Quercetin-loaded microcapsules ameliorate experimental colitis in mice by anti-inflammatory and antioxidant mechanisms.
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.
Departamento de Ciências Patológicas-Centro de Ciências Biológicas, Universidade Estadual de Londrina, Londrina, Brazil
Carla F S
CF
Guazelli
Victor
V
Fattori
Barbara B
BB
Colombo
Sandra R
SR
Georgetti
Fabiana T M C
FT
Vicentini
Rubia
R
Casagrande
Marcela M
MM
Baracat
Waldiceu A
WA
Verri
D019342:Acetic Acid / Q000009:adverse effects; D000284:Administration, Oral; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000032:analysis / Q000097:blood / Q000494:pharmacology* / Q000627:therapeutic use; D000975:Antioxidants / Q000032:analysis / Q000737:chemistry / Q000494:pharmacology*; D002214:Capsules; D003092:Colitis / Q000139:chemically induced* / Q000188:drug therapy; D004195:Disease Models, Animal; D016503:Drug Delivery Systems / Q000379:methods; D004487:Edema; D053583:Interleukin-1beta / Q000187:drug effects; D000067596:Interleukin-33; D007378:Interleukins / Q000378:metabolism; D008297:Male; D051379:Mice; D015394:Molecular Structure; D009504:Neutrophils / Q000187:drug effects; D009195:Peroxidase / Q000187:drug effects; D011794:Quercetin / Q000032:analysis / Q000097:blood / Q000737:chemistry / Q000494:pharmacology*
D000893:Anti-Inflammatory Agents; D000975:Antioxidants; D002214:Capsules; C506535:Il33 protein, mouse; D053583:Interleukin-1beta; D000067596:Interleukin-33; D007378:Interleukins; D011794:Quercetin; D009195:Peroxidase; D019342:Acetic Acid