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Background: Artesunate (ASA) acts as an •O₂ - source through the breakdown of endoperoxide bridges catalyzed by Fe 2+ , yet its efficacy in ASA-based nanodrugs is limited by poor intracellular delivery., Methods: ASA-hyaluronic acid (HA) conjugates were formed from hydrophobic ASA and hydrophilic HA by an esterification reaction first, and then self-targeting nanomicelles (NM) were developed using the fact that the amphiphilic conjugates of ASA and HA are capable of self-assembling in aqueous environments., Results: These ASA-HA NMs utilize CD44 receptor-mediated transcytosis to greatly enhance uptake by breast cancer cells. Subsequently, endogenous Fe 2+ from the tumor catalyzes the released ASA to produce highly toxic •O₂ - radicals to kill tumor cells, although sustained tumor growth inhibition can be achieved via in vivo experiments., Conclusions: Self-targeting NMs represent a promising strategy for enhancing ASA-based treatments, leveraging clinically approved drugs to expedite drug development and clinical research in oncology., (© 2024 The Author(s). Animal Models and Experimental Medicine published by John Wiley & Sons Australia, Ltd on behalf of The Chinese Association for Laboratory Animal Sciences.)