RGD-decorated solid lipid nanoparticles enhance tumor targeting, penetration and anticancer effect of asiatic acid

Nanomedicine (Lond). 2020 Jul;15(16):1567-1583. doi: 10.2217/nnm-2020-0035. Epub 2020 Jul 3.

Abstract

Aim: Asiatic acid (AA) is a promising anticancer agent, however, its delivery to glioblastoma is a major challenge. This work investigates the beneficial therapeutic efficacy of RGD-conjugated solid lipid nanoparticles (RGD-SLNs) for the selective targeting of AA to gliblastoma. Materials & methods: AA-containing RGD-SLNs were prepared using two different PEG-linker size. Targetability and efficacy were tested using monolayer cells and spheroid tumor models. Results: RGD-SLNs significantly improved cytotoxicity of AA against U87-MG monolayer cells and enhanced cellular uptake compared with non-RGD-containing SLNs. In spheroid models, AA-containing RGD-SLNs showed superior control in tumor growth, improved cytotoxicity and enhanced spheroid penetration when compared with AA alone or non-RGD-containing SLNs. Conclusion: This study illustrates the potential of AA-loaded RGD-SLNs as efficacious target-specific treatment for glioblastoma.

Keywords: Arg-Gly-Asp; Centella asiatica; arginine-glycine-aspartic acid; glioma; nanomedicine and PEG; nanotechnology; targeted delivery.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line, Tumor
  • Lipids
  • Nanoparticles*
  • Oligopeptides
  • Pentacyclic Triterpenes

Substances

  • Lipids
  • Oligopeptides
  • Pentacyclic Triterpenes
  • asiatic acid