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The delivery of biologically active (therapeutic) peptides and proteins into cells

M Grdisa1

  • 1Division of Molecular Medicine, Rudjer Boskovic Institute, Bijenicka 54, 10 000 Zagreb, Croatia. grdisa@irb.hr

Current Medicinal Chemistry
|March 4, 2011
PubMed

Insights

Cell-penetrating peptides enhance the delivery of therapeutic peptides and proteins. This review focuses on arginine-rich and amphipathic carriers for improved drug bioavailability and targeted therapy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Drug Delivery

Background:

  • Biologically active peptides and proteins show promise for targeted drug therapies, particularly in cancer treatment.
  • In vivo application is hindered by poor stability and cell permeability, necessitating advanced delivery systems.
  • Cell-penetrating peptides (CPPs) are emerging as effective vectors to overcome these delivery challenges.

Purpose of the Study:

  • To review the potential of cell-penetrating peptides as drug delivery systems.
  • To focus specifically on arginine-rich and amphipathic CPPs for therapeutic applications.
  • To highlight strategies for enhancing the bioavailability and efficacy of peptide/protein-based drugs.

Main Methods:

  • Literature review focusing on cell-penetrating peptides, particularly arginine-rich and amphipathic types.
  • Analysis of CPP mechanisms for enhancing cargo uptake.
  • Evaluation of CPPs' role in improving therapeutic protein and peptide bioavailability.

Main Results:

  • Cell-penetrating peptides significantly improve the cellular uptake of fused or attached peptide/protein cargos.
  • Arginine-rich and amphipathic CPPs demonstrate notable potential as efficient transporters.
  • These CPPs can enhance the in vivo stability and permeability of therapeutic molecules.

Conclusions:

  • Cell-penetrating peptides, especially arginine-rich and amphipathic variants, offer a promising strategy for overcoming delivery barriers of peptide/protein therapeutics.
  • Development of CPP-based delivery systems is crucial for advancing targeted therapies and increasing drug bioavailability.
  • Further research into CPPs can unlock their full potential in treating diseases like cancer.

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