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Anti-Inflammatory and Physicochemical Characterization of the Croton Rhamnifolioides Essential Oil Inclusion Complex in ?-Cyclodextrin.

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 ?-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 ?-cyclodextrin/Essential oil (?-CD/EO) may present an important tool in the study of new compounds for the development of anti-inflammatory drugs.

SUBMITTER: Oliveira Brito Pereira Bezerra Martins A

PROVIDER: S-EPMC7344496 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature

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Anti-Inflammatory and Physicochemical Characterization of the Croton Rhamnifolioides Essential Oil Inclusion Complex in β-Cyclodextrin.

Oliveira Brito Pereira Bezerra Martins Anita A Wanderley Almir Gonçalves AG Alcântara Isabel Sousa IS Rodrigues Lindaiane Bezerra LB Cesário Francisco Rafael Alves Santana FRAS Correia de Oliveira Maria Rayane MR Castro Fyama Ferreira E FFE Albuquerque Thaís Rodrigues de TR da Silva Maria Sanadia Alexandre MSA Ribeiro-Filho Jaime J Coutinho Henrique Douglas Melo HDM Menezes Paula Passos PP Quintans-Júnior Lucindo José LJ Araújo Adriano Antunes de Souza AAS Iriti Marcello M Almeida Jackson Roberto Guedes da Silva JRGDS Menezes Irwin Rose Alencar de IRA

Biology 20200530 6

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 pe ...[more]

PMID: 32486128

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Project description:Silymarin (SIL) is a poorly water-soluble flavonoid reported for different pharmacological properties. Its therapeutic applications are limited due to poor water solubility. In this study, the solubility of silymarin has been enhanced by preparing freeze-dried binary and ternary complexes using beta cyclodextrin (βCD) and d-α-tocopherol polyethylene glycol 1000 succinate (TPGS). The stoichiometry of the drug and the carrier was selected from the phase solubility study. The dissolution study was performed to assess the effect of complexation on the release pattern of SIL. The formation of inclusion complexes was confirmed by different physicochemical studies. Finally, a cell viability assay (MCF 7; breast cancer cell line) was performed to compare the activity with free SIL. The phase solubilization results revealed the formation of a stable complex (binary) with a stability constant and complexation efficiency (CE) value of 288 mol L-1 and 0.045%. The ternary sample depicted a significantly enhanced stability constant and CE value (890 mol L-1 and 0.14%). The release study results showed a marked increase in the release pattern after addition of βCD (alone) in the binary mixture (49.4 ± 3.1%) as well as inclusion complex (66.2 ± 3.2%) compared to free SIL (32.7 ± 1.85%). Furthermore, with the addition of TPGS in SIL-βCD (ternary), the SIL release was found to be significantly enhanced from the SIL ternary mixture (79.2 ± 2.13%) in 120 min. However, fast SIL release was achieved with 99.2 ± 1.7% in 45 min for the SIL ternary complex. IR and NMR spectral analysis results revealed the formation of a stable complex with no drug-polymer interaction. The formation of complexes was also confirmed by the molecular docking study (docking scores of 4.1 and -6.4 kcal/mol). The in vitro cell viability result showed a concentration-dependent activity. The IC50 value of the SIL ternary complex was found to be significantly lower than that of free SIL. The findings of the study concluded that the prepared SIL inclusion complex can be used as an alternative oral delivery system to enhance solubility, dissolution, and biological activity against the tested cancer cell line.

Dataset Information

Anti-Inflammatory and Physicochemical Characterization of the Croton Rhamnifolioides Essential Oil Inclusion Complex in ?-Cyclodextrin.

Publications

Anti-Inflammatory and Physicochemical Characterization of the <i>Croton Rhamnifolioides</i> Essential Oil Inclusion Complex in β-Cyclodextrin.

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