Targeted therapy of rheumatoid arthritis via macrophage repolarization
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...
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Taylor & Francis Group
2021
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oai:doaj.org-article:5628f207d0494f5fb46bdcb2522119ce2021-11-17T14:21:55ZTargeted therapy of rheumatoid arthritis via macrophage repolarization1071-75441521-046410.1080/10717544.2021.2000679https://doaj.org/article/5628f207d0494f5fb46bdcb2522119ce2021-01-01T00:00:00Zhttp://dx.doi.org/10.1080/10717544.2021.2000679https://doaj.org/toc/1071-7544https://doaj.org/toc/1521-0464The 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.Xu ZhouDandan HuangRunkong WangMingquan WuLiyang ZhuWei PengHe TuXuangeng DengHe ZhuZhong ZhangXinming WangXi CaoTaylor & Francis Grouparticlerheumatoid arthritismacrophage repolarizationfolate receptortriptolideliposomesTherapeutics. PharmacologyRM1-950ENDrug Delivery, Vol 28, Iss 1, Pp 2447-2459 (2021) |
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rheumatoid arthritis macrophage repolarization folate receptor triptolide liposomes Therapeutics. Pharmacology RM1-950 |
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rheumatoid arthritis macrophage repolarization folate receptor triptolide liposomes Therapeutics. Pharmacology RM1-950 Xu Zhou Dandan Huang Runkong Wang Mingquan Wu Liyang Zhu Wei Peng He Tu Xuangeng Deng He Zhu Zhong Zhang Xinming Wang Xi Cao Targeted therapy of rheumatoid arthritis via macrophage repolarization |
description |
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. |
format |
article |
author |
Xu Zhou Dandan Huang Runkong Wang Mingquan Wu Liyang Zhu Wei Peng He Tu Xuangeng Deng He Zhu Zhong Zhang Xinming Wang Xi Cao |
author_facet |
Xu Zhou Dandan Huang Runkong Wang Mingquan Wu Liyang Zhu Wei Peng He Tu Xuangeng Deng He Zhu Zhong Zhang Xinming Wang Xi Cao |
author_sort |
Xu Zhou |
title |
Targeted therapy of rheumatoid arthritis via macrophage repolarization |
title_short |
Targeted therapy of rheumatoid arthritis via macrophage repolarization |
title_full |
Targeted therapy of rheumatoid arthritis via macrophage repolarization |
title_fullStr |
Targeted therapy of rheumatoid arthritis via macrophage repolarization |
title_full_unstemmed |
Targeted therapy of rheumatoid arthritis via macrophage repolarization |
title_sort |
targeted therapy of rheumatoid arthritis via macrophage repolarization |
publisher |
Taylor & Francis Group |
publishDate |
2021 |
url |
https://doaj.org/article/5628f207d0494f5fb46bdcb2522119ce |
work_keys_str_mv |
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