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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Main Authors: Sam Maher, David J. Brayden, Luca Casettari, Lisbeth Illum
Format: Article
Language:English
Published: MDPI AG 2019-01-01
Series:Pharmaceutics
Subjects:
Online Access:http://www.mdpi.com/1999-4923/11/1/41
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author Sam Maher
David J. Brayden
Luca Casettari
Lisbeth Illum
author_facet Sam Maher
David J. Brayden
Luca Casettari
Lisbeth Illum
author_sort Sam Maher
collection DOAJ
description 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.
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spelling doaj.art-8c314de793fd4baa9eff52430ae2e3e02022-12-22T04:01:42ZengMDPI AGPharmaceutics1999-49232019-01-011114110.3390/pharmaceutics11010041pharmaceutics11010041Application of Permeation Enhancers in Oral Delivery of Macromolecules: An UpdateSam Maher0David J. Brayden1Luca Casettari2Lisbeth Illum3School of Pharmacy, Royal College of Surgeons in Ireland, St. Stephens Green, Dublin 2, IrelandSchool of Veterinary Medicine and UCD Conway Institute, University College Dublin, Belfield, Dublin 4, IrelandDepartment of Biomolecular Sciences, University of Urbino Carlo Bo, Piazza del Rinascimento 6, 61029 Urbino (PU), ItalyIDentity, 19 Cavendish Crescent North, The Park, Nottingham NG7 1BA, UKThe 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.http://www.mdpi.com/1999-4923/11/1/41permeation enhanceroral deliveryformulationpermeabilitysafetysimulated intestinal fluidhydrophobizationepithelium
spellingShingle Sam Maher
David J. Brayden
Luca Casettari
Lisbeth Illum
Application of Permeation Enhancers in Oral Delivery of Macromolecules: An Update
Pharmaceutics
permeation enhancer
oral delivery
formulation
permeability
safety
simulated intestinal fluid
hydrophobization
epithelium
title Application of Permeation Enhancers in Oral Delivery of Macromolecules: An Update
title_full Application of Permeation Enhancers in Oral Delivery of Macromolecules: An Update
title_fullStr Application of Permeation Enhancers in Oral Delivery of Macromolecules: An Update
title_full_unstemmed Application of Permeation Enhancers in Oral Delivery of Macromolecules: An Update
title_short Application of Permeation Enhancers in Oral Delivery of Macromolecules: An Update
title_sort application of permeation enhancers in oral delivery of macromolecules an update
topic permeation enhancer
oral delivery
formulation
permeability
safety
simulated intestinal fluid
hydrophobization
epithelium
url http://www.mdpi.com/1999-4923/11/1/41
work_keys_str_mv AT sammaher applicationofpermeationenhancersinoraldeliveryofmacromoleculesanupdate
AT davidjbrayden applicationofpermeationenhancersinoraldeliveryofmacromoleculesanupdate
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AT lisbethillum applicationofpermeationenhancersinoraldeliveryofmacromoleculesanupdate