Self-Assembly of Amphiphilic Drug-Dye Conjugates into Nanoparticles for Imaging and Chemotherapy

摘要

An amphiphilic drug-dye conjugate (PTX-Pt-BDP) was designed and synthesized with a platinum compound as the hydrophilic head. The precursor of PTX-Pt-BDP was obtained under mild conditions by means of a three-component Passerini reaction. PTX-Pt-BDP could self-assemble into nanoparticles (PTX-Pt-BDP NPs) in aqueous solution via a nanoprecipitation method. The obtained nanoparticles exhibited favorable structural stability in both water and physiological environment. PTX-Pt-BDP NPs could be endocytosed by cancer cells as revealed by confocal laser scanning microscopy and exert potent cytotoxicity. This work highlights the potential of nanomedicines from amphiphilic drug-dye conjugates for cancer cell imaging and chemotherapy.