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5th International Conference and Exhibition on Pharmaceutical Science and Technology
June 21-23, 2022
Bangkok, Thailand

Invited lecture:
Lipid-based Nanocarriers for Oral Delivery of Therapeutic Peptides: Hype or Hope?
Prof. Dr. A. Bernkop-Schnürch
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13th Global Drug Delivery & Formulation Summit
June 27-29, 2022
Berlin, Germany

Invited lecture:
Novel Nanotechnologies for Mucosal Delivery of Small Molecules and Biologics: Old Problems but New Solutions
Prof. Dr. A. Bernkop-Schnürch
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Preactivated thiomersWhen even higher mucoadhesive properties are needed, thiomers can be preactivated by the covalent attachment of mercaptonicotinamide substructures via disulfide bonds.

MucoadhesionMucoadhesive properties of polyacrylic acid (PAA) and thiolated polyacrylic acid (thiolated PAA), for instance, were strongly improved by preactivation (preactivated thiolated PAA) [Iqbal, J., Shahnaz, G., Dünnhaupt, S., Müller, C., Hintzen, F. and Bernkop-Schnürch, A. (2012) Preactivated thiomers as mucoadhesive polymers for drug delivery. Biomaterials, 33, 1528]. Furthermore, mucoadhesive properties of chitosan were 7-fold increased by thiolation and even 14-fold improved when this thiolated polymer was additionally preactivated [Dünnhaupt, S., Barthelmes, J., Thurner, C.C., Waldner, C., Sakloetsakun, D. and Bernkop-Schnürch A. (2012) S-protected thiolated chitosan: synthesis and in vitro characterization. Carbohydr. Polym., 90, 765].

 

 

Mucoadhesion


As the uptake of most drugs from mucosal membranes is controlled by a passive diffusion process, it is essential to provide on the absorption membrane a concentration gradient as steep as possible representing the driving force for drug absorption. In order to achieve that goal the delivery system has to be kept as long as possible in intimate contact with the absorption membrane, which can be guaranteed by utilizing mucoadhesive drug delivery systems. The mucoadhesive properties of all so far used polymers, however, are quite insufficient in order to guarantee this effect. In contrast to these ‘conventional’ polymers, whose mucoadhesive properties are exclusively based on non-covalent bonds, thiolated polymers or designated thiomers are capable of forming covalent bonds with cysteine-rich subdomains of the mucus gel layer. The bridging structure most commonly utilized in biological systems - namely the disulfide bond - is thereby used.

These improved mucoadhesive properties of thiolated polymers were meanwhile verified for various polymers. Due to the immobilization of thiol groups the mucoadhesive properties of chitosan and poly(acrylic acid), for instance, were improved at least 140-fold [Bernkop-Schnürch, A., Hornof, M. and Zoidl, T. (2003) Thiolated polymers – thiomers: modification of chitosan with 2-iminothiolane, Int. J. Pharm., 260, 229] and 20-fold [Marschütz, M.K., and Bernkop-Schnürch, A. (2002) Thiolated polymers: Advance in mucoadhesion by use of in-situ crosslinking poly(acrylic acid)-cysteine conjugates. Eur. J. Pharm. Sci., 15, 387],respectively. The mucoadhesive properties of drug delivery systems based on thiomers were also demonstratedin human volunteers.


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A. Bernkop-Schnürch, CSO ThioMatrix, was honored with the Gattefossé North America Award 2017
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