Peptide-enhanced oral delivery of therapeutic peptides and proteins
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Peptide-enhanced oral delivery of therapeutic peptides and proteins. / Kristensen, Mie; Foged, Camilla; Berthelsen, Jens; Nielsen, Hanne Mørck.
In: Journal of Drug Delivery Science and Technology, Vol. 23, No. 4, 2013, p. 365-373.Research output: Contribution to journal › Review › Research › peer-review
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TY - JOUR
T1 - Peptide-enhanced oral delivery of therapeutic peptides and proteins
AU - Kristensen, Mie
AU - Foged, Camilla
AU - Berthelsen, Jens
AU - Nielsen, Hanne Mørck
PY - 2013
Y1 - 2013
N2 - Systemic therapy upon oral delivery of biologics, such as peptide and protein drugs is limited due to their large molecular size, their low enzymatic stability and their inability to cross the intestinal epithelium. Ways to overcome the epithelial barrier include the use of peptide-based excipients such as the cell penetrating peptides (CPPs) and the tight junction modulating peptides (TJMPs), which are able to translocate across the cellular membranes in a non-disruptive way or reversibly modulate the integrity of intercellular tight junctions (TJs), respectively. However, because of the harsh environment throughout the gastrointestinal (GI) tract, chemical stability is an inherent challenge when employing amino acid-based excipients for oral delivery, and multiple approaches have been investigated to improve this. The exact mechanisms of transepithelial translocation are discussed, and it is believed that CPP-mediated translocation involves transcytosis and/or direct translocation through the epithelial cells; whereas TJMP-mediated translocation is dependent on interaction with transmembrane or peripheral TJ proteins. This review focuses on the CPPs and the TJMPs currently employed as excipients for oral delivery of peptide and protein drugs highlighting recent studies and the most promising compounds from these classes of peptide excipients.
AB - Systemic therapy upon oral delivery of biologics, such as peptide and protein drugs is limited due to their large molecular size, their low enzymatic stability and their inability to cross the intestinal epithelium. Ways to overcome the epithelial barrier include the use of peptide-based excipients such as the cell penetrating peptides (CPPs) and the tight junction modulating peptides (TJMPs), which are able to translocate across the cellular membranes in a non-disruptive way or reversibly modulate the integrity of intercellular tight junctions (TJs), respectively. However, because of the harsh environment throughout the gastrointestinal (GI) tract, chemical stability is an inherent challenge when employing amino acid-based excipients for oral delivery, and multiple approaches have been investigated to improve this. The exact mechanisms of transepithelial translocation are discussed, and it is believed that CPP-mediated translocation involves transcytosis and/or direct translocation through the epithelial cells; whereas TJMP-mediated translocation is dependent on interaction with transmembrane or peripheral TJ proteins. This review focuses on the CPPs and the TJMPs currently employed as excipients for oral delivery of peptide and protein drugs highlighting recent studies and the most promising compounds from these classes of peptide excipients.
M3 - Review
VL - 23
SP - 365
EP - 373
JO - Journal of Drug Delivery Science and Technology
JF - Journal of Drug Delivery Science and Technology
SN - 1773-2247
IS - 4
ER -
ID: 79188507