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. |
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| 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] |
| Copyright of Journal of Controlled Release is the property of Elsevier B.V. and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.) | |
| Database: | Engineering Source |
| FullText | Text: Availability: 0 |
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| Header | DbId: egs DbLabel: Engineering Source An: 151154072 AccessLevel: 6 PubType: Academic Journal PubTypeId: academicJournal PreciseRelevancyScore: 0 |
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| Items | – Name: Title Label: Title Group: Ti Data: Nasal biocompatible powder of Geraniol oil complexed with cyclodextrins for neurodegenerative diseases: physicochemical characterization and in vivo evidences of nose to brain delivery. – Name: Author Label: Authors Group: Au Data: <searchLink fieldCode="AR" term="%22Truzzi%2C+Eleonora%22">Truzzi, Eleonora</searchLink><relatesTo>1</relatesTo> (AUTHOR)<i> eleonora.truzzi@unimore.it</i><br /><searchLink fieldCode="AR" term="%22Rustichelli%2C+Cecilia%22">Rustichelli, Cecilia</searchLink><relatesTo>1</relatesTo> (AUTHOR)<i> cecilia.rustichelli@unimore.it</i><br /><searchLink fieldCode="AR" term="%22de+Oliveira+Junior%2C+Edilson+Ribeiro%22">de Oliveira Junior, Edilson Ribeiro</searchLink><relatesTo>2</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Ferraro%2C+Luca%22">Ferraro, Luca</searchLink><relatesTo>3</relatesTo> (AUTHOR)<i> frl@unife.it</i><br /><searchLink fieldCode="AR" term="%22Maretti%2C+Eleonora%22">Maretti, Eleonora</searchLink><relatesTo>1</relatesTo> (AUTHOR)<i> eleonora.maretti@unimore.it</i><br /><searchLink fieldCode="AR" term="%22Graziani%2C+Daniel%22">Graziani, Daniel</searchLink><relatesTo>4</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Botti%2C+Giada%22">Botti, Giada</searchLink><relatesTo>5</relatesTo> (AUTHOR)<i> giada.botti@unife.it</i><br /><searchLink fieldCode="AR" term="%22Beggiato%2C+Sarah%22">Beggiato, Sarah</searchLink><relatesTo>6</relatesTo> (AUTHOR)<i> bggsrh@unife.it</i><br /><searchLink fieldCode="AR" term="%22Iannuccelli%2C+Valentina%22">Iannuccelli, Valentina</searchLink><relatesTo>1</relatesTo> (AUTHOR)<i> valentina.iannuccelli@unimore.it</i><br /><searchLink fieldCode="AR" term="%22Lima%2C+Eliana+Martins%22">Lima, Eliana Martins</searchLink><relatesTo>2</relatesTo> (AUTHOR)<i> emlima@ufg.br</i><br /><searchLink fieldCode="AR" term="%22Dalpiaz%2C+Alessandro%22">Dalpiaz, Alessandro</searchLink><relatesTo>1,5</relatesTo> (AUTHOR)<i> dla@unife.it</i><br /><searchLink fieldCode="AR" term="%22Leo%2C+Eliana%22">Leo, Eliana</searchLink><relatesTo>1</relatesTo> (AUTHOR)<i> eliana.leo@unimore.it</i> – Name: TitleSource Label: Source Group: Src Data: <searchLink fieldCode="JN" term="%22Journal+of+Controlled+Release%22">Journal of Controlled Release</searchLink>. Jul2021, Vol. 335, p191-202. 12p. – Name: Subject Label: Subjects Group: Su Data: <searchLink fieldCode="DE" term="%22Neurodegeneration%22">Neurodegeneration</searchLink><br /><searchLink fieldCode="DE" term="%22Cyclodextrin+derivatives%22">Cyclodextrin derivatives</searchLink><br /><searchLink fieldCode="DE" term="%22Nasal+mucosa%22">Nasal mucosa</searchLink><br /><searchLink fieldCode="DE" term="%22Cyclodextrins%22">Cyclodextrins</searchLink><br /><searchLink fieldCode="DE" term="%22Parkinson's+disease%22">Parkinson's disease</searchLink><br /><searchLink fieldCode="DE" term="%22Drug+bioavailability%22">Drug bioavailability</searchLink><br /><searchLink fieldCode="DE" term="%22Plant+metabolites%22">Plant metabolites</searchLink><br /><searchLink fieldCode="DE" term="%22Nose%22">Nose</searchLink> – Name: Abstract Label: Abstract Group: Ab Data: 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] – Name: AbstractSuppliedCopyright Label: Group: Ab Data: <i>Copyright of Journal of Controlled Release is the property of Elsevier B.V. and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract.</i> (Copyright applies to all Abstracts.) |
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| RecordInfo | BibRecord: BibEntity: Identifiers: – Type: doi Value: 10.1016/j.jconrel.2021.05.020 Languages: – Code: eng Text: English PhysicalDescription: Pagination: PageCount: 12 StartPage: 191 Subjects: – SubjectFull: Neurodegeneration Type: general – SubjectFull: Cyclodextrin derivatives Type: general – SubjectFull: Nasal mucosa Type: general – SubjectFull: Cyclodextrins Type: general – SubjectFull: Parkinson's disease Type: general – SubjectFull: Drug bioavailability Type: general – SubjectFull: Plant metabolites Type: general – SubjectFull: Nose Type: general Titles: – TitleFull: Nasal biocompatible powder of Geraniol oil complexed with cyclodextrins for neurodegenerative diseases: physicochemical characterization and in vivo evidences of nose to brain delivery. Type: main BibRelationships: HasContributorRelationships: – PersonEntity: Name: NameFull: Truzzi, Eleonora – PersonEntity: Name: NameFull: Rustichelli, Cecilia – PersonEntity: Name: NameFull: de Oliveira Junior, Edilson Ribeiro – PersonEntity: Name: NameFull: Ferraro, Luca – PersonEntity: Name: NameFull: Maretti, Eleonora – PersonEntity: Name: NameFull: Graziani, Daniel – PersonEntity: Name: NameFull: Botti, Giada – PersonEntity: Name: NameFull: Beggiato, Sarah – PersonEntity: Name: NameFull: Iannuccelli, Valentina – PersonEntity: Name: NameFull: Lima, Eliana Martins – PersonEntity: Name: NameFull: Dalpiaz, Alessandro – PersonEntity: Name: NameFull: Leo, Eliana IsPartOfRelationships: – BibEntity: Dates: – D: 10 M: 07 Text: Jul2021 Type: published Y: 2021 Identifiers: – Type: issn-print Value: 01683659 Numbering: – Type: volume Value: 335 Titles: – TitleFull: Journal of Controlled Release Type: main |
| ResultId | 1 |
