PEGylated retinoate prodrug self-assembled nanomicelles loaded with triptolide for targeting treatment of rheumatoid arthritis and side effect attenuation
Huanhuan Zhu , Zhenzhen Wang , Jingru Cui , Yaning Ge , Min Yan , Xiangxiang Wu , Xiaofang Li , Huahui Zeng
{"title":"PEGylated retinoate prodrug self-assembled nanomicelles loaded with triptolide for targeting treatment of rheumatoid arthritis and side effect attenuation","authors":"Huanhuan Zhu , Zhenzhen Wang , Jingru Cui , Yaning Ge , Min Yan , Xiangxiang Wu , Xiaofang Li , Huahui Zeng","doi":"10.1016/j.colsurfb.2025.114618","DOIUrl":null,"url":null,"abstract":"<div><div>Triptolide (TP, an active ingredient from <em>Tripterygium wilfordii</em>) demonstrates significant efficacy in treating rheumatoid arthritis, but its low bioavailability and multi-organ toxicity limit its application. Herein, we developed a PEGylated retinoate self-assembled nanomicelles (FA-TP@VA NPs) modified with folic acid (FA) for inflammatory macrophage-targeted delivery of TP. FA-TP@VA NPs showed an appropriate size (192.70 ± 4.37 nm), good physical stability and high drug loading (79.83 ± 5.11 % for retinoate prodrug and 6.78 ± 0.13 % for TP). FA-TP@VA NPs exhibited high cellular uptake in M1 macrophages via folate-receptor pathway, thereby inhibiting their growth. Compared with TP, FA-TP@VA NPs could effectively inhibit synovitis and erosion of bone and reduce swelling and deformation of paws by downregulation of the levels of IL-1β, IL-6, and TNF-α. In ICA mice, FA-TP@VA NPs could enhance drug-specific enrichment in inflamed joints, effectively suppress hepatic oxidative stress and reduce systemic toxicity induced by TP. Overall, FA-TP@VA NPs are a facile, carrier-free, and promising strategy for the precise treatment of rheumatoid arthritis and synergetic attenuation of side effect.</div></div>","PeriodicalId":279,"journal":{"name":"Colloids and Surfaces B: Biointerfaces","volume":"251 ","pages":"Article 114618"},"PeriodicalIF":5.4000,"publicationDate":"2025-03-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Colloids and Surfaces B: Biointerfaces","FirstCategoryId":"1","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0927776525001250","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"BIOPHYSICS","Score":null,"Total":0}
引用次数: 0
Abstract
Triptolide (TP, an active ingredient from Tripterygium wilfordii) demonstrates significant efficacy in treating rheumatoid arthritis, but its low bioavailability and multi-organ toxicity limit its application. Herein, we developed a PEGylated retinoate self-assembled nanomicelles (FA-TP@VA NPs) modified with folic acid (FA) for inflammatory macrophage-targeted delivery of TP. FA-TP@VA NPs showed an appropriate size (192.70 ± 4.37 nm), good physical stability and high drug loading (79.83 ± 5.11 % for retinoate prodrug and 6.78 ± 0.13 % for TP). FA-TP@VA NPs exhibited high cellular uptake in M1 macrophages via folate-receptor pathway, thereby inhibiting their growth. Compared with TP, FA-TP@VA NPs could effectively inhibit synovitis and erosion of bone and reduce swelling and deformation of paws by downregulation of the levels of IL-1β, IL-6, and TNF-α. In ICA mice, FA-TP@VA NPs could enhance drug-specific enrichment in inflamed joints, effectively suppress hepatic oxidative stress and reduce systemic toxicity induced by TP. Overall, FA-TP@VA NPs are a facile, carrier-free, and promising strategy for the precise treatment of rheumatoid arthritis and synergetic attenuation of side effect.
期刊介绍:
Colloids and Surfaces B: Biointerfaces is an international journal devoted to fundamental and applied research on colloid and interfacial phenomena in relation to systems of biological origin, having particular relevance to the medical, pharmaceutical, biotechnological, food and cosmetic fields.
Submissions that: (1) deal solely with biological phenomena and do not describe the physico-chemical or colloid-chemical background and/or mechanism of the phenomena, and (2) deal solely with colloid/interfacial phenomena and do not have appropriate biological content or relevance, are outside the scope of the journal and will not be considered for publication.
The journal publishes regular research papers, reviews, short communications and invited perspective articles, called BioInterface Perspectives. The BioInterface Perspective provide researchers the opportunity to review their own work, as well as provide insight into the work of others that inspired and influenced the author. Regular articles should have a maximum total length of 6,000 words. In addition, a (combined) maximum of 8 normal-sized figures and/or tables is allowed (so for instance 3 tables and 5 figures). For multiple-panel figures each set of two panels equates to one figure. Short communications should not exceed half of the above. It is required to give on the article cover page a short statistical summary of the article listing the total number of words and tables/figures.