Cited by 681Advanced Drug Delivery SystemsDrug Solubulity and Delivery SystemsProteins in Food Systems

Approaches for enhancing oral bioavailability of peptides and proteins

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Renukuntla, Jwala, Vadlapudi, Aswani Dutt, Patel, Ashaben, Boddu, Sai H.S., Mitra, Ashim K.·2013·International Journal of Pharmaceutics

Abstract

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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Crossref · 10.1016/j.ijpharm.2013.02.030

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  1. Gangurde HH CMA Tamizharasi S Sivakumar T Upasani CD Approaches for Peptides and Proteins by Colon Specific Delivery: Review International Journal of Pharmaceutical Frontier Research 2011 Apr-Jun 1 110 125
  2. Vinay Kumar KV Sivakumar T T Tm Colon targeting drug delivery system: A review on recent approaches Int J Pharm Biomed Sci 2011 2 11 19

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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)
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
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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