As proven in clinical trials, superficial fungal infections can be effectively treated by single topical application of terbinafine hydrochloride (Ter-HCl) in a film forming system (FFS). Poly(lactic-co-glycolic acid) (PLGA) derivatives, originally synthesized with intention to get carriers with optimized properties for drug delivery, and multifunctional plasticizers - ethyl pyruvate, methyl salicylate, or triacetin - were used for formulation of Ter-HCl loaded FFSs. After spraying, a biodegradable, transparent, adhesive, and occlusive thin layer is formed on the skin, representing drug depot. In situ formed films were characterized by thermal, structural, viscoelastic, and antifungal properties as well as drug release and skin penetration. DSC and SEM showed fully amorphous films with Ter-HCl dissolved in PLGA in high concentration (up to 15%). FFSs are viscoelastic fluids with viscosity which can be easily adjusted by the type of plasticizer used and its concentration. The formulations showed excellent bioadhesion properties, thus ensuring persistence on the skin. In situ film based on branched PLGA/A plasticized with 10% of ethyl pyruvate allowed prolonged release of Ter-HCl by linear kinetics for the first 6 days with a total time of almost 14 days. During ex vivo human skin penetration experiment, Ter-HCl was found to be located only in its target layer, the epidermis. According to our results, plasticized branched PLGA derivatives loaded by Ter-HCl are suitable for the development of FFSs for superficial fungal infections treatment.
- MeSH
- antifungální látky MeSH
- lidé MeSH
- mykózy * MeSH
- nosiče léků * MeSH
- terbinafin MeSH
- uvolňování léčiv MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
Učební texty Univerzity Karlovy
2. vydání 161 stran : ilustrace, tabulky ; 30 cm
Vysokoškolská učebnice pro studující farmacie, která se zaměřuje na obecnou chemii.; Přehled obecné chemie pro posluchače 1. ročníku Farmaceutické fakulty UK. Výklad je zaměřen na stavbu atomu, teorii chemické vazby, na obecné znalosti o skupenských vlastnostech látek a na chemický děj.
- Konspekt
- Chemie. Mineralogické vědy
- Učební osnovy. Vyučovací předměty. Učebnice
- NLK Obory
- chemie, klinická chemie
- farmacie a farmakologie
- NLK Publikační typ
- učebnice vysokých škol
Učební texty Univerzity Karlovy
3. vydání 181 stran : ilustrace ; 21 cm
Skripta slouží pro výuku obecné a anorganické chemie ve studijním programu Farmacie i Zdravotnická bioanalytika.
- MeSH
- anorganická chemie MeSH
- chemie MeSH
- Konspekt
- Anorganická chemie
- Učební osnovy. Vyučovací předměty. Učebnice
- NLK Obory
- chemie, klinická chemie
- NLK Publikační typ
- učebnice vysokých škol
A series of benzaldehyde and salicylaldehyde-S-benzylisothiosemicarbazones was synthesized and tested against 12 different strains of mycobacteria, Gram-positive and Gram-negative bacteria, and the significant selectivity toward mycobacteria was proved. Twenty-eight derivatives were evaluated for the inhibition of isocitrate lyase, which is a key enzyme of the glyoxylate cycle necessary for latent tuberculosis infection, and their iron-chelating properties were investigated. Two derivatives, 5-bromosalicylaldehyde-S-(4-fluorobenzyl)-isothiosemicarbazone and salicylaldehyde-S-(4-bromobenzyl)-isothiosemicarbazone, influenced the isocitrate lyase activity and caused a better inhibition at 10 μmol/L than 3-nitropropionic acid, a standard inhibitor. The compounds were also found to act as exogenous chelators of iron, which is an obligate cofactor for many mycobacterial enzymes. Due to their low cytotoxicity, together with the activity against isocitrate lyase and the ability to sequester iron ions, the compounds belong to potential antibiotics with the main effect on mycobacteria.
- MeSH
- antibakteriální látky chemická syntéza chemie farmakologie MeSH
- antituberkulotika chemická syntéza chemie farmakologie MeSH
- gramnegativní bakterie účinky léků MeSH
- grampozitivní bakterie účinky léků MeSH
- inhibitory enzymů chemická syntéza chemie farmakologie MeSH
- isocitrátlyasa antagonisté a inhibitory MeSH
- Mycobacterium účinky léků MeSH
- racionální návrh léčiv MeSH
- thiosemikarbazony chemická syntéza chemie farmakologie MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Publikační typ
- časopisecké články MeSH
