Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, 110016, PR China.
Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, 110016, PR China.
Int J Pharm. 2023 Nov 25;647:123537. doi: 10.1016/j.ijpharm.2023.123537. Epub 2023 Oct 20.
The high level of reactive oxygen species (ROS) at the tumor site has been widely used in the tumor targeted delivery. However, the ROS stimulus-responsive vector itself is also a ROS consumer, and the consumption of endogenous ROS may not be sufficient to maintain sustained drug release. In this study, we designed and synthesized ROS/pH dual-sensitive polymer micelles for the co-delivery of emodin (EMD) and chlorambucil (CLB). The release of quinone methides (QM) can consume glutathione (GSH), on the one hand, it can enhance the chemotoxicity of phenylbutyrate nitrogen mustard, on the other hand, emodin can induce oxidative damage of tumor cells and maintain the sustained targeted release of drugs.
肿瘤部位的高活性氧（ROS）水平已被广泛用于肿瘤靶向递药。然而，ROS 刺激响应性载体本身也是活性氧的消耗者，内源性 ROS 的消耗可能不足以维持药物的持续释放。在本研究中，我们设计并合成了用于同时递送大黄素（EMD）和苯丁酸氮芥（CLB）的 ROS/pH 双重敏感聚合物胶束。醌甲腙（QM）的释放一方面可以消耗谷胱甘肽（GSH），另一方面可以增强苯丁酸氮芥的化学毒性，而大黄素可以诱导肿瘤细胞氧化损伤，维持药物的持续靶向释放。
