Translational Value of the Transdermal Administration of Bergamot Essential Oil and of Its Fractions

The essential oil of bergamot (BEO) has consistently proven antinociceptive and antiallodynic properties. Accordingly, the analgesic efficacy of the decolored essential oil (DEC), with higher levels of limonene, and the deterpenated (DET) fraction, with higher levels of linalool and linalyl acetate,...

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Main Authors: Damiana Scuteri, Laura Rombolà, Michele Crudo, Chizuko Watanabe, Hirokazu Mizoguchi, Shinobu Sakurada, Kengo Hamamura, Tsukasa Sakurada, Luigi Antonio Morrone, Paolo Tonin, Giacinto Bagetta, Maria Tiziana Corasaniti
Format: Article
Language:English
Published: MDPI AG 2022-05-01
Series:Pharmaceutics
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Online Access:https://www.mdpi.com/1999-4923/14/5/1006
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author Damiana Scuteri
Laura Rombolà
Michele Crudo
Chizuko Watanabe
Hirokazu Mizoguchi
Shinobu Sakurada
Kengo Hamamura
Tsukasa Sakurada
Luigi Antonio Morrone
Paolo Tonin
Giacinto Bagetta
Maria Tiziana Corasaniti
author_facet Damiana Scuteri
Laura Rombolà
Michele Crudo
Chizuko Watanabe
Hirokazu Mizoguchi
Shinobu Sakurada
Kengo Hamamura
Tsukasa Sakurada
Luigi Antonio Morrone
Paolo Tonin
Giacinto Bagetta
Maria Tiziana Corasaniti
author_sort Damiana Scuteri
collection DOAJ
description The essential oil of bergamot (BEO) has consistently proven antinociceptive and antiallodynic properties. Accordingly, the analgesic efficacy of the decolored essential oil (DEC), with higher levels of limonene, and the deterpenated (DET) fraction, with higher levels of linalool and linalyl acetate, was investigated using a formalin test after inhalation. The present study was aimed at characterizing the effects of BEO, its components with the highest pharmacological activity (represented by linalool, limonene, and linalyl acetate), and its DEC and DET fractions on the formalin test after transdermal administration relevant to clinical translation through topical application. To this aim, the schedule of intervention involved administration immediately after formalin injection or as a 5 min pretreatment followed by washout in ddY-strain mice. This study demonstrates, for the first time, the significant analgesic effect of all three constituents in the first and second phases, accounting for the efficacy of the essential oil in the formalin test. While all fractions revealed equal activity toward the phytocomplex in the early phase, the reduction in time of licking/biting during the late phase was more markedly induced by DEC. Moreover, pretreatment with BEO and its fractions followed by washout did not produce a significant reduction in licking/biting time in both phases of formalin-induced nociceptive response.
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spelling doaj.art-94af3fa09a8a4eda9751a3854515fd992023-11-23T12:38:01ZengMDPI AGPharmaceutics1999-49232022-05-01145100610.3390/pharmaceutics14051006Translational Value of the Transdermal Administration of Bergamot Essential Oil and of Its FractionsDamiana Scuteri0Laura Rombolà1Michele Crudo2Chizuko Watanabe3Hirokazu Mizoguchi4Shinobu Sakurada5Kengo Hamamura6Tsukasa Sakurada7Luigi Antonio Morrone8Paolo Tonin9Giacinto Bagetta10Maria Tiziana Corasaniti11Pharmacotechnology Documentation and Transfer Unit, Preclinical and Translational Pharmacology, Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, ItalyPreclinical and Translational Pharmacology, Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, ItalyPreclinical and Translational Pharmacology, Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, ItalyDepartment of Physiology and Anatomy, Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, 4-4-1 Komatsushima, Aoba-ku, Sendai 981-8558, JapanDepartment of Physiology and Anatomy, Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, 4-4-1 Komatsushima, Aoba-ku, Sendai 981-8558, JapanFirst Department of Pharmacology Fukuoka, Daiichi College of Pharmaceutical Sciences, Fukuoka 815-8511, JapanFirst Department of Pharmacology Fukuoka, Daiichi College of Pharmaceutical Sciences, Fukuoka 815-8511, JapanFirst Department of Pharmacology Fukuoka, Daiichi College of Pharmaceutical Sciences, Fukuoka 815-8511, JapanPreclinical and Translational Pharmacology, Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, ItalyRegional Center for Serious Brain Injuries, S. Anna Institute, 88900 Crotone, ItalyPharmacotechnology Documentation and Transfer Unit, Preclinical and Translational Pharmacology, Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, ItalyDepartment of Health Sciences, University “Magna Graecia” of Catanzaro, 88100 Catanzaro, ItalyThe essential oil of bergamot (BEO) has consistently proven antinociceptive and antiallodynic properties. Accordingly, the analgesic efficacy of the decolored essential oil (DEC), with higher levels of limonene, and the deterpenated (DET) fraction, with higher levels of linalool and linalyl acetate, was investigated using a formalin test after inhalation. The present study was aimed at characterizing the effects of BEO, its components with the highest pharmacological activity (represented by linalool, limonene, and linalyl acetate), and its DEC and DET fractions on the formalin test after transdermal administration relevant to clinical translation through topical application. To this aim, the schedule of intervention involved administration immediately after formalin injection or as a 5 min pretreatment followed by washout in ddY-strain mice. This study demonstrates, for the first time, the significant analgesic effect of all three constituents in the first and second phases, accounting for the efficacy of the essential oil in the formalin test. While all fractions revealed equal activity toward the phytocomplex in the early phase, the reduction in time of licking/biting during the late phase was more markedly induced by DEC. Moreover, pretreatment with BEO and its fractions followed by washout did not produce a significant reduction in licking/biting time in both phases of formalin-induced nociceptive response.https://www.mdpi.com/1999-4923/14/5/1006essential oil of bergamotclinical translationdecolored phytocomplexdeterpenated phytocomplexlimonenelinalool
spellingShingle Damiana Scuteri
Laura Rombolà
Michele Crudo
Chizuko Watanabe
Hirokazu Mizoguchi
Shinobu Sakurada
Kengo Hamamura
Tsukasa Sakurada
Luigi Antonio Morrone
Paolo Tonin
Giacinto Bagetta
Maria Tiziana Corasaniti
Translational Value of the Transdermal Administration of Bergamot Essential Oil and of Its Fractions
Pharmaceutics
essential oil of bergamot
clinical translation
decolored phytocomplex
deterpenated phytocomplex
limonene
linalool
title Translational Value of the Transdermal Administration of Bergamot Essential Oil and of Its Fractions
title_full Translational Value of the Transdermal Administration of Bergamot Essential Oil and of Its Fractions
title_fullStr Translational Value of the Transdermal Administration of Bergamot Essential Oil and of Its Fractions
title_full_unstemmed Translational Value of the Transdermal Administration of Bergamot Essential Oil and of Its Fractions
title_short Translational Value of the Transdermal Administration of Bergamot Essential Oil and of Its Fractions
title_sort translational value of the transdermal administration of bergamot essential oil and of its fractions
topic essential oil of bergamot
clinical translation
decolored phytocomplex
deterpenated phytocomplex
limonene
linalool
url https://www.mdpi.com/1999-4923/14/5/1006
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