Abstract
A high level of intracellular reactive oxygen species (ROS) is one of the remarkable intrinsic features of cancer cells. Therefore, ROS-responsive drug carriers have received great attention for cancer-selective drug delivery. In this study, ROS-responsive thioether-bearing polymers (TEP) were synthesized for effective intracellular delivery of piperlongumine (PL) into cancer cells. PL is a pro-oxidant drug that induces cytotoxic oxidative stress in cancer cells. PL-loaded TEP nanoparticles (PL-TEP NPs) were successfully formulated by a nanoemulsion method. PL-TEP NPs showed ROS-sensitive disassembly, which leads to ROS-sensitive drug release. In addition, PL-TEP NPs showed higher cytotoxicity in human breast cancer cells (MCF-7) than in normal human dermal fibroblast cells (hDFB), demonstrating their cancer cell-specific pro-oxidant therapy. This study demonstrates that ROS-responsive TEP NPs are effective drug carriers for efficient intracellular delivery of hydrophobic drug, PL.
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