DOX Loaded Aggregation-induced Emission Active Polymeric Nanoparticles as a Fluorescence Resonance Energy Transfer Traceable Drug Delivery System for Self-indicating Cancer Therapy.

In this study, an AIE-active polymer (FTP) was successfully prepared and employed to load anti-cancer drug doxorubicin (DOX) for self-indicating cancer therapy via dual FRET process. Our results demonstrated that the FTP polymer could self-assemble into nanoparticles (NPs) in aqueous solutions to give strong fluorescence emission via intramolecular FRET process. The DOX loaded FTP NPs (drug loading content: 21.77%) were homogeneous particles with size around 50 nm and neutral surface charge, which showed preferable colloidal stability, hemolysis and selective drug release with comparable in vivo antitumor effects to DOX·HCl. In particular, the FRET process between FTP (donor) and DOX (acceptor) could serve as indicator for monitoring the in vitro and in vivo drug release profile, which might be a promising platform to realize real-time monitoring of drug localization and release during the delivery process. STATEMENT OF SIGNIFICANCE: 1. An amphiphilic polymer containing aggregation-induced emission segments and polyethylene glycol (PEG) chains (FTP) was firstly synthesized, which is capable of exerting strong fluorescence via intramolecular Förster resonance energy transfer (FRET) in the aggregate state. 2. The FTP polymer could self-assembled into homogeneous nanoparticles in aqueous environment with decent DOX loading capacity. 3. The DOX loaded FTP nanoparticles can afford FRET-traceable monitoring of the drug release both in vitro and in vivo.