Abstract

Abstract Small molecule targeted inhibitor therapies often have several drawbacks, including limited oral bioavailability, quick metabolism, toxic effects that limit dosage, and poor water solubility. This study aims to develop a nanodrug self‐delivery system that does not require a carrier by utilizing the self‐assembly of camptothecin (CPT) and dihydroartemisinin (DHA). CPT/DHA nanoparticles (NPs) with varying diameters can be synthesized without requiring further carrier materials or chemical modifications by changing the CPT‐to‐DHA ratio (10:1, 5:1, 2:1, 1:1). Even more crucially, CPT/DHA NPs generate an AIE impact when they self‐assemble. CPT/DHA NPs are used for cell tracking and bioimaging fluorescent probes. We chose CPT/DHA NPs (2:1) with a size of approximately 140 nm for the anticancer examinations. The A549 cells were used to assess the cytotoxicity, morphological changes by biochemical staining methods and apoptosis by flow cytometric techniques of CPT/DHA NPs. Finally, in vitro anticancer research proved that CPT/DHA NPs are biocompatible and have strong synergistic anticancer properties.