Modular‐Peptides‐Based Ternary Complex for Precisely Tracking the Targeted Process and Delivery of Gene/Chemo‐Drug

Abstract Highly effective transporting and real‐time monitoring of the drug delivery system (DDS) has attracted much attention from researchers. However, separately tracking the multiple components in a complex DDS as well as its delivery process is challengeable. Here, a multi‐fluorescence‐labeled ternary complex is designed for delivering the therapeutic agents and monitoring the multiple components. Ternary complex (A@TR) is formed by three parts, including a) the carrier module TFD, which is a cell‐penetrating peptide (TAT) conjugated with anti‐cancer drug doxorubicin (DOX) and fluorescent molecule fluorescein isothiocyanate (FITC); b) therapeutic genes (ASO); c) the targeting module RDP based on a cyclic RGDFK peptide and aggregation‐induced‐emission luminogen PyTPE. The labeling of FITC through the covalent bond can stably track the location of anticancer drugs and genes in the long term. Meanwhile, the mark of PyTPE can monitor the process of targeting‐mediated endocytosis over time. After being internalized by tumor cells selectively, chemodrug and therapeutic genes can achieve a superior tumor inhibited effect. By utilizing the multi‐channel fluorescence, this ternary complex could achieve precisely monitoring the targeted binding process of DDS and delivery processes of therapeutic agents.