Open AccessAn Amphiphilic Micromolecule Self-Assembles into Vesicles for Visualized and Targeted Drug Delivery
Author(s) -
Wei Ma,
Jing Bi,
Hao Wu,
Guisheng Zhang
Publication year - 2020
Publication title -
acs medicinal chemistry letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.065
H-Index - 66
ISSN - 1948-5875
DOI - 10.1021/acsmedchemlett.0c00212
Subject(s) - amphiphile , moiety , vesicle , conjugate , in vivo , doxorubicin , chemistry , in vitro , drug delivery , biophysics , ligand (biochemistry) , combinatorial chemistry , biochemistry , stereochemistry , chemotherapy , receptor , membrane , biology , copolymer , organic chemistry , mathematical analysis , genetics , mathematics , microbiology and biotechnology , polymer
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.