Paclitaxel Prodrug Nanomedicine for Potential CT-imaging Guided Breast Cancer Therapy

Nanotheranostics, which combine the therapeutic and diagnostic functions in one integrated system, have received extensive attentions in cancer treatments because they enable non-invasive diagnosis, tumor-targeted drug delivery, and real-time monitoring of therapeutic response. However, due to the high systemic toxicity of commonly used chemotherapeutics, current treatment still has limitations. Herein, to simultaneously achieve safe cancer therapy and therapeutic response monitoring, an iodinated prodrug strategy was proposed. 2,3,5-Triiodobenzoic acid (TIBA) was used to modify both paclitaxel (PTX) and the polymeric vehicle, so that the encapsulation efficiency of PTX could be increased and the systemic toxicity could be reduced. As-prepared prodrug nanoparticles could accumulate passively in the tumor site and promptly release loaded drugs in response to the overexpressed GSH in cancer cells, which then caused efficient cell cycle arrest and apoptosis like that of the parent PTX. With this rational design, safe and efficient antitumor therapy and real-time computer tomography (CT) imaging could be simultaneously realized, facilitating potential CT imaging-guided therapy of metastatic breast cancer.