Palladium based nanoparticles for the treatment of advanced melanoma

Sci Rep. 2019 Mar 1;9(1):3255. doi: 10.1038/s41598-019-40258-6.

Abstract

IGF1R and CD44 are overexpressed in most advanced melanomas so we designed chemotherapeutic nanoparticles to target those receptors. Tris(dibenzylideneacetone)dipalladium (Tris DBA-Pd) is a novel inhibitor of N-myristoyltransferase 1 (NMT-1) and has proven in vivo activity against melanoma. However, poor solubility impairs its effectiveness. To improve its therapeutic efficacy and overcome drug resistance in advanced melanomas, we synthesized Tris DBA-Pd hyaluronic acid nanoparticles (Tris DBA-Pd HANP) and evaluated them against in vivo xenografts of LM36R, an aggressive BRAF mutant human melanoma resistant to BRAF inhibitors. We treated xenografted mice in four arms: empty HANPs, free Tris DBA-Pd, Tris DBA-Pd HANPs, and Tris DBA-Pd HANPs with IGF1R antibody. The Tris DBA-Pd HANP group was the most responsive to treatment and showed the greatest depletion of CD44-positive cells on IHC. Surprisingly, the HANP containing IGF1R antibody was less effective than particles without antibody, possibly due to steric hindrance of IGF1R and CD44 binding. Tris DBA-Pd nanoparticles are an effective therapy for CD44-positive tumors like melanoma, and further development of these nanoparticles should be pursued.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Down-Regulation / genetics
  • Gene Expression Regulation, Neoplastic
  • Humans
  • Hyaluronan Receptors / metabolism
  • Hyaluronic Acid / chemistry
  • Male
  • Melanoma / pathology*
  • Melanoma / therapy*
  • Metal Nanoparticles / therapeutic use*
  • Mice, Nude
  • Neoplasm Staging
  • Organometallic Compounds / chemistry
  • Palladium / therapeutic use*
  • Particle Size
  • Transcriptome / genetics
  • Up-Regulation / genetics
  • Xenograft Model Antitumor Assays

Substances

  • Hyaluronan Receptors
  • Organometallic Compounds
  • tris(dibenzylideneacetone)dipalladium
  • Palladium
  • Hyaluronic Acid