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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Bibliographic Details
Published in:Pharmaceutics 2022-05, Vol.14 (5), p.1006
Main Authors: Scuteri, Damiana, Rombolà, Laura, Crudo, Michele, Watanabe, Chizuko, Mizoguchi, Hirokazu, Sakurada, Shinobu, Hamamura, Kengo, Sakurada, Tsukasa, Morrone, Luigi Antonio, Tonin, Paolo, Bagetta, Giacinto, Corasaniti, Maria Tiziana
Format: Article
Language:English
Subjects:
Analgesics
clinical translation
decolored phytocomplex
deterpenated phytocomplex
essential oil of bergamot
Experiments
Intervention
Laboratory animals
limonene
linalool
Oils & fats
Pain
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Summary: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.
ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics14051006