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Real time MRI to elucidate the functionality of coating films intended for modified release

Bernin, Diana ; Marucci, Mariagrazia LU ; Boissier, Catherine ; Hjärtstam, Johan ; Olsson, Ulf LU and Abrahmsén-Alami, Susanna (2019) In Journal of Controlled Release 311-312. p.117-124
Abstract

Polymer films based on mixtures of ethyl cellulose (EC) and hydroxypropyl cellulose (HPC) have been widely used to coat pellets and tablets to modify the release profile of drugs. For three different EC/HPC films we used 1H and 19F MRI in combination with a designed release cell to monitor the drug, polymer and water in 5 dimensional (5D) datasets; three spatial, one diffusion or relaxation and a temporal dimension, in real time. We observed that the water inflow through the films correlated with the initiation of the dissolution of the drug in the tablet beneath the film. Leaching of the pore forming HPC further accelerated water penetration and resulted in a drug release onset after a hydrostatic pressure was... (More)

Polymer films based on mixtures of ethyl cellulose (EC) and hydroxypropyl cellulose (HPC) have been widely used to coat pellets and tablets to modify the release profile of drugs. For three different EC/HPC films we used 1H and 19F MRI in combination with a designed release cell to monitor the drug, polymer and water in 5 dimensional (5D) datasets; three spatial, one diffusion or relaxation and a temporal dimension, in real time. We observed that the water inflow through the films correlated with the initiation of the dissolution of the drug in the tablet beneath the film. Leaching of the pore forming HPC further accelerated water penetration and resulted in a drug release onset after a hydrostatic pressure was generated below the film indicated by positional changes of the film. For the more permeable film, both water ingress and drug egress showed a large variability of release over the film surface indicating the heterogeneity of the system. Furthermore, the 1H diffusion dataset revealed the formation of a gel layer of HPC at the film surface. We conclude that the setup presented provides a significant level of details, which are not achieved with traditional methods.

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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
F MRI, H MRI, Controlled release, Diffusion, Drug release, Polymer, Pore formation
in
Journal of Controlled Release
volume
311-312
pages
8 pages
publisher
Elsevier
external identifiers
  • scopus:85071742536
  • pmid:31454531
ISSN
0168-3659
DOI
10.1016/j.jconrel.2019.08.025
language
English
LU publication?
yes
id
ed344782-7a98-4883-8934-8fb92ac5a27c
date added to LUP
2019-09-16 13:22:33
date last changed
2019-11-25 09:34:25
@article{ed344782-7a98-4883-8934-8fb92ac5a27c,
  abstract     = {<p>Polymer films based on mixtures of ethyl cellulose (EC) and hydroxypropyl cellulose (HPC) have been widely used to coat pellets and tablets to modify the release profile of drugs. For three different EC/HPC films we used <sup>1</sup>H and <sup>19</sup>F MRI in combination with a designed release cell to monitor the drug, polymer and water in 5 dimensional (5D) datasets; three spatial, one diffusion or relaxation and a temporal dimension, in real time. We observed that the water inflow through the films correlated with the initiation of the dissolution of the drug in the tablet beneath the film. Leaching of the pore forming HPC further accelerated water penetration and resulted in a drug release onset after a hydrostatic pressure was generated below the film indicated by positional changes of the film. For the more permeable film, both water ingress and drug egress showed a large variability of release over the film surface indicating the heterogeneity of the system. Furthermore, the <sup>1</sup>H diffusion dataset revealed the formation of a gel layer of HPC at the film surface. We conclude that the setup presented provides a significant level of details, which are not achieved with traditional methods.</p>},
  author       = {Bernin, Diana and Marucci, Mariagrazia and Boissier, Catherine and Hjärtstam, Johan and Olsson, Ulf and Abrahmsén-Alami, Susanna},
  issn         = {0168-3659},
  language     = {eng},
  pages        = {117--124},
  publisher    = {Elsevier},
  series       = {Journal of Controlled Release},
  title        = {Real time MRI to elucidate the functionality of coating films intended for modified release},
  url          = {http://dx.doi.org/10.1016/j.jconrel.2019.08.025},
  doi          = {10.1016/j.jconrel.2019.08.025},
  volume       = {311-312},
  year         = {2019},
}