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Pharmaceutics 2019, 11(1), 41; https://doi.org/10.3390/pharmaceutics11010041

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

1
School of Pharmacy, Royal College of Surgeons in Ireland, St. Stephens Green, Dublin 2, Ireland
2
School of Veterinary Medicine and UCD Conway Institute, University College Dublin, Belfield, Dublin 4, Ireland
3
Department of Biomolecular Sciences, University of Urbino Carlo Bo, Piazza del Rinascimento 6, 61029 Urbino (PU), Italy
4
IDentity, 19 Cavendish Crescent North, The Park, Nottingham NG7 1BA, UK
*
Author to whom correspondence should be addressed.
Received: 21 December 2018 / Revised: 11 January 2019 / Accepted: 14 January 2019 / Published: 19 January 2019
(This article belongs to the Special Issue Transmucosal Absorption Enhancers in the Drug Delivery Field)
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Abstract

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. View Full-Text
Keywords: permeation enhancer; oral delivery; formulation; permeability; safety; simulated intestinal fluid; hydrophobization; epithelium permeation enhancer; oral delivery; formulation; permeability; safety; simulated intestinal fluid; hydrophobization; epithelium
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Maher, S.; Brayden, D.J.; Casettari, L.; Illum, L. Application of Permeation Enhancers in Oral Delivery of Macromolecules: An Update. Pharmaceutics 2019, 11, 41.

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