Tumor-targeting, enzyme-activated nanoparticles for simultaneous cancer diagnosis and photodynamic therapy.

Specific targeting towards tumors and the on-site activation of photosensitizers to diagnose tumors and reduce side effects for patients are currently the main challenges for photodynamic therapy (PDT) in the clinic. Herein, uniform diiodostyryl bodipy conjugated hyaluronic acid nanoparticles (DBHA-NPs) were successfully synthesized. The evaluation of their PDT effect at both a cellular level and in animal models of tumor-bearing mice shows that the DBHA-NPs present a remarkable suppression of tumorous growth due to their specific targeting and enhanced permeability and retention (EPR) effect. More importantly, the enzyme-activated "self-assembly and disaggregation" behavior in tumors can lead to the on-site activation of DBHA-NPs, which can diagnose the tumor exactly and reduce the side effects for patients significantly. These findings confirm that DBHA-NPs have significant potential for photodynamically activated cancer theranostics in a clinical setting.