A novel multifunctional aggregation-induced emission (AIE) nanoaggregate for targeted imaging and enzyme-triggered chemotherapy was successfully fabricated via a one-step assembly. In this system, a quaternary ammonium-modified tetraphenylethene derivative (QA-TPE) acted as the AIE fluorophore as well as the chemotherapeutic agent, and a water-soluble acidic polysaccharide, hyaluronic acid (HA) acted as the aggregation-inducing scaffold, AIE turn-on agent, and targeting agent for CD44 receptor-mediated cancer cells. More importantly, HA endowed the QA-TPE/HA nanoaggregate both good biocompatibility and hysteretic chemotherapy activity, which were achieved by controlling the release of QA-TPE using the endogenous HAase in CD44 receptor-mediated cancer cells.
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