1. PH-sensitive BSA-modified resveratrol micelles targeting macrophages alleviate symptoms of rheumatoid arthritis.
- Author
-
Xie H, Zhao J, Wang S, Kong L, Li X, Aga E, Gong Ga LZ, and Ye B
- Subjects
- Animals, Mice, RAW 264.7 Cells, Hydrogen-Ion Concentration, Male, Anti-Inflammatory Agents pharmacology, Anti-Inflammatory Agents therapeutic use, Anti-Inflammatory Agents chemistry, Cytokines metabolism, Humans, Drug Carriers chemistry, Resveratrol pharmacology, Resveratrol therapeutic use, Resveratrol chemistry, Serum Albumin, Bovine chemistry, Micelles, Macrophages drug effects, Macrophages immunology, Arthritis, Rheumatoid drug therapy
- Abstract
Rheumatoid arthritis (RA) is a chronic autoimmune inflammatory disease, leading to severe inflammatory infiltration and joint damage, accompanied by a decrease in pH of joint microenvironment. Macrophages play an important role in the pathogenesis of RA, with high expression of bovine serum albumin (BSA) receptors on the surface of macrophages. Resveratrol (Res) has strong anti-inflammatory effects, but its application is limited due to its poor water solubility and low bioavailability. Therefore, we constructed pH-sensitive micelles by encapsulating Res and modifying BSA on the surface of the micelles (BSA-Res@Ms), thereby greatly improving the therapeutic effect of RA. Our research results indicated that BSA-Res@Ms had a smooth and uniform appearance, small particle size, high drug encapsulation efficiency, good stability, and pH-sensitive properties. In vitro, BSA-Res@Ms increased the uptake of Res by RAW264.7 cells, reduced the levels of pro-inflammatory cytokines and cleared excess ROS produced by activated RAW264.7 cells, and inhibited the generation of osteoclasts. In vivo, BSA-Res@Ms could target inflamed joint sites, significantly alleviate joint inflammation symptoms, inhibit activated macrophages, improve synovial hyperplasia and inflammatory cell infiltration, and protect cartilage. BSA-Res@Ms provide a very promising method for the treatment of RA, which can effectively improve the inflammatory manifestations of RA., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024. Published by Elsevier B.V.)
- Published
- 2024
- Full Text
- View/download PDF