins, Parkinson's disease, Drug bioavailability, Plant metabolites, Nose
Abstract: Recently, many studies have shown that plant metabolites, such as geraniol (GER), may exert anti-inflammatory effects in neurodegenerative diseases and, in particular, Parkinson's disease (PD) models. Unfortunately, delivering GER to the CNS via nose-to-brain is not feasible due to its irritant effects on the mucosae. Therefore, in the present study β-cyclodextrin (βCD) and its hydrophilic derivative hydroxypropyl-beta-cyclodextrin (HPβCD) were selected as potential carriers for GER nose-to-brain delivery. Inclusion complexes were formulated and the biocompatibility with nasal mucosae and drug bioavailability into cerebrospinal fluid (CSF) were studied in rats. It has been demonstrated by DTA, FT-IR and NMR analyses that both the CDs were able to form 1:1 GER-CD complexes, arising long-term stable powders after the freeze-drying process. GER-HPβCD-5 and GER-βCD-2 complexes exhibited comparable results, except for morphology and solubility, as demonstrated by SEM analysis and phase solubility study, respectively. Even though both complexes were able to directly and safely deliver GER to CNS, GER-βCD-2 displayed higher ability in releasing GER in the CSF. In conclusion, βCD complexes can be considered a very promising tool in delivering GER into the CNS via nose-to-brain route, preventing GER release into the bloodstream and ensuring the integrity of the nasal mucosa. [Display omitted] • Geraniol (GER), a natural antioxidant oil, has a potential in neurodegenerative disease therapy. • GER administered via nose-to-brain destroys the nasal mucosa. • GER complexed with βCD and the more hydrosoluble HPβCD forms solid and stable inclusion complexes. • GER-βCD and GER-HPβCD complexes were administered to rats via nose-to-brain. • βCD selectively targets GER in CSF 100 times more effectively than HPβCD, preserving nasal mucosae. [ABSTRACT FROM AUTHOR]
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Database: Engineering Source
Description
Abstract:Recently, many studies have shown that plant metabolites, such as geraniol (GER), may exert anti-inflammatory effects in neurodegenerative diseases and, in particular, Parkinson's disease (PD) models. Unfortunately, delivering GER to the CNS via nose-to-brain is not feasible due to its irritant effects on the mucosae. Therefore, in the present study β-cyclodextrin (βCD) and its hydrophilic derivative hydroxypropyl-beta-cyclodextrin (HPβCD) were selected as potential carriers for GER nose-to-brain delivery. Inclusion complexes were formulated and the biocompatibility with nasal mucosae and drug bioavailability into cerebrospinal fluid (CSF) were studied in rats. It has been demonstrated by DTA, FT-IR and NMR analyses that both the CDs were able to form 1:1 GER-CD complexes, arising long-term stable powders after the freeze-drying process. GER-HPβCD-5 and GER-βCD-2 complexes exhibited comparable results, except for morphology and solubility, as demonstrated by SEM analysis and phase solubility study, respectively. Even though both complexes were able to directly and safely deliver GER to CNS, GER-βCD-2 displayed higher ability in releasing GER in the CSF. In conclusion, βCD complexes can be considered a very promising tool in delivering GER into the CNS via nose-to-brain route, preventing GER release into the bloodstream and ensuring the integrity of the nasal mucosa. [Display omitted] • Geraniol (GER), a natural antioxidant oil, has a potential in neurodegenerative disease therapy. • GER administered via nose-to-brain destroys the nasal mucosa. • GER complexed with βCD and the more hydrosoluble HPβCD forms solid and stable inclusion complexes. • GER-βCD and GER-HPβCD complexes were administered to rats via nose-to-brain. • βCD selectively targets GER in CSF 100 times more effectively than HPβCD, preserving nasal mucosae. [ABSTRACT FROM AUTHOR]
ISSN:01683659
DOI:10.1016/j.jconrel.2021.05.020