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An Amphiphilic Micromolecule Self-Assembles into Vesicles for Visualized and Targeted Drug Delivery.

Described here is the first example of the construction of multifunctional drug delivery systems by employing an amphiphilic micromolecule. The intrinsic aggregation-induced emissive and tumor-targeting amphiphilic conjugate of β-d-galactose with tetraphenylethene (TPE-Gal), in which the hydrophobic TPE moiety spontaneously acts as the imaging chromophore and the hydrophilic Gal moiety spontaneously acts as the targeting ligand and galactosidase trigger, can self-assemble into fluorescent vesicles that can efficiently load both water-soluble and -insoluble anticancer drugs. In vitro and in vivo evaluations revealed that the pH/β-d-galactosidase dual-responsive doxorubicin (DOX)-loaded vesicles TPE-Gal@DOX exhibited good targeting effect and higher antitumor efficacy than free DOX. H&E staining analysis displayed remarkable necroses and weak cell proliferation in the tumor area and no toxicity to major organs, indicating the superior targeting antitumor therapeutic efficacy of TPE-Gal@DOX.