Application of Permeation Enhancers in Oral Delivery of Macromolecules: An Update

The application of permeation enhancers (PEs) to improve transport of poorly absorbed active pharmaceutical ingredients across the intestinal epithelium is a widely tested approach. Several hundred compounds have been shown to alter the epithelial barrier, and although the research emphasis has broa...

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Published inPharmaceutics Vol. 11; no. 1; p. 41
Main Authors Maher, Sam, Brayden, David J, Casettari, Luca, Illum, Lisbeth
Format Journal Article
LanguageEnglish
Published Switzerland MDPI AG 19.01.2019
MDPI
Subjects
Amino acids
Clinical trials
Drug dosages
epithelium
formulation
hydrophobization
Insulin
oral delivery
Peptides
Permeability
permeation enhancer
Pharmaceutical industry
Review
safety
simulated intestinal fluid
Sodium
Surfactants
United States > US
Israel
safety
oral delivery
permeability
formulation
epithelium
simulated intestinal fluid
hydrophobization
permeation enhancer
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Summary:The application of permeation enhancers (PEs) to improve transport of poorly absorbed active pharmaceutical ingredients across the intestinal epithelium is a widely tested approach. Several hundred compounds have been shown to alter the epithelial barrier, and although the research emphasis has broadened to encompass a role for nanoparticle approaches, PEs represent a key constituent of conventional oral formulations that have progressed to clinical testing. In this review, we highlight promising PEs in early development, summarize the current state of the art, and highlight challenges to the translation of PE-based delivery systems into safe and effective oral dosage forms for patients.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-3
content type line 23
ObjectType-Review-1
ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics11010041