Carrier-free Nanodrug for the Chemical-Photodynamic Synergistic Treatment of Lung Cancer

Abstract

The theophylline derivative d17 is a candidate drug for nonsmall cell lung cancer (NSCLC) treatment previously developed by our group. However, it has the limitations of inadequate bioavailability, poor targeting, and insignificant therapeutic effect. Chemo-photodynamic synergistic therapy is a promising method of synergistic antitumor therapy. Herein, d17 and photosensitizer chlorin e6 (Ce6) were loaded into nanoparticles (NPs) via supramolecular self-assembly, which are selfassembled through π−π stacking and hydrogen bond interactions to form nanospheres with a size of about 85 nm and a surface charge of −33 mV. Compared with free Ce6, the d17−Ce6 NPs have good hydrophilicity and stability and can effectively accumulate in NSCLC tumor tissues due to the enhancement and retention effect. More significantly, the d17−Ce6 NPs can synergistically inhibit tumor growth compared with other treatment groups with no obvious toxicity. Taken together, the d17−Ce6 NPs may be an effective carrier-free nanodrug for the chemophotodynamic synergistic treatment of NSCLC.