Cargando…
Uptake in the Central Nervous System of Geraniol Oil Encapsulated in Chitosan Oleate Following Nasal and Oral Administration
The pharmacological activities of geraniol include anticancer and neuroprotective properties. However, its insolubility in water easily induces separation from aqueous formulations, causing administration difficulties. Here we propose new emulsified formulations of geraniol by using the amphiphilic...
Autores principales: | , , , , , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2019
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6471858/ https://www.ncbi.nlm.nih.gov/pubmed/30832389 http://dx.doi.org/10.3390/pharmaceutics11030106 |
_version_ | 1783412121234571264 |
---|---|
author | Bonferoni, Maria Cristina Ferraro, Luca Pavan, Barbara Beggiato, Sarah Cavalieri, Elena Giunchedi, Paolo Dalpiaz, Alessandro |
author_facet | Bonferoni, Maria Cristina Ferraro, Luca Pavan, Barbara Beggiato, Sarah Cavalieri, Elena Giunchedi, Paolo Dalpiaz, Alessandro |
author_sort | Bonferoni, Maria Cristina |
collection | PubMed |
description | The pharmacological activities of geraniol include anticancer and neuroprotective properties. However, its insolubility in water easily induces separation from aqueous formulations, causing administration difficulties. Here we propose new emulsified formulations of geraniol by using the amphiphilic polymer chitosan-oleate (CS-OA) as surfactant to combine mucoadhesive and absorption enhancer properties with stabilization effects on the oil dispersion. The formulation based on CS-OA 2% (w/w) (G-CS-OA-2.0%) showed viscosity values compatible with oral and nasal administration to rats, and mean diameter of the dispersed phase of 819 ± 104 nm. G-CS-OA-2.0% oral administration sensibly increases the geraniol bioavailability with respect to coarse emulsions obtained without CS-OA (AUC values in the bloodstream were 42,713 ± 1553 µg∙mL(−1)∙min and 2158 ± 82 µg∙mL(−1)∙min following administration of 50 mg/kg or 1 mg/kg, respectively), and enhances the aptitude of geraniol to reach the central nervous system from the bloodstream (AUC values in the cerebrospinal fluid were 7293 ± 408 µg∙mL(−1)∙min and 399 ± 25 µg∙mL(−1)∙min after oral administration of 50 mg/kg or 1 mg/kg, respectively). Moreover, relevant geraniol amounts were detected in the cerebrospinal fluid following the G-CS-OA-2% nasal administration (AUC values in the cerebrospinal fluid were 10,778 ± 477 µg∙mL(−1)∙min and 5571 ± 290 µg∙mL(−1)∙min after nasal administration of 4 mg/kg or 1 mg/kg, respectively). |
format | Online Article Text |
id | pubmed-6471858 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-64718582019-04-27 Uptake in the Central Nervous System of Geraniol Oil Encapsulated in Chitosan Oleate Following Nasal and Oral Administration Bonferoni, Maria Cristina Ferraro, Luca Pavan, Barbara Beggiato, Sarah Cavalieri, Elena Giunchedi, Paolo Dalpiaz, Alessandro Pharmaceutics Article The pharmacological activities of geraniol include anticancer and neuroprotective properties. However, its insolubility in water easily induces separation from aqueous formulations, causing administration difficulties. Here we propose new emulsified formulations of geraniol by using the amphiphilic polymer chitosan-oleate (CS-OA) as surfactant to combine mucoadhesive and absorption enhancer properties with stabilization effects on the oil dispersion. The formulation based on CS-OA 2% (w/w) (G-CS-OA-2.0%) showed viscosity values compatible with oral and nasal administration to rats, and mean diameter of the dispersed phase of 819 ± 104 nm. G-CS-OA-2.0% oral administration sensibly increases the geraniol bioavailability with respect to coarse emulsions obtained without CS-OA (AUC values in the bloodstream were 42,713 ± 1553 µg∙mL(−1)∙min and 2158 ± 82 µg∙mL(−1)∙min following administration of 50 mg/kg or 1 mg/kg, respectively), and enhances the aptitude of geraniol to reach the central nervous system from the bloodstream (AUC values in the cerebrospinal fluid were 7293 ± 408 µg∙mL(−1)∙min and 399 ± 25 µg∙mL(−1)∙min after oral administration of 50 mg/kg or 1 mg/kg, respectively). Moreover, relevant geraniol amounts were detected in the cerebrospinal fluid following the G-CS-OA-2% nasal administration (AUC values in the cerebrospinal fluid were 10,778 ± 477 µg∙mL(−1)∙min and 5571 ± 290 µg∙mL(−1)∙min after nasal administration of 4 mg/kg or 1 mg/kg, respectively). MDPI 2019-03-03 /pmc/articles/PMC6471858/ /pubmed/30832389 http://dx.doi.org/10.3390/pharmaceutics11030106 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Bonferoni, Maria Cristina Ferraro, Luca Pavan, Barbara Beggiato, Sarah Cavalieri, Elena Giunchedi, Paolo Dalpiaz, Alessandro Uptake in the Central Nervous System of Geraniol Oil Encapsulated in Chitosan Oleate Following Nasal and Oral Administration |
title | Uptake in the Central Nervous System of Geraniol Oil Encapsulated in Chitosan Oleate Following Nasal and Oral Administration |
title_full | Uptake in the Central Nervous System of Geraniol Oil Encapsulated in Chitosan Oleate Following Nasal and Oral Administration |
title_fullStr | Uptake in the Central Nervous System of Geraniol Oil Encapsulated in Chitosan Oleate Following Nasal and Oral Administration |
title_full_unstemmed | Uptake in the Central Nervous System of Geraniol Oil Encapsulated in Chitosan Oleate Following Nasal and Oral Administration |
title_short | Uptake in the Central Nervous System of Geraniol Oil Encapsulated in Chitosan Oleate Following Nasal and Oral Administration |
title_sort | uptake in the central nervous system of geraniol oil encapsulated in chitosan oleate following nasal and oral administration |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6471858/ https://www.ncbi.nlm.nih.gov/pubmed/30832389 http://dx.doi.org/10.3390/pharmaceutics11030106 |
work_keys_str_mv | AT bonferonimariacristina uptakeinthecentralnervoussystemofgeranioloilencapsulatedinchitosanoleatefollowingnasalandoraladministration AT ferraroluca uptakeinthecentralnervoussystemofgeranioloilencapsulatedinchitosanoleatefollowingnasalandoraladministration AT pavanbarbara uptakeinthecentralnervoussystemofgeranioloilencapsulatedinchitosanoleatefollowingnasalandoraladministration AT beggiatosarah uptakeinthecentralnervoussystemofgeranioloilencapsulatedinchitosanoleatefollowingnasalandoraladministration AT cavalierielena uptakeinthecentralnervoussystemofgeranioloilencapsulatedinchitosanoleatefollowingnasalandoraladministration AT giunchedipaolo uptakeinthecentralnervoussystemofgeranioloilencapsulatedinchitosanoleatefollowingnasalandoraladministration AT dalpiazalessandro uptakeinthecentralnervoussystemofgeranioloilencapsulatedinchitosanoleatefollowingnasalandoraladministration |