Cell-penetrating peptides as tools to enhance non-injectable delivery of biopharmaceuticals. Issue 2 (2nd April 2016)

• Record Type: Journal Article
• Authors: Kristensen, Mie; Nielsen, Hanne Mørck
• Is Part Of: Tissue barriers. Volume 4:Issue 2(2016)
• Publication Date: 2016-04-02
• Subjects: cell-penetrating peptides -- delivery vectors -- drug delivery -- epithelium -- mucosal barriers -- non-injectable delivery -- peptide and protein drugs; Biological transport -- Periodicals; Tissues -- Periodicals; Biological Transport -- Periodicals; Tissues -- Periodicals; 571
• DOI: 10.1080/21688370.2016.1178369
• Languages: English
• ISSNs: 2168-8370

Abstract

ABSTRACT: Non-injectable delivery of peptide and protein drugs is hampered by their labile nature, hydrophilicity, and large molecular size; thus limiting their permeation across mucosae, which represent major biochemical and physical barriers to drugs administered via e.g. the oral, nasal, and pulmonary routes. However, in recent years cell-penetrating peptides (CPP) have emerged as promising tools to enhance mucosal delivery of co-administered or conjugated peptide and protein cargo and more advanced CPP-cargo formulations are emerging. CPPs act as transepithelial delivery vectors, but the mechanism(s) by which CPPs mediate cargo translocation across an epithelium is so far poorly understood; both due to the fact that multiple factors influence the resulting uptake and trafficking mechanisms as well as to the complicated nature of sensitive studies of this. In addition to a proper mechanistic understanding, documentation of CPP-mediated delivery in higher animal species than rodent as well as extensive toxicological studies are necessary for CPP-containing non-injectable DDSs to reach the clinic.