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Abstract
Croton rhamnifolioides is used in popular medicine for the treatment of inflammatory diseases. The objective of this study was to characterize and evaluate the anti-inflammatory effect of C. rhamnifolioides essential oil complexed in β-cyclodextrin (COEFC). The physicochemical characterization of the complexes was performed using different physical methods. The anti-inflammatory activity was evaluated in vivo by ear edema, paw edema, cotton pellet-induced granuloma, and vascular permeability by Evans blue extravasation. The mechanism of action was validated by molecular docking of the major constituent into the cyclooxygenase-2 (COX-2 enzyme). All doses of the COEFC reduced acute paw edema induced by carrageenan and dextran, as well as vascular permeability. Our results suggest the lowest effective dose of all samples inhibited the response induced by histamine or arachidonic acid as well as the granuloma formation. The complexation process showed that the pharmacological effects were maintained, however, showing similar results using much lower doses. The results demonstrated an involvement of the inhibition of pathways dependent on eicosanoids and histamine. Complexation of β-cyclodextrin/Essential oil (β-CD/EO) may present an important tool in the study of new compounds for the development of anti-inflammatory drugs.
Highlights
Essential oils are complex mixtures of natural compounds obtained from aromatic plants
The results presented in this study demonstrated a significant reduction in vascular permeability and total proteins in the peritoneal fluid of mice treated with COEFC
The physicochemical characterization of the Croton rhamnifolioides essential oil showed that co-evaporation (CE) is the best inclusion method for β-cyclodextrin complexation due to a higher stability
Summary
Essential oils are complex mixtures of natural compounds obtained from aromatic plants. Because of their volatility, these compounds are characterized by an intense odor [1] and have specific physicochemical characteristics, including liquid composition at room temperature, oily aspect, colorless or slightly yellowish appearance, and low stability when exposed to air, humidity, light, heat, and metals [2]. Many medicinal plants rich in essential oils have their therapeutic effects attributed to the presence of these volatile mixtures. It has been shown that, depending on the chemical composition, essential oils are relatively safe when used in low concentrations; they can show signs of toxicity to humans when administered in high concentrations or when administered in repeated doses [3]. The complexation in cyclodextrin is an important strategy of the drug delivery system
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