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

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 self-assembled 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 chemo-photodynamic synergistic treatment of NSCLC.