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[Display omitted] • Cur@PLGA-NPs are a novel AIE formulation capable of providing rich optical properties. • Hydrophobic interaction, electrostatic interaction, and π-π conjugation are responsible for the AIE properties. • The curcumin-based nano-AIE formulation could be successful used to image live cells. To revise the emission of curcumin (Cur) from "off" to "on", poly (D, L-lactide-co-glycolide) acid (PLGA) nanoparticles loaded with Cur were embedded in a polyvinyl alcohol (PVA) emulsifier (named Cur@PLGA-NPs). First, the emission intensities of different nanoformulations, including liposomes, bovine serum albumin (BSA) nanoparticles, and PLGA nanoparticles, were examined to discover the most effective carriers for Cur luminescence. As a result, Cur@PLGA-NPs exhibited the highest fluorescence intensity due to aggregation-induced emission (AIE), with quantum yields of 23.78% in aqueous solution and 21.52% in the solid state. According to X-ray diffraction (XRD) data, Cur@PLGA-NPs existed in the amorphous state, with a size of 217.2 ± 5.2 nm, an encapsulation efficiency (EE) of 69.98%, and a drug loading efficiency (LE) of 1.37%. The intramolecular interactions, which included hydrophobic interactions, electrostatic interactions, π-π interactions and solvatochromic effects, stabilized the chromophore cluster of Cur@PLGA-NPs in terms of nanoparticle formulation. Compared with free Cur, Cur@PLGA-NPs sensitized CT26 cells more efficiently with an IC 50 value of 16.9 μmol/L and an apoptotic rate of 17.20% at 10 μmol/L Cur. Because of the robust fluorescence emission based on AIE, Cur@PLGA-NPs were utilized as a nano-AIE probe for cell bioimaging, and many red fluorescent signals were observed in CT26 cells after treatment. These results suggest that Cur@PLGA-NPs provide a novel amorphous AIE formulation with imaging and bioactive capabilities. [ABSTRACT FROM AUTHOR]