Disulfide-based PEGylated prodrugs: Reconversion kinetics, self-assembly and antitumor efficacy

Rational Engineering Docetaxel Prodrug Nanoassemblies: Response Modules Guiding Efficacy Enhancement and Toxicity Reduction

“…In short, the fabricated prodrugs usually consist of three modules, including active drug modules, response modules and modification modules. The modification modules generally have good biocompatibility and can balance the intermolecular forces between DTX molecules to avoid aggregation. , The response modules play a vital role of controlling the intelligent drug release in tumor cells, which is essential for inhibiting the malignant proliferation of tumor cells and safety. , According to the specific redox-microenvironment of tumor cells, many sensitive bonds are chosen as response modules to selectively release active drugs. − Among them, disulfide bonds are extensively used due to their distinct dual redox-responsiveness. − Since DTX is a potent chemotherapy drug with a low tolerance dose in clinic, we wonder whether there is a delicate balance of retaining antitumor potency and good tolerance by choosing appropriate response modules to construct DTX prodrugs. Moreover, as a significant part of the prodrugs, we wonder whether the subtle difference on structural positions of disulfide bonds could affect the assemble ability, activation sensibility, cytotoxicity, delivery efficacy, antitumor potency, and systematic toxicity of DTX prodrug nanoassemblies.…”