Abstract
Methotrexate (MTX) is an anchor drug for the treatment of rheumatoid arthritis (RA); however, long-term and high-dose usage of MTX for patients can cause many side effects and toxic reactions. To address these difficulties, selectively delivering MTX to the inflammatory site of a joint is promising in the treatment of RA. In this study, we prepared MTX-PEI@HA nanoparticles (NPs), composed of hyaluronic acid (HA) as the hydrophilic negative electrical shell, and MTX-linked branched polyethyleneimine (MTX-PEI) NPs as the core. MTX-PEI@HA NPs were prepared in the water phase by a one-pot method. The polymeric NPs were selectively internalized via CD44 receptor-mediated endocytosis in the activated macrophages. In the in vivo mice mode study, treatment with MTX-PEI@HA NPs mitigated inflammatory arthritis with notable safety at a high dose of MTX. We highlight the distinct advantages of aqueous-synthesized NPs coated with HA for arthritis-selective targeted delivery, thus verifying MTX-PEI@HA NPs as a promising MTX-based nanoplatform for treatment of RA.
Highlights
Methotrexate (MTX) is an anchor drug for the treatment of rheumatoid arthritis (RA); long-term and high-dose usage of MTX for patients can cause many side effects and toxic reactions
Drug loading via electrostatic interaction is a straightforward method in nanoplatform
In order to explore its possibility, we first studied the interaction between methotrexate and PEI
Summary
Methotrexate (MTX) is an anchor drug for the treatment of rheumatoid arthritis (RA); long-term and high-dose usage of MTX for patients can cause many side effects and toxic reactions. To address these difficulties, selectively delivering MTX to the inflammatory site of a joint is promising in the treatment of RA. Since the re-introduction of methotrexate (MTX) in the early 1980 s, MTX has become the most highly effective, fast-acting, disease modifying anti-rheumatic drug and is one of the most widely used and the first-line DMARD for the treatment of RA [9,10,11]. Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations
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