Targeted therapy of rheumatoid arthritis via macrophage repolarization

Xu Zhou, Dandan Huang, Runkong Wang, Mingquan Wu, Liyang Zhu, Wei Peng, He Tu, Xuangeng Deng, He Zhu, Zhong Zhang, Xinming Wang & Xi Cao
The polarization of macrophages plays a critical role in the physiological and pathological progression of rheumatoid arthritis (RA). Activated M1 macrophages overexpress folate receptors in arthritic joints. Hence, we developed folic acid (FA)-modified liposomes (FA-Lips) to encapsulate triptolide (TP) (FA-Lips/TP) for the targeted therapy of RA. FA-Lips exhibited significantly higher internalization efficiency in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells than liposomes (Lips) in the absence of folate. Next, an adjuvant-induced arthritis (AIA) rat model was established...
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