期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 447, 期 1-2, 页码 75-93出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2013.02.030
关键词
Oral delivery; Proteins; Peptides; Nanoparticles; Microparticles; GI tract
资金
- NIH [R01 GM064320-03, R01EY09171, R01EY010659, R01 AI071199-01A2]
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. (C) 2013 Elsevier B. V. All rights reserved.
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