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Dehydration affects drug transport over nasal mucosa

Ali, Abdullah; Wahlgren, Marie LU ; Rembratt-Svensson, Birgitta; Daftani, Ameena; Falkman, Peter; Wollmer, Per LU and Engblom, Johan (2019) In Drug delivery 26(1). p.831-840
Abstract

Formulations for nasal drug delivery often rely on water sorption to adhere to the mucosa, which also causes a higher water gradient over the tissue and subsequent dehydration. The primary aim of this study was therefore to evaluate mucosal response to dehydration and resolve the hypothesis that mucoadhesion achieved through water sorption could also be a constraint for drug absorption via the nasal route. The effect of altering water activity of the vehicle on Xylometazoline HCl and 51Cr-EDTA uptake was studied separately ex vivo using flow through diffusion cells and excised porcine mucosa. We have shown that a modest increase in the water gradient over mucosa induces a substantial decrease in drug uptake for both... (More)

Formulations for nasal drug delivery often rely on water sorption to adhere to the mucosa, which also causes a higher water gradient over the tissue and subsequent dehydration. The primary aim of this study was therefore to evaluate mucosal response to dehydration and resolve the hypothesis that mucoadhesion achieved through water sorption could also be a constraint for drug absorption via the nasal route. The effect of altering water activity of the vehicle on Xylometazoline HCl and 51Cr-EDTA uptake was studied separately ex vivo using flow through diffusion cells and excised porcine mucosa. We have shown that a modest increase in the water gradient over mucosa induces a substantial decrease in drug uptake for both Xylometazoline HCl and 51Cr-EDTA. A similar result was obtained when comparing two different vehicles on the market; Nasoferm® (Nordic Drugs, Sweden) and BLOX4® (Bioglan, Sweden). Mucoadhesion based on water sorption can slow down drug uptake in the nasal cavity. However, a clinical study is required to determine whether prolonged duration of the vehicle in situ or preventing dehydration of the mucosa is the most important factor for improving bioavailability.

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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
dehydration, drug transport, Mucoadhesion, nasal drug delivery, water activity
in
Drug delivery
volume
26
issue
1
pages
10 pages
publisher
Informa Healthcare
external identifiers
  • scopus:85071047269
ISSN
1071-7544
DOI
10.1080/10717544.2019.1650848
language
English
LU publication?
yes
id
045702d8-7f8b-43ff-8695-6ef07a70e925
date added to LUP
2019-09-05 16:24:09
date last changed
2019-09-26 04:41:38
@article{045702d8-7f8b-43ff-8695-6ef07a70e925,
  abstract     = {<p>Formulations for nasal drug delivery often rely on water sorption to adhere to the mucosa, which also causes a higher water gradient over the tissue and subsequent dehydration. The primary aim of this study was therefore to evaluate mucosal response to dehydration and resolve the hypothesis that mucoadhesion achieved through water sorption could also be a constraint for drug absorption via the nasal route. The effect of altering water activity of the vehicle on Xylometazoline HCl and <sup>51</sup>Cr-EDTA uptake was studied separately ex vivo using flow through diffusion cells and excised porcine mucosa. We have shown that a modest increase in the water gradient over mucosa induces a substantial decrease in drug uptake for both Xylometazoline HCl and <sup>51</sup>Cr-EDTA. A similar result was obtained when comparing two different vehicles on the market; Nasoferm<sup>®</sup> (Nordic Drugs, Sweden) and BLOX4<sup>®</sup> (Bioglan, Sweden). Mucoadhesion based on water sorption can slow down drug uptake in the nasal cavity. However, a clinical study is required to determine whether prolonged duration of the vehicle in situ or preventing dehydration of the mucosa is the most important factor for improving bioavailability.</p>},
  author       = {Ali, Abdullah and Wahlgren, Marie and Rembratt-Svensson, Birgitta and Daftani, Ameena and Falkman, Peter and Wollmer, Per and Engblom, Johan},
  issn         = {1071-7544},
  keyword      = {dehydration,drug transport,Mucoadhesion,nasal drug delivery,water activity},
  language     = {eng},
  month        = {01},
  number       = {1},
  pages        = {831--840},
  publisher    = {Informa Healthcare},
  series       = {Drug delivery},
  title        = {Dehydration affects drug transport over nasal mucosa},
  url          = {http://dx.doi.org/10.1080/10717544.2019.1650848},
  volume       = {26},
  year         = {2019},
}