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

ABSTRACT: 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.

SUBMITTER: Ma W 

PROVIDER: S-EPMC7430949 | biostudies-literature | 2020 Aug

REPOSITORIES: biostudies-literature