Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 11, Issue 8, Pages 1562-1566Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.0c00212
Keywords
beta-D-Galactose-modified tetraphenylethenes; aggregation-induced emission; fluorescent vesicles; cell imaging; targeted drug delivery
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Funding
- NNSFC [U1604285, 21877206]
- PCSIRT [IRT1061]
- 111 Project [D17007]
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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 beta-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/beta-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.
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