ROS-responsive copolymer micelles for inflammation triggered delivery of ibuprofen

Colloids Surf B Biointerfaces. 2022 Sep:217:112590. doi: 10.1016/j.colsurfb.2022.112590. Epub 2022 May 23.

Abstract

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.

Keywords: Anti-inflammatory; Ibuprofen; Inflammation triggered drug delivery; Polymeric micelles; ROS-responsive.

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Humans
  • Ibuprofen* / pharmacology
  • Inflammation / chemically induced
  • Inflammation / drug therapy
  • Micelles*
  • Polymers
  • Reactive Oxygen Species

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Micelles
  • Polymers
  • Reactive Oxygen Species
  • Ibuprofen