Intra-Articular injection of acid-sensitive stearoxyl-ketal-dexamethasone microcrystals for long-acting arthritis therapy.

ABSTRACT: Despite advances in treatment of chronic arthritis, there is still a strong need for the development of long-acting formulations that can enable local and sustained drug release at the inflamed tissues. In this work, we fabricated microcrystals of an acid-sensitive stearoxyl-ketal-dexamethasone prodrug for treatment of arthritis. Microcrystals of the prodrug with two sizes were successfully engineered and showed pH-dependent hydrolysis kinetics in vitro. In a collagen-induced arthritis rat model, we evaluated the influence of particle size and injection dose on anti-inflammatory effect after intra-articular injection. Such prodrug demonstrated long-acting anti-arthritis effects with good safety. Our results indicate ketal-based prodrugs are promising for the development of long-acti

SUBMITTER: Xu Y 

PROVIDER: S-EPMC8105419 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature