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Effect of Amino Acids Derivatives And Ceramides on Skin Barrier Function
Janůšová, Barbora ; Vávrová, Kateřina (advisor) ; Balgavý, Pavol (referee) ; Rabišková, Miloslava (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of inorganic and organic chemistry Candidate: Mgr. Barbora Janůšová Supervisor: doc. PharmDr. Kateřina Vávrová, Ph.D. Title of Doctoral Thesis: Effect of amino acids derivatives and ceramides on skin barrier function The main goal of my thesis was to contribute to the understanding of behavior of the ceramides and skin barrier function modulators based on amino acids derivatives, as well as to elucidate the relationship between their structure and activity. Transdermal permeation enhancers are compounds that temporarily decrease skin barrier properties to promote drug flux. In the first part of my thesis, enhancers with amino acids (proline, sarcosine, alanine, β-alanine, and glycine) attached to hydrophobic chain(s) via a biodegradable ester link were investigated. The double-chain lipid-like substances displayed no enhancing effect, whereas single-chain substances significantly increased skin permeability. The most active enhancer - proline derivative L-Pro2 reached enhancement ratios of up to 40 at 1% concentration, which is higher than that of the well-established and standard enhancers Azone, DDAIP, DDAK, and Transkarbam 12. No stereoselectivity was observed. L-Pro2 acted synergistically with propylene glycol and...
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