Advanced

Will a water gradient in oral mucosa affect transbuccal drug absorption?

Ali, Abdullah ; Wahlgren, Marie LU ; Pedersen, Lina and Engblom, Johan (2018) In Journal of Drug Delivery Science and Technology 48. p.338-345
Abstract

Formulations for buccal drug delivery often comprise polymers to facilitate mucoadhesion based on water sorption. The main objective of the current study was therefore to evaluate the effect of dehydration on drug uptake through oral mucosa. We have used diffusion cells with excised porcine mucosa to study uptake of three alternative drugs (i.e., Metronidazole, Benzydamine and Xylometazoline) together with polyethylene glycol (PEG) as the model polymer for adjusting water activity in the test solutions. Taking drug activity into account, we can conclude that addition of PEG results in a drug flux through mucosa that is about two times lower for Metronidazole and more than 40 times lower for Xylometazoline compared to that from a pure... (More)

Formulations for buccal drug delivery often comprise polymers to facilitate mucoadhesion based on water sorption. The main objective of the current study was therefore to evaluate the effect of dehydration on drug uptake through oral mucosa. We have used diffusion cells with excised porcine mucosa to study uptake of three alternative drugs (i.e., Metronidazole, Benzydamine and Xylometazoline) together with polyethylene glycol (PEG) as the model polymer for adjusting water activity in the test solutions. Taking drug activity into account, we can conclude that addition of PEG results in a drug flux through mucosa that is about two times lower for Metronidazole and more than 40 times lower for Xylometazoline compared to that from a pure PBS-solution. However, for Benzydamine the uptake through mucosa was more or less the same, which could possibly be due to the high PEG-concentration (65 wt%) affecting the dissociation constant and thus the permeability. These results indicate that an increased water gradient may have the same limiting effect on permeability through oral mucosa as previously seen for skin. Thus, water gradient effects should be a factor to consider when developing buccal adhesive formulations.

(Less)
Please use this url to cite or link to this publication:
author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
Buccal drug delivery, Drug transport, Formulation, Hydration, Oral mucosa, Permeability
in
Journal of Drug Delivery Science and Technology
volume
48
pages
8 pages
publisher
EDITIONS SANTE
external identifiers
  • scopus:85055034037
ISSN
1773-2247
DOI
10.1016/j.jddst.2018.10.004
language
English
LU publication?
yes
id
363c7ce2-72b5-44e5-a1e4-3ffafd8a0089
date added to LUP
2018-10-26 13:50:01
date last changed
2020-04-02 02:09:44
@article{363c7ce2-72b5-44e5-a1e4-3ffafd8a0089,
  abstract     = {<p>Formulations for buccal drug delivery often comprise polymers to facilitate mucoadhesion based on water sorption. The main objective of the current study was therefore to evaluate the effect of dehydration on drug uptake through oral mucosa. We have used diffusion cells with excised porcine mucosa to study uptake of three alternative drugs (i.e., Metronidazole, Benzydamine and Xylometazoline) together with polyethylene glycol (PEG) as the model polymer for adjusting water activity in the test solutions. Taking drug activity into account, we can conclude that addition of PEG results in a drug flux through mucosa that is about two times lower for Metronidazole and more than 40 times lower for Xylometazoline compared to that from a pure PBS-solution. However, for Benzydamine the uptake through mucosa was more or less the same, which could possibly be due to the high PEG-concentration (65 wt%) affecting the dissociation constant and thus the permeability. These results indicate that an increased water gradient may have the same limiting effect on permeability through oral mucosa as previously seen for skin. Thus, water gradient effects should be a factor to consider when developing buccal adhesive formulations.</p>},
  author       = {Ali, Abdullah and Wahlgren, Marie and Pedersen, Lina and Engblom, Johan},
  issn         = {1773-2247},
  language     = {eng},
  pages        = {338--345},
  publisher    = {EDITIONS SANTE},
  series       = {Journal of Drug Delivery Science and Technology},
  title        = {Will a water gradient in oral mucosa affect transbuccal drug absorption?},
  url          = {http://dx.doi.org/10.1016/j.jddst.2018.10.004},
  doi          = {10.1016/j.jddst.2018.10.004},
  volume       = {48},
  year         = {2018},
}