Abstract
Carvacrol is the main phenolic monoterpene isolated from the essential oils of plants from the genus Origanum L., Lamiaceae. Carvacrol has several biological activities, including antioxidant, antimicrobial and anti-inflammatory activities. The present study aimed to develop a carvacrol-loaded nanoemulsion and evaluate whether it improves the anti-inflammatory activity of the oil. A nanoemulsion was produced and its average droplet size, polydispersity index, and zeta potential were characterized. To evaluate its anti-inflammatory activity, a complete Freund’s adjuvant-induced paw edema mouse model was used, and interleukin (IL)-1β levels were quantified using ELISA. To assess toxicity, behavioral changes and biochemical parameters in mice were evaluated. The nanoemulsion was shown to be 125.00 ± 0.782 nm in size, with a polydispersity index of 0.200 ± 0.001 and zeta potential of − 26.37 ± 0.59 mV. After intraperitoneal administration, carvacrol and the carvacrol-loaded nanoemulsion showed similar anti-inflammatory efficacy as dexamethasone. Notably, both tested samples had longer anti-inflammatory effects than the control drug. The pharmacological profiles of orally administered carvacrol and its nanoemulsion were different. Although carvacrol (200 mg/kg) did not exhibit anti-inflammatory activity upon oral administration, carvacrol-loaded nanoemulsion administered at the same dose and route induced an anti-edematogenic effect that persisted for up to 24 h. Oral administration of carvacrol-loaded nanoemulsion, but not carvacrol, reduced pro-inflammatory cytokine IL-1β levels in the inflamed mouse paw, with similar efficacy to dexamethasone. Moreover, daily treatment with carvacrol-loaded nanoemulsion did not induce any behavioral or biochemical alterations. Nanoemulsification improved the pharmacological properties of carvacrol.
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The data that support the findings of this study are available from the corresponding author upon reasonable request.
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Funding
This work was supported by the Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) (Process 88887.633432/2021–00) and Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) (grant number INCT/Rennofito 465536/2014–0).
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RLS: investigation, conceptualization, methodology, writing—original draft. COM: investigation, methodology, writing—original draft. LCFO: investigation, methodology, writing—original draft. ELW: investigation, methodology, writing—original draft. CFV: conceptualization, writing original draft, review and editing, funding acquisition. EEO: conceptualization, writing original draft, review and editing, supervision, project administration, funding acquisition.
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The experiments were approved by the Institutional Animal Care and Use Committee Fiocruz (CEUA/IGM 025/2017).
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de Souza, R.L., de Oliveira Melo, C., Opretzka, L.C.F. et al. Nanoemulsion Improves the Anti-inflammatory Activity of Carvacrol upon Oral Administration. Rev. Bras. Farmacogn. 33, 164–172 (2023). https://doi.org/10.1007/s43450-022-00355-6
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DOI: https://doi.org/10.1007/s43450-022-00355-6