Targeting Macrophages and Synoviocytes Intracellular Milieu to Augment Anti‐Inflammatory Drug Potency

Using a preclinical in vivo model of arthritis and the gold standard disease-modifying anti-rheumatic drug, methotrexate, pH-responsive phosphorylcholine polymersomes, elicit both anti-inflammatory anti-arthritic therapeutic efficacy, while drastically minimizing off-target toxicity. First, selective accumulation polymersomes within synovium inflamed joints. Second, targeting ability toward activated macrophages synoviocytes, via scavenger receptors, allow their uptake endocytosis. And third, pH-responsiveness enables drug escape from early endosomes hence its intracellular milieu delivery. On-site augment methotrexate loaded enable complete abrogation synovial inflammation prevent disease progression severity. Overall, vitro investigations reveal potential as promising nanotherapy for treating arthritic inflammation.