Infrared Responsive Choline Phosphate Lipids for Synergistic Cancer Therapy

Graphical Spot on : A light-inducible Lip-cRGDfk/ICG/Dox liposome simultaneously loads a water-soluble drug (Dox) and photothermal transduction agents (ICG), targets the tumor site, and locally heats it up under external laser irradiation. Due to the conformational transformation of CP lipids, the anticancer drug Dox is released at a specific time and in a specific space to kill tumor cells. This brings about a combination of chemotherapy and photothermal therapy for the noninvasive treatment of tumors. Choline phosphate lipids have been designed and developed as new-generation zwitterionic nanocarriers with excellent biocompatibility and bioorthogonality to provide a more programmable performance for cancer therapy. However, there is a lack of spatiotemporal and reversible control for drug release at target tumor cells, which can lead to severe adverse effects to normal tissue and discounted treatment outcome. Here, light-inducible Lip-cRGDfk/ICG/Dox liposomes were developed for synergistic cancer therapy. ICG can effectively convert light energy into selective heating in a local environment upon laser irradiation, thus inducing thermal ablation of tumor cells, and further reversibly trigger the spatiotemporal release of anticancer drugs (Dox) at tumor cells due to the conformation transformation of CP lipids to synergistically kill tumor cells. That Lip-cRGDfk/ICG/Dox exhibited a significant improvement for breast cancer therapy in vitro and in vivo is also demonstrated, thus it can serve as an efficient platform to noninvasively and spatiotemporally control the activation of cytotoxicity at tumor cells for precision cancer therapy.