Intestinal permeation enhancers for oral peptide delivery.
Intestinal permeation enhancers (PEs) are one of the most widely tested strategies to improve oral delivery of therapeutic peptides. This article assesses the intestinal permeation enhancement action of over 250 PEs that have been tested in intestinal delivery models. In depth analysis of pre-clinical data is presented for PEs as components of proprietary delivery systems that have progressed to clinical trials. Given the importance of co-presentation of sufficiently high concentrations of PE and peptide at the small intestinal epithelium, there is an emphasis on studies where PEs have been formulated with poorly permeable molecules in solid dosage forms and lipoidal dispersions.
RCSI School of Pharmacy, Royal College of Surgeons in Ireland, St Stephen's Green, Dublin 2, Ireland.
Sam
S
Maher
Department of Pharmacy and Pharmacology, University of Bath, UK.
Randall J
RJ
Mrsny
UCD School of Veterinary Medicine and Conway Institute, University College Dublin, Belfield, Dublin 4, Ireland. Electronic address: david.brayden@ucd.ie.
David J
DJ
Brayden
D000284:Administration, Oral; D000818:Animals; D002986:Clinical Trials as Topic; D016503:Drug Delivery Systems / Q000379:methods*; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects*; D007413:Intestinal Mucosa / Q000378:metabolism*; D007422:Intestines / Q000187:drug effects*; D010455:Peptides / Q000008:administration & dosage* / Q000378:metabolism* / Q000493:pharmacokinetics
D010455:Peptides
Emulsions; Intestinal permeation enhancers; Oral peptide delivery; Paracellular transport; Solid dose formulation; Surfactants; Transcellular