title: Coated chitosan pellets containing rutin intended for the treatment of inflammatory bowel disease: in vitro characteristics and in vivo evaluation.
abstract: Preparation of coated pellets intended for rutin colon delivery, their evaluation in vitro and in vivo in experimental colitis in rats was the purpose of this study. Pellets were obtained using extrusion/spheronization and coated with three types of coatings (caffeic acid/hypromellose/alginic acid; sodium alginate/hypromellose/zinc acetate; sodium alginate/chitosan). Dissolution using buffers of pH values, β-glucosidase and times corresponding to gastrointestinal tract (GIT) was provided. Pellets coated with alginate/chitosan showed low rutin dissolution (12-14%) in upper GIT conditions and fast release (87-89%) under colon conditions; that is a good presumption of intended rutin release. After colitis induction and development, the rats were treated with pellets and rutin solution administered orally, solution also rectally. Colon/body weight ratio, myeloperoxidase activity and histological evaluation were performed. Rutin was able to promote colonic healing at the dose of 10mg/kg: colon/body weight ratio decreased and myeloperoxidase activity was significantly suppressed. Pellets coated with alginate/chitosan applied orally and rutin solution administered rectally showed the best efficacy. The combination of rutin as natural product, mucoadhesive chitosan degraded in the colon and sodium alginate as the main coating substance in the form of pellets create a promising preparation for therapy of this severe illness.
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackého 1-3, 612 42 Brno, Czech Republic. rabiskovam@vfu.cz
authors.forename: Miloslava
authors.initials: M
authors.lastname: Rabišková
authors.forename: Tereza
authors.initials: T
authors.lastname: Bautzová
authors.forename: Jan
authors.initials: J
authors.lastname: Gajdziok
authors.forename: Kateřina
authors.initials: K
authors.lastname: Dvořáčková
authors.forename: Alf
authors.initials: A
authors.lastname: Lamprecht
authors.forename: Yann
authors.initials: Y
authors.lastname: Pellequer
authors.forename: Jiřina
authors.initials: J
authors.lastname: Spilková
mesh_terms: D000284:Administration, Oral; D000464:Alginates / Q000737:chemistry; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D002021:Buffers; D002109:Caffeic Acids / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D048271:Chitosan / Q000737:chemistry*; D003092:Colitis / Q000139:chemically induced / Q000188:drug therapy* / Q000473:pathology; D003106:Colon / Q000187:drug effects* / Q000473:pathology; D004195:Disease Models, Animal; D004339:Drug Compounding; D004343:Drug Implants; D004355:Drug Stability; D005765:Gastrointestinal Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D065347:Hypromellose Derivatives; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D012431:Rutin / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods; D013997:Time Factors; D014302:Trinitrobenzenesulfonic Acid; D019345:Zinc Acetate / Q000737:chemistry
chemical_list: D000464:Alginates; D000893:Anti-Inflammatory Agents; D002021:Buffers; D002109:Caffeic Acids; D004343:Drug Implants; D005765:Gastrointestinal Agents; D006603:Hexuronic Acids; D065347:Hypromellose Derivatives; D012431:Rutin; D020723:Glucuronic Acid; D014302:Trinitrobenzenesulfonic Acid; D008747:Methylcellulose; D048271:Chitosan; D019345:Zinc Acetate; C040048:caffeic acid