UniSA STEM, University of South Australia, Mawson Lakes, South Australia 5095, Australia.
UniSA STEM, University of South Australia, Mawson Lakes, South Australia 5095, Australia.
Colloids Surf B Biointerfaces. 2022 Sep;217:112590. doi: 10.1016/j.colsurfb.2022.112590. Epub 2022 May 23.
Non-steroidal anti-inflammatory drugs (NSAIDs) are commonly used for the treatment of pain, inflammation and fever. However, most NSAIDs are poorly water soluble, making it difficult to be administered thus high doses are required to reach the intended therapeutic effect, resulting in associated side effects. In this study, ROS-responsive micellar systems based on a block copolymer consisting of methylpropyl thioether (MTPA) and N'N-dimethylacrylamide was developed and loaded with ibuprofen (IBU). Using lipopolysaccharide activated RAW 264.7 macrophage like cells, we demonstrated that IBU was released from the copolymer, specifically in the presence of ROS. Interestingly, IBU encapsulated in ROS-responsive nanoparticles exhibited greater anti-inflammatory potency compared to its free form. The work highlights the potential of the ROS-responsive micellar system developed in this work to be used as carrier of NSAIDs for the treatment of relevant inflammatory conditions.
非甾体抗炎药(NSAIDs)常用于治疗疼痛、炎症和发热。然而,大多数 NSAIDs 的水溶性较差,难以给药,因此需要高剂量才能达到预期的治疗效果,从而导致相关的副作用。在这项研究中,开发了基于嵌段共聚物的 ROS 响应胶束系统,该共聚物由甲基丙基硫醚(MTPA)和 N'N-二甲基丙烯酰胺组成,并负载布洛芬(IBU)。使用脂多糖激活的 RAW 264.7 巨噬细胞样细胞,我们证明了 IBU 从共聚物中释放出来,特别是在 ROS 的存在下。有趣的是,与游离形式相比,包封在 ROS 响应性纳米颗粒中的 IBU 表现出更强的抗炎效力。这项工作强调了本工作中开发的 ROS 响应胶束系统作为 NSAIDs 载体用于治疗相关炎症疾病的潜力。