Peptide micelle-mediated curcumin delivery for protection of islet β-cells under hypoxia

J Drug Target. 2016 Aug;24(7):618-23. doi: 10.3109/1061186X.2015.1132220. Epub 2016 Jan 15.


Islet transplantation is one of many therapeutic approaches for the treatment of diabetes. During transplant procedures, the isolated islets are subjected to hypoxic conditions, and undergo the apoptotic process. Curcumin has a cytoprotective effect, and may therefore be useful for the protection of islets under hypoxia. However, curcumin is hydrophobic, and an efficient curcumin carrier is required for effective treatment. In this study, R3V6 peptide micelles, composed of a 3-arginine stretch and 6-valine stretch, were evaluated as a curcumin carrier to INS-1 insulinoma cells. Curcumin was loaded into R3V6 micelles at a weight ratio of 10:3 (R3V6:curcumin). The size and surface charge of the curcumin-loaded R3V6 micelles (R3V6-curcumin) were approximately 250 nm and 17.49 mV, respectively. R3V6-curcumin delivered curcumin to the INS-1 cells more efficiently than either curcumin alone or a simple mixture of R3V6 and curcumin. MTT assay indicated that under hypoxia, R3V6-curcumin protected INS-1 cells more efficiently than curcumin alone. TUNEL and reactive oxygen species (ROS) assays suggested that R3V6-curcumin reduced INS-1 cell apoptosis under hypoxia. These results demonstrate that R3V6 peptide micelles are an effective carrier of curcumin, and that R3V6-curcumin may improve the viability of pancreatic β-cells in islet transplantation.

Keywords: Apoptosis; curcumin; hypoxia; pancreatic β-cell; peptide micelle.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Cell Hypoxia / drug effects
  • Cell Line, Tumor
  • Curcumin / administration & dosage*
  • Curcumin / pharmacology*
  • Cytoprotection
  • Drug Carriers / chemistry*
  • In Situ Nick-End Labeling
  • Insulin-Secreting Cells / drug effects*
  • Insulin-Secreting Cells / metabolism
  • Insulin-Secreting Cells / pathology
  • Oligopeptides / chemistry*
  • Particle Size
  • Rats
  • Reactive Oxygen Species / metabolism
  • Surface Properties


  • Drug Carriers
  • Oligopeptides
  • Reactive Oxygen Species
  • Curcumin