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Effects of Added Surfactant on Swelling and Molecular Transport in Drug-Loaded Tablets Based on Hydrophobically Modified Poly(acrylic acid)

Knöös, Patrik LU ; Wahlgren, Marie LU ; Topgaard, Daniel LU ; Ulvenlund, Stefan LU and Piculell, Lennart LU (2014) In The Journal of Physical Chemistry Part B 118(32). p.9757-9767
Abstract
A combination of NMR chemical shift imaging and self-diffusion experiments is shown to give a detailed molecular picture of the events that occur when tablets of hydrophobically modified poly(acrylic acid) loaded with a drug (griseofulvin) swell in water in the presence or absence of surfactant (sodium octylbenzenesulfonate). The hydrophobic substituents on the polymer bind and trap the surfactant molecules in mixed micelles, leading to a slow effective surfactant transport that occurs via a small fraction of individually dissolved surfactant molecules in the water domain. Because of the efficient binding of surfactant, the penetrating water is found to diffuse past the penetrating surfactant into the polymer matrix, pushing the surfactant... (More)
A combination of NMR chemical shift imaging and self-diffusion experiments is shown to give a detailed molecular picture of the events that occur when tablets of hydrophobically modified poly(acrylic acid) loaded with a drug (griseofulvin) swell in water in the presence or absence of surfactant (sodium octylbenzenesulfonate). The hydrophobic substituents on the polymer bind and trap the surfactant molecules in mixed micelles, leading to a slow effective surfactant transport that occurs via a small fraction of individually dissolved surfactant molecules in the water domain. Because of the efficient binding of surfactant, the penetrating water is found to diffuse past the penetrating surfactant into the polymer matrix, pushing the surfactant front outward as the matrix swells. The added surfactant has little effect on the transport of drug because both undissolved solid drug and surfactant-solubilized drug function as reservoirs that essentially follow the polymer as it swells. However, the added surfactant nevertheless has a strong indirect effect on the release of griseofulvin, through the effect of the surfactant on the solubility and erosion of the polymer matrix. The surfactant effectively solubilizes the hydrophobically modified polymer, making it fully miscible with water, leading to a more pronounced swelling and a slower erosion of the polymer matrix. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
The Journal of Physical Chemistry Part B
volume
118
issue
32
pages
9757 - 9767
publisher
The American Chemical Society
external identifiers
  • wos:000340443100022
  • scopus:84906074835
ISSN
1520-5207
DOI
10.1021/jp501288u
language
English
LU publication?
yes
id
471999f6-c3de-48d7-a036-1b94404b6fbd (old id 4656309)
date added to LUP
2014-09-24 14:13:29
date last changed
2017-08-06 03:58:59
@article{471999f6-c3de-48d7-a036-1b94404b6fbd,
  abstract     = {A combination of NMR chemical shift imaging and self-diffusion experiments is shown to give a detailed molecular picture of the events that occur when tablets of hydrophobically modified poly(acrylic acid) loaded with a drug (griseofulvin) swell in water in the presence or absence of surfactant (sodium octylbenzenesulfonate). The hydrophobic substituents on the polymer bind and trap the surfactant molecules in mixed micelles, leading to a slow effective surfactant transport that occurs via a small fraction of individually dissolved surfactant molecules in the water domain. Because of the efficient binding of surfactant, the penetrating water is found to diffuse past the penetrating surfactant into the polymer matrix, pushing the surfactant front outward as the matrix swells. The added surfactant has little effect on the transport of drug because both undissolved solid drug and surfactant-solubilized drug function as reservoirs that essentially follow the polymer as it swells. However, the added surfactant nevertheless has a strong indirect effect on the release of griseofulvin, through the effect of the surfactant on the solubility and erosion of the polymer matrix. The surfactant effectively solubilizes the hydrophobically modified polymer, making it fully miscible with water, leading to a more pronounced swelling and a slower erosion of the polymer matrix.},
  author       = {Knöös, Patrik and Wahlgren, Marie and Topgaard, Daniel and Ulvenlund, Stefan and Piculell, Lennart},
  issn         = {1520-5207},
  language     = {eng},
  number       = {32},
  pages        = {9757--9767},
  publisher    = {The American Chemical Society},
  series       = {The Journal of Physical Chemistry Part B},
  title        = {Effects of Added Surfactant on Swelling and Molecular Transport in Drug-Loaded Tablets Based on Hydrophobically Modified Poly(acrylic acid)},
  url          = {http://dx.doi.org/10.1021/jp501288u},
  volume       = {118},
  year         = {2014},
}