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Design of Multifunctional Micelle for Tumor‐Targeted Intracellular Drug Release and Fluorescent Imaging

Figure 1. Illustrative preparation of PTX and QD-loaded micelle and pH-tunable drug release. Over the past two decades, nanoscale polymeric micelles have demonstrated great potential in delivering anticancer drugs.[1–3] However, in spite of the successes both in vitro and in vivo,[1a,b,4] application of polymeric micelles for drug delivery has encountered two intractable problems.[1c] At first, premature drug leakage exists in sample storage or during blood circulation. Secondly, accumulation of micelles in tumor tissues and cells is poor due to their easy clearance by reticuloendothelial system and lack of active targeting to tumor cells, which leads to the decreased therapeutic effect and causes undesired side effects of the transported anticancer drugs. So far, only few reports are available on regulating drug release property of polymeric micelles in terms of inhibiting premature drug leakage.[1d] On the other hand, accumulation of drug-loaded micelles in tumor cells can be enhanced by the active targeting strategy utilizing ligands to generate specific interaction between micelles and molecular bio-markers on tumor cell membranes.[1a,b,5] For instance, folic acid (FA) was employed to potentiate the gene and siRNA delivery to folate receptor (FR)-enriched tumors, which resulted in improved therapeutic effect both in vitro and in vivo.[6] Moreover, multifunctional nanocarriers combining imaging function with drug delivery are emerging as the next generation of nanomedicines to improve the outcome of drug therapy.[1b] To date, reports on polymeric micelles with a combined feature of