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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Autores principales: Xu Zhou, Dandan Huang, Runkong Wang, Mingquan Wu, Liyang Zhu, Wei Peng, He Tu, Xuangeng Deng, He Zhu, Zhong Zhang, Xinming Wang, Xi Cao
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Lenguaje:EN
Publicado: Taylor & Francis Group 2021
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Acceso en línea:https://doaj.org/article/5628f207d0494f5fb46bdcb2522119ce
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spelling 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)
institution DOAJ
collection DOAJ
language EN
topic rheumatoid arthritis
macrophage repolarization
folate receptor
triptolide
liposomes
Therapeutics. Pharmacology
RM1-950
spellingShingle 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
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