Evaluation of the Safety and Gastrointestinal Migration of Guanidinylated Chitosan after Oral Administration to Rats

Arginine-rich membrane-permeable peptides (APPs) can be delivered to cells by forming complexes with various membrane-impermeable bioactive molecules such as proteins. We recently reported on the preparation of guanidinylated chitosan (GCS) that mimics arginine peptides, using chitosan, a naturally occurring cationic polysaccharide, and confirmed it enhances protein permeability in an vitro cell system. However, studies vivo safety GCS are not available. To address this, we evaluated its translocation into gastrointestinal tract rats after single oral administration excessive dose (500 mg/kg) observed changes body weight, major organ weights, tissue sections for periods up 2 weeks. The results indicated causes no deleterious effects. rhodamine-labeled evaluation migration suggested disappearance from appeared slower than non-dose group pre-guanidinylated due mucoadhesive properties. In future, plan investigate use improve absorption Class III IV drugs, which poorly water-soluble well membrane-permeable.