Targeted therapy of rheumatoid arthritis via macrophage repolarization

Autor: Xu Zhou, Dandan Huang, Runkong Wang, Mingquan Wu, Liyang Zhu, Wei Peng, He Tu, Xuangeng Deng, He Zhu, Zhong Zhang, Xinming Wang, Xi Cao
Jazyk: angličtina
Rok vydání: 2021
Předmět:
Zdroj: Drug Delivery, Vol 28, Iss 1, Pp 2447-2459 (2021)
Druh dokumentu: article
ISSN: 1071-7544
1521-0464
10717544
DOI: 10.1080/10717544.2021.2000679
Popis: 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 to explore the biodistribution profiles of FA-Lips which showed markedly selective accumulation in inflammatory paws. Moreover, FA-Lips/TP exhibited greatly improved therapeutic efficacy and low toxicity in AIA rats by targeting M1 macrophages and repolarizing macrophages from M1 to M2 subtypes. Overall, a safe FA-modified liposomal delivery system encapsulating TP was shown to achieve inflammation-targeted therapy against RA via macrophage repolarization.
Databáze: Directory of Open Access Journals