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Polymer-drug interactions and wetting of solid dispersions

Dahlberg, Carina LU ; Millqvist-Fureby, Anna LU ; Schuleit, Michael and Furó, István (2010) In European Journal of Pharmaceutical Sciences 39(1-3). p.125-133
Abstract

We demonstrate the ability of drugs to influence the wetting of solid dispersion tablets in unexpected ways. Five model drugs of different water solubility and ability to interact with the involved polymers were incorporated in hydrophilic polymer matrices, made of either hydroxypropyl methylcellulose (HPMC) or polyvinyl pyrrolidone (PVP). The physical mixtures of all combinations of drug and polymer presented surface hydrophobicities, as measured by the equilibrium advancing contact angle of water, which are expected for materials that do not influence the interactions of each other with water. However, the solid dispersions containing HPMC deviated from this regular behaviour and displayed contact angles below those of the pure... (More)

We demonstrate the ability of drugs to influence the wetting of solid dispersion tablets in unexpected ways. Five model drugs of different water solubility and ability to interact with the involved polymers were incorporated in hydrophilic polymer matrices, made of either hydroxypropyl methylcellulose (HPMC) or polyvinyl pyrrolidone (PVP). The physical mixtures of all combinations of drug and polymer presented surface hydrophobicities, as measured by the equilibrium advancing contact angle of water, which are expected for materials that do not influence the interactions of each other with water. However, the solid dispersions containing HPMC deviated from this regular behaviour and displayed contact angles below those of the pure compounds involved, either drug or polymer. This behaviour is explained by changed surface exposure of HPMC side groups, as a result of changes in intermolecular hydrogen bonds. In addition to water contact angle measurements, we employed NMR imaging to monitor the time course of water ingress and swelling.

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author
; ; and
publishing date
type
Contribution to journal
publication status
published
keywords
Contact angle, Hydrophilic matrices, Hydroxypropyl methylcellulose (HPMC), Nuclear magnetic resonance imaging, Polyvinyl pyrrolidone (PVP)
in
European Journal of Pharmaceutical Sciences
volume
39
issue
1-3
pages
9 pages
publisher
Elsevier
external identifiers
  • scopus:73749083466
  • pmid:19932176
ISSN
0928-0987
DOI
10.1016/j.ejps.2009.11.005
language
English
LU publication?
no
id
8659d724-0264-41e0-ba60-fe32c4c86a7a
date added to LUP
2025-04-02 22:33:21
date last changed
2025-04-16 23:18:55
@article{8659d724-0264-41e0-ba60-fe32c4c86a7a,
  abstract     = {{<p>We demonstrate the ability of drugs to influence the wetting of solid dispersion tablets in unexpected ways. Five model drugs of different water solubility and ability to interact with the involved polymers were incorporated in hydrophilic polymer matrices, made of either hydroxypropyl methylcellulose (HPMC) or polyvinyl pyrrolidone (PVP). The physical mixtures of all combinations of drug and polymer presented surface hydrophobicities, as measured by the equilibrium advancing contact angle of water, which are expected for materials that do not influence the interactions of each other with water. However, the solid dispersions containing HPMC deviated from this regular behaviour and displayed contact angles below those of the pure compounds involved, either drug or polymer. This behaviour is explained by changed surface exposure of HPMC side groups, as a result of changes in intermolecular hydrogen bonds. In addition to water contact angle measurements, we employed NMR imaging to monitor the time course of water ingress and swelling.</p>}},
  author       = {{Dahlberg, Carina and Millqvist-Fureby, Anna and Schuleit, Michael and Furó, István}},
  issn         = {{0928-0987}},
  keywords     = {{Contact angle; Hydrophilic matrices; Hydroxypropyl methylcellulose (HPMC); Nuclear magnetic resonance imaging; Polyvinyl pyrrolidone (PVP)}},
  language     = {{eng}},
  month        = {{01}},
  number       = {{1-3}},
  pages        = {{125--133}},
  publisher    = {{Elsevier}},
  series       = {{European Journal of Pharmaceutical Sciences}},
  title        = {{Polymer-drug interactions and wetting of solid dispersions}},
  url          = {{http://dx.doi.org/10.1016/j.ejps.2009.11.005}},
  doi          = {{10.1016/j.ejps.2009.11.005}},
  volume       = {{39}},
  year         = {{2010}},
}