cRGD functionalised nanocarriers for targeted delivery of bioactives

J Drug Target. 2019 Feb;27(2):111-124. doi: 10.1080/1061186X.2018.1473409. Epub 2018 May 23.

Abstract

The integrins αvβ3 play a very imperative role in angiogenesis and are overexpressed in endothelial cells of the tumour. Recent years have witnessed huge exploration in the field of αvβ3 integrin-mediated bioactive targeting for treatment of cancer. In these studies, the cRGD peptide has been employed extensively owing to their binding capacity to the αvβ3 integrin. Principally, RGD-based approaches comprise of antagonist molecules of the RGD sequence, drug-RGD conjugates, and most importantly tethering of the nanocarrier surface with the RGD peptide as targeting ligand. Targeting tumour vasculature or cells via cRGD conjugated nanocarriers have emerged as a promising technique for delivering chemotherapeutic drugs and imaging agents for cancer theranostics. In this review, primary emphasis has been given on the application of cRGD-anchored nanocarriers for targeted delivery of drugs, imaging agents, etc. for tumour therapy.

Keywords: integrin receptors; cRGD; cancer; nanocarriers; targeting.

Publication types

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

MeSH terms

  • Drug Delivery Systems*
  • Endothelial Cells / drug effects
  • Humans
  • Integrins / administration & dosage*
  • Nanostructures / chemistry*
  • Peptides, Cyclic / chemistry*
  • Peptides, Cyclic / metabolism*

Substances

  • Integrins
  • Peptides, Cyclic
  • cyclic arginine-glycine-aspartic acid peptide