Abstract
Cell-penetrating peptides provide a highly promising strategy for intracellular drug delivery. One relevant clinical application of cell-penetrating peptides is cancer therapeutics. Peptide based delivery could increase the uptake of drugs in tumor cells and thereby increase the efficacy of the treatment, either of conventional small molecular drugs or oligonucleotide based therapeutics. This review is focused on the cancer applications of cell penetrating peptides as delivery systems; different aspects of drug loading, cargoes and delivery are discussed together with methods for targeted delivery, activatable cell-penetrating peptides and transducible agents coupled to cell-penetrating peptides.
Highlights
Cell-penetrating peptides (CPPs) provide a promising solution to the problems commonly related with drug delivery of conventional cancer chemotherapeutics as well as oligonucleotide based treatments
Increases in efficacy have been observed for chimeric peptides based on known CPPs such as transportan, based on a combination of a galanin and a mastoparan sequence [3], truncated versions known peptides such as transportan 10 (TP10) [4] and chemically modified CPPs using a range of different modifications
There are several strategies to selectively target cancer cells with CPPs conjugated with targeting ligands: Cell targeting peptides, activatable cell-penetrating peptides and transducible agents
Summary
Cell-penetrating peptides (CPPs) provide a promising solution to the problems commonly related with drug delivery of conventional cancer chemotherapeutics as well as oligonucleotide based treatments. Synthetic or designed CPPs can range from simple polyarginine structures to more complex peptide sequences designed for helix formation or interaction with cargoes and membranes (see Table 1 for examples of structures) This ability to transport cargoes over the cellular plasma membrane makes CPPs a promising class of drug delivery vehicles and a large number of different drug-CPP constructs have been synthesized, the cargoes that have been delivered range from classical molecular drugs to different types of oligonucleotides and proteins. Peptide complexes have been used for oligonucleotide delivery in a large number of different systems in vitro as well as in vivo, the complexation with peptides has been found to increase the stability and serum half-life of oligonucleotide cargoes [7] Advantages of this method are the relative ease of preparation, that one peptide sequence can be used for a range of different cargoes without chemical modification and that the peptides could potentially shield the cargo from exposure to serum proteins and thereby extend the blood circulation time in vivo [8]. The complex is formed by electrostatic and hydrophobic interactions between the CPP and the cargo
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