Current status of selected oral peptide technologies in advanced preclinical development and in clinical trials

The development of oral dosage forms that allows absorption of therapeutic peptides to the systemic circulation is one of the greatest challenges for the pharmaceutical industry. Currently, a number of technologies including either mixtures of penetration enhancers or protease inhibitors and/or nano...

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Bibliographic Details
Published in:	Advanced drug delivery reviews Vol. 106; no. Pt B; pp. 223 - 241
Main Authors:	Aguirre, T.A.S., Teijeiro-Osorio, D., Rosa, M., Coulter, I.S., Alonso, M.J., Brayden, D.J.
Format:	Journal Article
Language:	English
Published:	Netherlands Elsevier B.V 15-11-2016
Subjects:	Administration, Oral Animals Biological Availability Clinical Trials as Topic Drug Delivery Systems Excipients - administration & dosage Excipients - pharmacokinetics Humans Intestinal Absorption Intestinal permeation enhancers Oral nanotechnology Oral peptides Peptide clinical trials Peptides - administration & dosage Peptides - pharmacokinetics Therapeutic peptides Peptide clinical trials Oral peptides Therapeutic peptides Intestinal permeation enhancers Oral nanotechnology
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Summary:	The development of oral dosage forms that allows absorption of therapeutic peptides to the systemic circulation is one of the greatest challenges for the pharmaceutical industry. Currently, a number of technologies including either mixtures of penetration enhancers or protease inhibitors and/or nanotechnology-based products are under clinical development. Typically, these formulations are presented in the form of enteric-coated tablets or capsules. Systems undergoing preclinical investigation include further advances in nanotechnology, including intestinal microneedle patches, as well as their combination with regional delivery to the colon. This review critically examines four selected promising oral peptide technologies at preclinical stage and the twelve that have progressed to clinical trials, as indicated in www.clinicaltrials.gov. We examined these technologies under the criteria of peptide selection, formulation design, system components and excipients, intestinal mechanism of action, efficacy in man, and safety issues. The conclusion is that most of the technologies in clinical trials are incremental rather than paradigm-shifting and that even the more clinically advanced oral peptide drugs examples of oral bioavailability appear to yield oral bioavailability values of only 1–2% and are, therefore, only currently suitable for a limited range of peptides. Progress of selected oral peptides in clinical trials and in preclinical research for either systemic or local intestinal delivery * [Display omitted]
Bibliography:	ObjectType-Article-2 SourceType-Scholarly Journals-1 ObjectType-Feature-3 content type line 23 ObjectType-Review-1
ISSN:	0169-409X 1872-8294
DOI:	10.1016/j.addr.2016.02.004