Harnessing the power of cell-penetrating peptides: activatable carriers for targeting systemic delivery of cancer therapeutics and imaging agents.

Journal Article (Review;Journal Article)

Targeted delivery of cancer therapeutics and imaging agents aims to enhance the accumulation of these molecules in a solid tumor while avoiding uptake in healthy tissues. Tumor-specific accumulation has been pursued with passive targeting by the enhanced permeability and retention effect, as well as with active targeting strategies. Active targeting is achieved by functionalization of carriers to allow specific interactions between the carrier and the tumor environment. Functionalization of carriers with ligands that specifically interact with overexpressed receptors on cancer cells represents a classic approach to active tumor targeting. Cell-penetrating peptides (CPPs) provide a non-specific and receptor-independent mechanism to enhance cellular uptake that offers an exciting alternative to traditional active targeting approaches. While the non-specificity of CPP-mediated internalization has the intriguing potential to make this approach applicable to a wide range of tumor types, their promiscuity is, however, a significant barrier to their clinical utility for systemically administered applications. Many approaches have been investigated to selectively turn on the function of systemically delivered CPP-functionalized carriers specifically in tumors to achieve targeted delivery of cancer therapeutics and imaging agents.

Full Text

Duke Authors

Cited Authors

  • MacEwan, SR; Chilkoti, A

Published Date

  • January 2013

Published In

Volume / Issue

  • 5 / 1

Start / End Page

  • 31 - 48

PubMed ID

  • 22977001

Pubmed Central ID

  • PMC3573534

Electronic International Standard Serial Number (EISSN)

  • 1939-0041

International Standard Serial Number (ISSN)

  • 1939-5116

Digital Object Identifier (DOI)

  • 10.1002/wnan.1197


  • eng