14th Hellenic Polymer Society International Conference
22-25 November, 2023, Thessaloniki, Greece

Invited lecture: Thiolated Polymers – Thiomers: Utilizing the most prominent bridging structure designed by nature

Prof. Dr. A. Bernkop-Schnürch
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2nd Edition International Conference on Nanotechnology & Materials Science
Conference
September 23-25, 2024
Paris, France

Invited lecture:
Thiolated Nanocarriers for Drug Delivery: Mimicking the Workhorses of Our Body

Prof. Dr. A. Bernkop-Schnürch
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In order to improve the bioavailability of non-invasively administered drugs permeation enhancing drug delivery systems are often essential. Thiolated polymers have been demonstrated to show a strong permeation enhancing effect for the uptake of drugs from mucosal membranes such as the intestinal [Clausen, A.E., Kast, C.E. and Bernkop-Schnürch, A. (2002). The role of glutathione in the permeation enhancing effect of thiolated polymers. Pharm. Res., 19, 602; Clausen, A.E., and Bernkop-Schnürch, A. (2001) Thiolated Carboxy- methylcellulose: In vitro evaluation of its permeation enhancing effect on peptide drugs. Eur. J. Parm. Biopharm., 51, 25; Kast, C.E. and Bernkop-Schnürch, A. (2002) Influence of the molecular mass on the permeation enhancing effect of different poly(acrylates). STP pharma, 12, 351] and nasal mucosa [Leitner V.M., Guggi D., Bernkop-Schnürch A. (2004) Thiomers in noninvasive polypeptide delivery: in vitro and in vivo characterization of a polycarbophil-cysteine/glutathione gel formulation for human growth hormone. J. Pharm. Sci. 93, 1682].

In comparison to most low molecular weight permeation enhancers, thiolated polymers offer the advantage of not being absorbed from the mucosal membrane. Hence, their permeation enhancing effect can be maintained for a comparatively longer period of time and systemic toxic side effects of the auxiliary agent can be excluded. The mechanism being responsible for the permeation enhancing effect of thiomers has been discovered within the last years showing a reversible opening of the tight junctions and the role of glutathione as permeation mediator [Clausen, A.E., Kast, C.E. and Bernkop-Schnürch, A. (2002). The role of glutathione in the permeation enhancing effect of thiolated polymers. Pharm. Res., 19, 602].

As this permeation enhancing mechanism differs from most conventionally used permeation enhancers such as fatty acids, the effect can be even further improved by the combination of both types of permeation enhancing systems. The permeation enhancing properties of thiomers were also demonstrated in various in vivo studies.

Furthermore, this permeation enhancing effect of thiomers is even much higher when they are preactivated [e.g. Wang, X., Iqbal, J., Rahmat, D. and Bernkop-Schnürch, A. (2012) Preactivated thiomers: permeation enhancing properties. Int. J. Pharm., 438, 217].

A. Bernkop-Schnürch, CSO ThioMatrix, was honored with the Science Award of Tyrol 2023
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