Oral delivery of oleuropein-loaded lipid nanocarriers alleviates inflammation and oxidative stress in acute colitis

Int J Pharm. 2020 Aug 30:586:119515. doi: 10.1016/j.ijpharm.2020.119515. Epub 2020 Jun 13.

Abstract

Inflammation and oxidative stress pathways have emerged as novel targets in the management of inflammatory bowel diseases (IBD). Targeting the drug to the inflamed colon remains a challenge. Nanostructured lipid carriers (NLCs) have been reported to accumulate in inflamed colonic mucosa. The antioxidant/antiinflamatory polyphenol oleuropein (OLE) was loaded in NLCs (NLC-OLE). NLC-OLE showed to be more effective in decreasing the TNF-α secretion and intracellular reactive oxygen species (ROS) by activated macrophages (J774) compared to the conventional form of OLE. OLE efficacy was preserved within NLC-OLE ameliorating inflammation in a murine model of acute colitis: reduced levels of TNF-α and IL-6, decreased neutrophil infiltration and improved histopathology of the colon were reported. In addition, NLC-OLE enhanced the ROS scavenging activity of OLE in the colon after oral administration. These data suggest that the proposed NLC-OLE could be a promising drug delivery system for OLE in IBD treatment.

Keywords: Inflammatory bowel disease; Nanostructured lipid carrier; Oleuropein; Olive oil; Oxidative stress; Polyphenols.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Oral
  • Animals
  • Anti-Inflammatory Agents / administration & dosage
  • Anti-Inflammatory Agents / pharmacology
  • Antioxidants / administration & dosage
  • Antioxidants / pharmacology
  • Cell Line
  • Colitis / drug therapy*
  • Colitis / pathology
  • Disease Models, Animal
  • Drug Carriers / chemistry
  • Drug Delivery Systems*
  • Inflammation / drug therapy*
  • Inflammation / pathology
  • Iridoid Glucosides
  • Iridoids / administration & dosage*
  • Iridoids / pharmacology
  • Lipids / chemistry
  • Macrophages / drug effects
  • Macrophages / pathology
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Nanostructures
  • Oxidative Stress / drug effects
  • Reactive Oxygen Species / metabolism

Substances

  • Anti-Inflammatory Agents
  • Antioxidants
  • Drug Carriers
  • Iridoid Glucosides
  • Iridoids
  • Lipids
  • Reactive Oxygen Species
  • oleuropein