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Cited by 299

The DOI matches its Crossref record; 108 of the 108 references it cites were found in a registry or an index.

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

Open access
Aguirre, T.A.S., Teijeiro-Osorio, D., Rosa, M., Coulter, I.S., Alonso, M.J., Brayden, D.J.·2016·Advanced Drug Delivery Reviews

Abstract

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.

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Metadata

Authors
Aguirre, T. A. S., Teijeiro-Osorio, D., Rosa, M., Coulter, I. S., Alonso, M. J., & Brayden, D. J.
Venue
Advanced Drug Delivery Reviews
Publisher
Elsevier BV
Published
2016-11
Volume
106
Issue
Pt B
Pages
223-241
ISSN
0169-409X (ISSN-L)
OpenAlex
W2284082872
Cited by
299
References
108
FWCI
2.27
Type
journal article
Language
en
Open access
green

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CoChat. (2026). Citation check: Current status of selected oral peptide technologies in advanced preclinical development and in clinical trials. https://app.cochat.ai/papers/10.1016/j.addr.2016.02.004
The paper
Aguirre, T. A. S., Teijeiro-Osorio, D., Rosa, M., Coulter, I. S., Alonso, M. J., & Brayden, D. J. (2016). Current status of selected oral peptide technologies in advanced preclinical development and in clinical trials. Advanced Drug Delivery Reviews. https://doi.org/10.1016/j.addr.2016.02.004

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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.