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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
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8th European Cyclodextrin Conference
September 9-12, 2025
Milano, Italy
Invited lecture:
Thiolated Cyclodextrins in Drug Delivery
Prof. Dr. A. Bernkop-Schnürch
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 Degradation of the peptide
drug leu-enkephalin by aminopeptidase N(grey graph). Due to the addition of 0.5% thiomer drug stability is significantly improved (blue graph) [Bernkop-Schnürch, A., Zarti, H. and Walker, G.F. (2001) Thiolation of polycarbophil enhances its inhibition of soluble and intestinal brush border membrane bound aminopeptidase N. J. Pharm. Sci., 90, 1907].
 Hydrolysis of the substrate
hippuryl-L-phenylalanine (HPA) to L-phenylalanine (PA) and hippuric acid by
carboxypeptidase A (grey graph). Due to the addition of 012.5% thiomer drug stability is significantly improved (blue graph). [Bernkop-Schnürch, A. and Thaler, S.
(2000). Polycarbophil-cysteine conjugates as platforms for oral (poly)peptide
delivery systems. J. Pharm. Sci., 89, 901]
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Enzyme Inhibition
Many non-invasively administered drugs such as therapeutic peptides or nucleic
acids are degraded on the mucosa by membrane bound enzymes strongly reducing
their bioavailability. In case of oral administration this ‘enzymatic
barrier’ is even more pronounced as an additional degradation caused by
luminally secreted enzymes takes place. Because of their capability to bind
Zn2+ ions via thiol groups, thiomers are potent inhibitors of most membrane
bound and secreted zinc-dependent enzymes.Due to this enzyme inhbitory effect, thiomers can sginificantly improve the bioavailability of non-invasively administered drugs.
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News
Thiomatrix joined the EU-project TENTACLE (101191747) focusing on the use of thiomers for in situ bioprinting.
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ThioMatrix Hotline:
+43 512 890046
Mo-Th 9.00-17.00
and Fr 9.00-14.00
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