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

作　　者：Yang Xu Ziqi Chen Zunkai Xu Yanyan Du Jianghao Han Xiaoyong Yuan Shubiao Zhang Shutao Guo 

机构地区：[1]Key Laboratory of Functional Polymer Materials of Ministry of Education,State Key Laboratory of Medicinal Chemical Biology and Institute of Polymer Chemistry,College of Chemistry,Nankai University,Tianjin 300071,China [2]Key Laboratory of Biotechnology and Bioresources Utilization of Ministry of Education,Dalian Minzu University,Dalian 116600,China [3]Clinical College of Ophthalmology,Tianjin Medical University,Tianjin Eye Hospital,Tianjin Key Laboratory of Ophthalmology and Visual Science,Tianjin Eye Institute,Tianjin 300022,China

出　　处：《Asian Journal of Pharmaceutical Sciences》2021年第2期213-221,共9页亚洲药物制剂科学（英文）

基　　金：We acknowledge financial support from the National Natural Science Foundation of China(51773098,81670817,81970772,21908019 and 21776044);Natural Science Foundation of Tianjin City of China(18JCYBJC28300);the Fundamental Research Funds for Central Universities(China).

摘　　要：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-acting injectables and may stimulate the development of new treatments for chronic diseases.

关 键 词：MICROCRYSTALS DEXAMETHASONE PRODRUGS Long-acting formulations ARTHRITIS 

分 类 号：R943[医药卫生—药剂学]