The DOI matches its Crossref record; 217 of the 219 references it cites were found in a registry or an index.
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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1 retracted
RETRACTED: In situ-forming hydrogels for sustained ophthalmic drug delivery
Nanjawade, B. K., Manvi, F. V., & Manjappa, A. S. (2007) · Journal of Controlled Release · doi:10.1016/j.jconrel.2007.07.009 · Cited by 213
RetractedPhysiology of the Gastrointestinal Tract
Johnson, L. R. (2006) · Elsevier eBooks · doi:10.1016/b978-0-12-088394-3.x5000-4 · Cited by 4,616
Hydrogels in pharmaceutical formulations
Peppas, N. (2000) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/s0939-6411(00)00090-4 · Cited by 4,011
Biodegradable nanoparticles for drug and gene delivery to cells and tissue
Panyam, J., & Labhasetwar, V. D. (2003) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(02)00228-4 · Cited by 3,417
Nanoparticle-based targeted drug delivery
Singh, R., & Lillard, J. W. (2009) · Experimental and Molecular Pathology · doi:10.1016/j.yexmp.2008.12.004 · Cited by 2,845
In Vivo Protein Transduction: Delivery of a Biologically Active Protein into the Mouse
Schwarze, S. R., Ho, A. L., Vocero-Akbani, A. M., & Dowdy, S. F. (1999) · Science · doi:10.1126/science.285.5433.1569 · Cited by 2,418
Pharmaceutical Applications of Cyclodextrins. 1. Drug Solubilization and Stabilization
Loftsson, Þ., & Brewster, M. E. (1996) · Journal of Pharmaceutical Sciences · doi:10.1021/js950534b · Cited by 2,179
Cyclodextrins as pharmaceutical solubilizers
Brewster, M. E., & Loftsson, Þ. (2007) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2007.05.012 · Cited by 1,942
Williams, A. C., & Barry, B. W. (2003) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2003.10.025 · Cited by 1,746
Prodrugs: design and clinical applications
Rautio, J., Kumpulainen, H., Heimbach, T., Oliyai, R., Oh, D.-M., Järvinen, T., & Savolainen, J. (2008) · Nature Reviews Drug Discovery · doi:10.1038/nrd2468 · Cited by 1,681
Research works printed but not linked: 3
- Gangurde, 2011, Approaches for peptides and proteins by colon specific delivery: Review, Int. J. Pharm. Frontier Res., 1, 110
- Vinay Kumar, 2011, Colon targeting drug delivery system: A review on recent approaches, Int. J. Pharm. Biomed. Sci., 2, 11
- Yang, H.P.A. (CA), Nguyen, Vu Anh (San Jose, CA), Dong, Liang C. (Mountain View, CA), Wong, Patrick S. L. (Palo Alto, CA), 1999. Peptide Formulation, in: States, U. (Ed.). Alza Corporation (Palo Alto, CA).
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Basics and Recent Advances in Peptide and Protein Drug Delivery
Bruno, B. J., Miller, G. D., & Lim, C. S. (2013) · Therapeutic Delivery · doi:10.4155/tde.13.104 · Cited by 771
Elmowafy, E. M., Tiboni, M., & Soliman, M. E. (2019) · Journal of Pharmaceutical Investigation · doi:10.1007/s40005-019-00439-x · Cited by 642
Physicochemical properties of mucus and their impact on transmucosal drug delivery
Leal, J., Smyth, H. D. C., & Ghosh, D. (2017) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2017.09.018 · Cited by 560
Thin films as an emerging platform for drug delivery
Karki, S., Kim, H., Na, S.-J., Shin, D., Jo, K., & Lee, J. (2016) · Asian Journal of Pharmaceutical Sciences · doi:10.1016/j.ajps.2016.05.004 · Cited by 544
Nanoparticles for oral delivery: Design, evaluation and state-of-the-art
Date, A. A., Hanes, J. S., & Ensign, L. M. (2016) · Journal of Controlled Release · doi:10.1016/j.jconrel.2016.06.016 · Cited by 551
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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