An activatable fluorescent prodrug of paclitaxel and BODIPY

Abstract

Chemotherapy benefits can be greatly boosted by developing multifunctional prodrug nanoplatforms with high drug loading and spatially and temporally regulated drug release. Here, we report a tumorous heterogeneity-activatable prodrug (PTX-S-BDP), bridging paclitaxel (PTX) and BODIPY (BDP-OH) with a redox stress responsive linker, for fluorescence imaging-guided chemotherapy. PTX-S-BDP was co-assembled with Pluronic F-127 to obtain PTX-S-BDP nanoparticles (PTX-S-BDP NPs) with water dispersibility. The emerging nanoplatform contributes to visual chemotherapy modality, by virtue of refined cellular real-time localization of chemotherapeutics through the fluorescence of BDP-OH. In addition, in vitro experiments verify that PTX-S-BDP NPs exhibit comparable cytotoxicity to Taxol, superior cellular imaging, and better cell selectivity to cancer cells. The novel prodrug nanoplatform overcomes the challenge of PTX hydrophobicity, low drug loading, and uncontrolled drug retention and release, and is anticipated to provide some reference value in the development of prodrugs in the future.