title: Therapeutic efficacy of quercetin enzyme-responsive nanovesicles for the treatment of experimental colitis in rats.
abstract: Biocompatible quercetin nanovesicles were developed by coating polyethylene glycol-containing vesicles with chitosan and nutriose, aimed at targeting the colon. Uncoated and coated vesicles were prepared using hydrogenated soy phosphatidylcholine and quercetin, a potent natural anti-inflammatory and antioxidant drug. Physicochemical characterization was carried out by light scattering, cryogenic microscopy and X-ray scattering, the results showing that vesicles were predominantly multilamellar and around 130 nm in size. The in vitro release of quercetin was investigated under different pH conditions simulating the environment of the gastrointestinal tract, and confirmed that the chitosan/nutriose coating improved the gastric resistance of vesicles, making them a potential carrier system for colon delivery. The preferential localization of fluorescent vesicles in the intestine was demonstrated using the In Vivo FX PRO Imaging System. Above all, a marked amelioration of symptoms of 2,4,6-trinitrobenzenesulfonic acid-induced colitis was observed in animals treated with quercetin-loaded coated vesicles, favoring the restoration of physiological conditions. Therefore, quercetin-loaded chitosan/nutriose-coated vesicles can represent a valuable therapeutic tool for the treatment of chronic intestinal inflammatory diseases, and presumably a preventive system, due to the synergic action of antioxidant quercetin and beneficial prebiotic effects of the chitosan/nutriose complex.
authors.affiliation: Dept. Scienze della Vita e dell'Ambiente, University of Cagliari, Cagliari, Italy.
authors.forename: Ines
authors.initials: I
authors.lastname: Castangia
authors.affiliation: Dept. of Pharmacy and Pharmaceutical Technology, University of Valencia, Valencia, Spain; Institute of Molecular Recognition and Technological Development, Inter-Universitary Institute from Polytechnic University of Valencia and University of Valencia, Spain.
authors.forename: Amparo
authors.initials: A
authors.lastname: Nácher
authors.affiliation: Dept. Scienze della Vita e dell'Ambiente, University of Cagliari, Cagliari, Italy. Electronic address: caddeoc@unica.it.
authors.forename: Carla
authors.initials: C
authors.lastname: Caddeo
authors.affiliation: Dept. of Pharmacy and Pharmaceutical Technology, University of Valencia, Valencia, Spain; Institute of Molecular Recognition and Technological Development, Inter-Universitary Institute from Polytechnic University of Valencia and University of Valencia, Spain.
authors.forename: Virginia
authors.initials: V
authors.lastname: Merino
authors.affiliation: Dept. of Pharmacy and Pharmaceutical Technology, University of Valencia, Valencia, Spain; Institute of Molecular Recognition and Technological Development, Inter-Universitary Institute from Polytechnic University of Valencia and University of Valencia, Spain.
authors.forename: Octavio
authors.initials: O
authors.lastname: Díez-Sales
authors.affiliation: Dept. of Pharmacy and Pharmaceutical Technology, University of Valencia, Valencia, Spain; Institute of Molecular Recognition and Technological Development, Inter-Universitary Institute from Polytechnic University of Valencia and University of Valencia, Spain.
authors.forename: Ana
authors.initials: A
authors.lastname: Catalán-Latorre
authors.affiliation: Barcelona Centre for International Health Research (CRESIB, Hospital Clínic-Universitat de Barcelona), Barcelona, Spain; Institute for Bioengineering of Catalonia (IBEC), Barcelona, Spain.
authors.forename: Xavier
authors.initials: X
authors.lastname: Fernàndez-Busquets
authors.affiliation: Dept. Scienze della Vita e dell'Ambiente, University of Cagliari, Cagliari, Italy.
authors.forename: Anna Maria
authors.initials: AM
authors.lastname: Fadda
authors.affiliation: Dept. Scienze della Vita e dell'Ambiente, University of Cagliari, Cagliari, Italy.
authors.forename: Maria
authors.initials: M
authors.lastname: Manconi
mesh_terms: D000818:Animals; D000975:Antioxidants / Q000737:chemistry / Q000494:pharmacology; D048271:Chitosan / Q000737:chemistry / Q000494:pharmacology; D020099:Coated Materials, Biocompatible; D003092:Colitis / Q000151:congenital / Q000188:drug therapy / Q000201:enzymology / Q000473:pathology; D004337:Drug Carriers / Q000737:chemistry / Q000494:pharmacology; D008297:Male; D053758:Nanoparticles / Q000737:chemistry*; D011794:Quercetin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D014302:Trinitrobenzenesulfonic Acid / Q000633:toxicity
chemical_list: D000975:Antioxidants; D020099:Coated Materials, Biocompatible; D004337:Drug Carriers; C012526:quercitrin; D014302:Trinitrobenzenesulfonic Acid; D048271:Chitosan; D011794:Quercetin
keywords: Chitosan/nutriose complex; Colon targeting; Phospholipid vesicles; Quercetin; Rat colitis