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Quercetin-Loaded Microcapsules Ameliorate Experimental Colitis in Mice by Anti-inflammatory and Antioxidant Mechanisms

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    Quercetin-Loaded Microcapsules Ameliorate Experimental Colitis in Mice by Anti-inflammatory and Antioxidant Mechanisms
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    † Departamento de Ciências Patológicas—Centro de Ciências Biológicas, Universidade Estadual de Londrina, Londrina 86051-990, Brazil
    ‡ Departamento de Ciências Farmacêuticas—Centro de Ciências de Saúde, Universidade Estadual de Londrina, Londrina 86038-350, Brazil
    § Departamento de Ciências Farmacêuticas—Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto 14040-903, Brazil
    *Tel: + 55 43 3371 4979. Fax: + 55 43 3371 4387. E-mail: [email protected]; [email protected]
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    Journal of Natural Products

    Cite this: J. Nat. Prod. 2013, 76, 2, 200–208
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    https://doi.org/10.1021/np300670w
    Published January 24, 2013
    Copyright © 2013 The American Chemical Society and American Society of Pharmacognosy
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    Abstract

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    Quercetin (1) is an anti-inflammatory and antioxidant flavonoid. However, the oral administration of 1 did not lead to beneficial effects in experimental animal colitis models, which involve cytokines and oxidative stress. A possible explanation is that the absorption profile of 1 prevents its activity. Therefore, it was reasoned that the controlled release of 1 would improve its therapeutic effect. Thus, the therapeutic effect and mechanisms of 1-loaded microcapsules in acetic acid-induced colitis in mice were evaluated. Microcapsules were prepared using pectin/casein polymer and 1. The oral administration of 1-loaded microcapsules decreased neutrophil recruitment, attenuated histological alterations, and reduced macroscopical damage, edema, and IL-1β and IL-33 production in the colon samples. Microcapsules loaded with 1 also prevented the reduction of anti-inflammatory cytokine IL-10 and the antioxidant capacity of the colon. These preclinical data indicate that pectin/casein polymer microcapsules loaded with 1 improved the anti-inflammatory and antioxidant effects of 1 compared to the nonencapsulated drug. Therefore, quercetin seems to be a promising active molecule in inflammatory bowel disease if provided with adequate controlled release.

    Copyright © 2013 The American Chemical Society and American Society of Pharmacognosy

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    Cite this: J. Nat. Prod. 2013, 76, 2, 200–208
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    Published January 24, 2013
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