Donor-Acceptor-Type Conjugated Polymer-Based Multicolored Drug Carriers with Tunable Aggregation-Induced Emission Behavior for Self-Illuminating Cancer Therapy.

Nowadays, multicolored drug carriers have exhibited high significance in designing self-illuminating drug delivery systems to adapt different experimental conditions. In this study, we developed an efficient strategy for self-illuminating antitumor therapy using multicolored aggregation-induced emission (AIE)-active drug carriers by tuning electron donor moieties in donor-acceptor (D-A) structures. Three amphipathic conjugated polymers, to , were successfully synthesized using an AIE-active tetraphenylethylene (TPE) moiety and donor-acceptor (D-A)-type electronic structure. Interestingly, the fluorescence behavior of to could be tuned between aggregation-caused quenching and AIE by changing the electron donor moiety. Their fluorescence color in aqueous solution could be easily adjusted from yellow to red by choosing stronger electron donors. After the anticancer drug paclitaxel was loaded, two AIE-active polymers, and , could be engineered into polymer dots (Pdots) and applied in self-illuminating cancer therapy. The Pdots could not only reveal their location by a yellow- or red-colored fluorescence signal but also exhibit almost two times in vivo antitumor efficacy, high biocompatibility, and obvious tumor-targeting behavior compared to the commercially available anticancer drug Taxol. Furthermore, dots exhibited similar in vivo antitumor efficacy and biocompatibility compared to nonemission Abraxane, a commercially available drug delivery system. This work demonstrates the significant application of a D-A-type structure in the design of self-illuminating drug delivery systems.