Fabrication of AIE-Featured Probe-Incorporated Multifunctional Polymeric Micelles for Cellular Imaging and Intelligent Delivery of Paclitaxel

An aggregation-induced emission (AIE)-featured amphiphilic polymer was synthesized by linking hyaluronic acid (HA) with a tetraphenylethene (TPE) derivative via hydrazone bonds (HA-hyd-TPE). The polymer exhibited a powerful AIE effect and could self-assemble to form polymeric micelles. The paclitaxel (PTX)-loaded micelles had a mean size as low as 82.2 nm, with a drug loading capacity of 10.7% and an entrapment efficiency of 79.8%. According to in vitro drug release testing, the micelles exhibited a rapid release of PTX under acidic conditions. In vitro cell viability experiments indicated the significant inhibition ability of the micelles on the growth and proliferation of MCF-7 cells. Cellular uptake assessment confirmed the excellent cellular imaging capability of HA-hyd-TPE micelles, and the micelles could be specifically internalized by MCF-7 cells. Furthermore, the superior antitumor activity and negligible systemic toxicity of the micelles were demonstrated by an in vivo antitumor test. All results suggested that HA-hyd-TPE micelles might be promising carriers for both bioimaging and efficient cancer treatment.