Pre-blocked molecular shuttle as an in-situ real-time theranostics.


Key Laboratory of Smart Drug Delivery (Ministry of Education), State Key Laboratory of Medical Neurobiology, Department of Pharmaceutics, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai, 201203, PR China. Electronic address: [Email]


Real-time monitor of drug-release from drug formulations in a noninvasive way can provide spatio-temporal information for drug activation and guide further clinical rational administration. In this work, a molecular shuttle, as a typical nanosized artificial molecular machine, was managed to act as a conceptually-new nanotheranostics for oxaliplatin. A post-recognition strategy was utilized, where a default supramolecular-dye couple was pre-blocked. The rational design, synthesis, characterization and proof-of-concept of this strategy were described in detail. The drug-release upon reducing environment can be translated into near-infrared (NIR) fluorescence signal (OFF-to-ON), allowing to track the drug-release procedure by multi-modal images including IVIS, FLECT and photoacoustic imaging. The versatile nanotheranostics system can target to triple negative breast tumor via conjugated F3 peptide, and show an improved anti-tumor efficacy with much lower side effect. The intelligent nanotheranostics system based on molecular shuttle provides new reference for precision medicine in preclinical trial and postclinical evaluation.


Molecular recognition,Molecular shuttle,Oxaliplatin,Real-time monitoring,Theranostics,

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