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Approaches for enhancing oral bioavailability of peptides and proteins
Open accessAbstract
Oral delivery of peptide and protein drugs faces immense challenge partially due to the gastrointestinal (GI) environment. In spite of considerable efforts by industrial and academic laboratories, no major breakthrough in the effective oral delivery of polypeptides and proteins has been accomplished. Upon oral administration, gastrointestinal epithelium acts as a physical and biochemical barrier for absorption of proteins resulting in low bioavailability (typically less than 1-2%). An ideal oral drug delivery system should be capable of (a) maintaining the integrity of protein molecules until it reaches the site of absorption, (b) releasing the drug at the target absorption site, where the delivery system appends to that site by virtue of specific interaction, and (c) retaining inside the gastrointestinal tract irrespective of its transitory constraints. Various technologies have been explored to overcome the problems associated with the oral delivery of macromolecules such as insulin, gonadotropin-releasing hormones, calcitonin, human growth factor, vaccines, enkephalins, and interferons, all of which met with limited success. This review article intends to summarize the physiological barriers to oral delivery of peptides and proteins and novel pharmaceutical approaches to circumvent these barriers and enhance oral bioavailability of these macromolecules.
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“mAbs have limited oral bioavailability (typically <1–2%)15 and are therefore not usually administered orally.”
From Tutorial on monoclonal antibody pharmacokinetics and its considerations in early development (2018) · cites this paper as [15]
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Metadata
- Authors
- Renukuntla, J., Vadlapudi, A. D., Patel, A., Boddu, S. H. S., & Mitra, A. K.
- Affiliations
- South College (US)
- University of Missouri–Kansas City (US)
- University of Toledo (US)
- Corresponding author
- Mitra, Ashim K.
- Venue
- International Journal of Pharmaceutics
- Publisher
- Elsevier BV
- Published
- 2013-04
- Volume
- 447
- Issue
- 1-2
- Pages
- 75-93
- ISSN
- 0378-5173 (ISSN-L)
- PMC
- PMC3680128
- OpenAlex
- W2008173042
- Cited by
- 681
- References
- 219
- Citations by year
- 2026: 37 · 2025: 55 · 2024: 47 · 2023: 55 · 2022: 67 · 2021: 40 · 2020: 67 · 2019: 55 · 2018: 61 · 2017: 63 · 2016: 49 · 2015: 37 · 2014: 34 · 2013: 11
- FWCI
- 5.50
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- International Journal of Pharmaceutics (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- NIH (R01 GM064320-03, R01EY09171, R01EY010659, R01 AI071199-01A2)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Life Sciences › Agricultural and Biological Sciences › Food Science › Proteins in Food Systems
- Keywords
- oral bioavailability, gastrointestinal barrier, protein stability, drug absorption, peptide delivery, insulin, gonadotropin-releasing hormone, vaccines, interferon, enkephalin, growth factors
- MeSH terms
- Administration, Oral, Animals, Biological Availability, Chemistry, Pharmaceutical, Humans, Intestinal Absorption, Peptides, Proteins
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