Evaluation of Nanotargeted 111In-Cyclic RGDfK-Liposome in a Human Melanoma Xenotransplantation Model

Int J Mol Sci. 2021 Jan 22;22(3):1099. doi: 10.3390/ijms22031099.

Abstract

Nanotargeted liposomes may be modified with targeting peptide on the surface of a prepared liposome to endow specificity and elevate targeting efficiency. The aim of this study was to develop a radioactive targeted nanoparticle, the 111In-cyclic RGDfK-liposome, and its advantage of recognizing the αVβ3 integrin was examined. The cyclic RGDfK modified liposomes were demonstrated the ability to bind the αVβ3 integrin expressed on the surface of human melanoma cell in vitro and in vivo. The effects of the cyclic RGDfK-liposome on the functioning of phagocytes was also examined, showing no considerable negative effects on the engulfment of bacteria and the generation of reactive oxygen species. Based upon these findings, the cyclic RGDfK- liposome is said to be a promising agent for tumor imaging.

Keywords: 111In-cyclic RGDfK-liposome; Nanotargeted liposome; αVβ3 integrin.

MeSH terms

  • Animals
  • Cell Adhesion
  • Cell Line, Tumor
  • Female
  • Humans
  • Indium Radioisotopes / chemistry*
  • Integrin alphaVbeta3 / metabolism*
  • Liposomes / chemistry*
  • Melanoma / metabolism*
  • Mice
  • Mice, Inbred BALB C
  • Neoplasm Transplantation
  • Peptides / chemistry
  • Peptides, Cyclic / chemistry*
  • Phagocytes
  • RAW 264.7 Cells
  • Reactive Oxygen Species / metabolism
  • Tomography, Emission-Computed, Single-Photon
  • X-Ray Microtomography

Substances

  • Indium Radioisotopes
  • Integrin alphaVbeta3
  • Liposomes
  • Peptides
  • Peptides, Cyclic
  • Reactive Oxygen Species
  • cyclic (arginyl-glycyl-aspartyl-phenylalanyl-lysyl)
  • Indium-111