Formulation Strategies to Improve Oral Peptide Delivery

Maher, Sam; Ryan, Benedict K.; Duffy, Aoife; Brayden, David J.

doi:10.4155/ppa.14.15

Cited by 62 publications

(41 citation statements)

References 170 publications

(139 reference statements)

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“…and low values (1)(2)(3)(4)(5)(6)(7)(8)(9)(10) [165]. The hydrophobic moiety of the surfactant also influences enhancement action.…”

Section: Hlb In Permeation Enhancementmentioning

confidence: 99%

“…The capacity of C 10 to clinically improve intestinal drug absorption was demonstrated in rectal suppositories of ampicillin, for which it gained approval in Sweden (1992) and Japan (1985 [2]). C 10 is efficacious in both small and large intestine, although it was more effective in the colon for FD4 and insulin in rat intestinal instillation [20,70,118,184,185].…”

Section: Case 1: C 10mentioning

confidence: 99%

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Intestinal permeation enhancers for oral peptide delivery

Maher

Mrsny

Brayden

2016

Advanced Drug Delivery Reviews

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290

201

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Publication informationAdvanced Drug Delivery Reviews, (Part B): 277-319 Publisher ElsevierItem record/more information http://hdl.handle.net/10197/7800Publisher's statement þÿ T h i s i s t h e a u t h o r s v e r s i o n o f a w o r k t h a t w a s a c c e p t e d f o r p u b l i c a t i o n i n A d v a n c e d D r u g Delivery Reviews. Changes resulting from the publishing process, such as peer review,

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“…and low values (1)(2)(3)(4)(5)(6)(7)(8)(9)(10) [165]. The hydrophobic moiety of the surfactant also influences enhancement action.…”

Section: Hlb In Permeation Enhancementmentioning

confidence: 99%

Section: Case 1: C 10mentioning

confidence: 99%

Intestinal permeation enhancers for oral peptide delivery

Maher

Mrsny

Brayden

2016

Advanced Drug Delivery Reviews

Self Cite

290

201

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“…Medium chain fatty acids (MCFA) are powerful permeation enhancers acting in part by re-organising tricellulin and claudin 5 proteins at the tight junction (18), as well as through a mild detergent fluidizing effect on the plasma membrane (19). Several peptides are in oral clinical trials using MCFA-based technologies (20,21). One of the lead MCFA in clinical trials, capric acid, is found in mM concentrations in dairy products, and its sodium salt (C 10 ) has shown extensive enhancement effects in vitro and in vivo (22).…”

Section: Introductionmentioning

confidence: 99%

Stability, toxicity and intestinal permeation enhancement of two food-derived antihypertensive tripeptides, Ile-Pro-Pro and Leu-Lys-Pro

et al. 2015

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Publication information Peptides, 71 : 1-7Publisher Elsevier Item record/more information http://hdl.handle.net/10197/8723 Publisher's statementThis is the author's version of a work that was accepted for publication in Peptides. Changes resulting from the publishing process, such as peer review, editing, corrections, structural formatting, and other quality control mechanisms may not be reflected in this document. Changes may have been made to this work since it was submitted for publication. A definitive version was subsequently published in Peptides (VOL 71, ISSUE 2015, (2015 colonic mucosae were low, but were significantly increased in each tissue type by the medium chain fatty acids (MCFA) permeation enhancers, sodium caprate (C 10 ) and the sodium salt of 10-undecylenic acid (uC 11 ). IPP and LKP were therefore stable against intestinal and liver peptidases and were non-cytotoxic; their P app values across rat intestinal mucosae were low, but could be increased by MCFA. There is potential to make on oral dosage form once in vivo pharmacology is confirmed.

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“…Peptides, including insulin, are unstable and poorly permeate the small intestinal epithelium, hence their low oral bioavailability [38]. PEs are present in several solid-dose oral formulations for peptides, of which two technologies are advanced clinically [39,40].…”

Section: Hca: Cytotoxicity Of Polymers and Permeation Enhancersmentioning

confidence: 99%

High-content analysis for drug delivery and nanoparticle applications

Brayden

Cryan

Dawson

et al. 2015

Drug Discovery Today

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Publication information Drug Discovery Today, 20 (8): 942-957Publisher Elsevier Item record/more information http://hdl.handle.net/10197/6636 Publisher's statementThis is the author's version of a work that was accepted for publication in Drug Discovery Today. Changes resulting from the publishing process, such as peer review, editing, corrections, structural formatting, and other quality control mechanisms may not be reflected in this document. Changes may have been made to this work since it was submitted for publication. A definitive version was subsequently published in Drug Discovery Today, 20 (8), (2015 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. Page 1 of 26A c c e p t e d M a n u s c r i p t Sally-Ann CryanSally-Ann Cryan has a pharmacy degree and a PhD in pharmaceutics ( Jeremy SimpsonJeremy Simpson carried out his PhD at the University of Warwick, followed postdoctoral work at the Scripps Research Institute in San Diego, and the Imperial Cancer Research Fund in London. After 9 years as a staff member at the European Molecular Biology Laboratory (EMBL) in Heidelberg (Germany), he was appointed as professor of cell biology at UCD, in 2008. He currently applies high-throughput imaging technologies to study subcellular transport pathways and the internalization routes taken by nanoparticles in cells. He runs the UCD Cell Screening Laboratory and is the author of more than 80 publications.High-content analysis (HCA) provides quantitative multiparametric cellular fluorescence data. From its origins in discovery toxicology, it is now addressing fundamental questions in drug delivery. Nanoparticles (NPs), polymers, and intestinal permeation enhancers are being harnessed in drug delivery systems to modulate plasma membrane properties and the intracellular environment. Identifying comparative mechanistic cytotoxicity on sublethal events is crucial to expedite the development of such systems. NP uptake and intracellular routing pathways are also being dissected using chemical and genetic perturbations, with the potential to assess the intracellular fate of targeted and untargeted particles in vitro. As we discuss here, HCA is set to make a major impact in preclinical delivery research by elucidating the intracellular pathways of NPs and the in vitro mechanistic-based toxicology of formulation constituents. A brief recap of cytotoxicity assaysIn vitro cell-based assays have long been used to assess the cytotoxic effects of drug exposure [1]. Cells undergoing acute necrosis swell and lose metabolic capacity, thereby losing the capacity to maintain a barrier to the extracellular space and the ability ...

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Formulation Strategies to Improve Oral Peptide Delivery

Cited by 62 publications

References 170 publications

Intestinal permeation enhancers for oral peptide delivery

Intestinal permeation enhancers for oral peptide delivery

Stability, toxicity and intestinal permeation enhancement of two food-derived antihypertensive tripeptides, Ile-Pro-Pro and Leu-Lys-Pro

High-content analysis for drug delivery and nanoparticle applications

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