Coated chitosan pellets containing rutin intended for the treatment of inflammatory bowel disease: in vitro characteristics and in vivo evaluation
Language English Country Netherlands Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
22079717
DOI
10.1016/j.ijpharm.2011.10.045
PII: S0378-5173(11)01024-6
Knihovny.cz E-resources
- MeSH
- Alginates chemistry MeSH
- Anti-Inflammatory Agents administration & dosage chemistry pharmacology MeSH
- Administration, Oral MeSH
- Time Factors MeSH
- Chemistry, Pharmaceutical MeSH
- Chitosan chemistry MeSH
- Hypromellose Derivatives MeSH
- Technology, Pharmaceutical methods MeSH
- Gastrointestinal Agents administration & dosage chemistry pharmacology MeSH
- Colitis chemically induced drug therapy pathology MeSH
- Colon drug effects pathology MeSH
- Hydrogen-Ion Concentration MeSH
- Rats MeSH
- Glucuronic Acid chemistry MeSH
- Trinitrobenzenesulfonic Acid MeSH
- Hexuronic Acids chemistry MeSH
- Caffeic Acids chemistry MeSH
- Drug Implants MeSH
- Methylcellulose analogs & derivatives chemistry MeSH
- Disease Models, Animal MeSH
- Zinc Acetate chemistry MeSH
- Rats, Wistar MeSH
- Drug Compounding MeSH
- Buffers MeSH
- Solubility MeSH
- Rutin administration & dosage chemistry pharmacology MeSH
- Drug Stability MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Male MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Alginates MeSH
- Anti-Inflammatory Agents MeSH
- caffeic acid MeSH Browser
- Chitosan MeSH
- Hypromellose Derivatives MeSH
- Gastrointestinal Agents MeSH
- Glucuronic Acid MeSH
- Trinitrobenzenesulfonic Acid MeSH
- Hexuronic Acids MeSH
- Caffeic Acids MeSH
- Drug Implants MeSH
- Methylcellulose MeSH
- Zinc Acetate MeSH
- Buffers MeSH
- Rutin MeSH
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.
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