Discovery & Development Europe 2025: Formulation & Drug Delivery Congress
July 1-2, 2025
Basel, Switzerland

Invited lecture:
Oral Delivery Of Peptide And Protein Drugs – Oral Delivery of GLP-1 Analogues

Prof. Dr. A. Bernkop-Schnürch
more...

8th European Cyclodextrin Conference
September 9-12, 2025
Milano, Italy

Invited lecture:
Thiolated Cyclodextrins in Drug Delivery

Prof. Dr. A. Bernkop-Schnürch
more...

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].

Thiomatrix joined the EU-project TENTACLE (101191747) focusing on the use of thiomers for in situ bioprinting.
more....

Download references about thiomers