A novel dexamethasone-loaded liposome alleviates rheumatoid arthritis in rats

作者：Jia, Mengdi; Deng, Caifeng; Luo, Jingwen; Zhang, Pei; Sun, Xun; Zhang, Zhirong; Gong, Tao^*

来源：International Journal of Pharmaceutics, 2018, 540(1-2): 57-64.

DOI：10.1016/j.ijpharm.2018.02.001

• Dexamethasone
• Biodistribution
• Novel liposome
• Moderate toxic effects
• Clinical application
• Rheumatoid arthritis

In this study, an inflammation-targeted delivery system based on a liposomal carrier was developed to deliver hydrophobic dexamethasone against arthritis. Using two FDA-approved excipients for intravenous injection, dexamethasone loaded liposome (Dex-Lip) was prepared by a thin-film hydration method. The biodistribution of 1,1'-dioctadecyl-3,3,3',3'-tetramethylindodicarbocyanine-loaded liposomes (DiD-Lips) were performed in rats with adjuvant-induced arthritis and demonstrated specific targeting efficacy in the disease site. DiD-Lips showed prolonged retention time in the inflammatory joint tissues compared with free DiD. Dex-Lips effectively suppressed the joint swelling in arthritis rats and significantly down-regulated serum pro-inflammatory cytokines including tumor necrosis factor-alpha and interleukin-1 beta when compared to free dexamethasone. Furthermore, Dex-Lips had no significantly impact on the body weight, alleviated the hyperglycemia and improved haematological profiles of rheumatoid arthritis rats during the treatment process. Taken together, a safe liposomal delivery system was developed to achieve inflammation targeted therapy against arthritis.

• 出版日期2018-4-5
• 单位四川大学