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CONTROLLED DRUG RELEASE
| Due to a sustained drug
release, a prolonged therapeutic level of drugs exhibiting a short
elimination half-live can be maintained. Consequently the frequency of
dosing can be reduced contributing to an improved compliance. The release of
drugs out of polymeric carrier systems can be controlled by a simple
diffusion process. So far the efficacy of such delivery systems, however,
was limited by a too rapid disintegration and/or erosion of the polymeric
network [Bernkop-Schnürch, A., Scholler, S., and Biebel, R.G. (2000).
Development of controlled drug release systems based on polymer-cysteine
conjugates. J. Control. Release, 66, 39-48; Clausen, A.E., and
Bernkop-Schnürch, A. (2001) Development and in vitro evaluation of a peptide
drug delivery system based on thiolated polycarbophil. Pharm. Ind., 63,
312-317]. By using thiolated polymers this essential shortcoming can be
overcome. Because of the formation of inter- and intrachain disulfide bonds
during the swelling process, the stability of the polymeric drug carrier
matrix is strongly improved. Hence, a controlled drug release for numerous
hours is guaranteed. This controlled drug release has also been demonstrated
by studies in human volunteers. |
The formation of inter- and
intramolecular disulfide bonds within the polymeric network stabilizes drug
delivery systems based on thiomers. Click on the picture. |
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Disintegration behaviour of
tablets based on polycarbophil (PCP) or sodium carboxymethylcellulose (CMC). Click
on the graph to see the
improvement in stability by using the corresponding thiolated polymers. [Bernkop-Schnürch, A., Scholler, S.,
and Biebel, R.G. (2000). Development of controlled drug release systems
based on polymer-cysteine conjugates. J. Control. Release, 66, 39-48]
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Release profile of
fluoresein from tablets based on poly(acrylic acid). Click on the graph to see the
improvement in the sustained release utilizing the thiolated version of the
polymer [adopted from Hornof et al. (Hornof,
M.D., Weyenberg, W., Ludwig, A., and Bernkop–Schnürch, A. (2003). A
mucoadhesive ocular insert: Development and in vivo evaluation in humans. J.
Control. Rel. 89, 419-428)]. |
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