Kartogenin Conjugated Chitosan-Nano/Microparticles for the Intra-Articular Osteoarthritis Treatment

摘要

The conjugation of amine group of CS and carboxylic group of KGN was successfully carried out with EDC/NHS catalysis. The hydrophobic KGN could reside inside of the CS-KGN conjugated particles during ionic gelation with TPP. In vitro release studies demonstrated that the release of KGN from CS-KGN particles was delayed by the conjugation of KGN with CS. Due to the localized nature of the disease, IA drug injection is an attractive treatment approach for OA. However, the potential benefits of IA therapy for OA are not achieved using currently available medications and delivery vehicles due to the rapid clearance of therapeutic substances from the synovial space. In this study, the designed particles showed long retention time up to 3 weeks. In conclusion, CS-KGN conjugated particles have considerable potential for creating a sustained release KGN delivery system and providing long-term exposure of KGN in OA joint.