PURPOSE: Skin permeation/penetration enhancers are substances that enable drug delivery through or into the skin. METHODS: To search for new enhancers with high but reversible activity and acceptable toxicity, we synthesized a series of D-glucose derivatives, both hydrophilic and amphiphilic. RESULTS: Initial evaluation of the ability of these sugar derivatives to increase permeation and penetration of theophylline through/into human skin compared with a control (no enhancer) or sorbitan monolaurate (Span 20; positive control) revealed dodecyl 6-amino-6-deoxy-α-D-glucopyranoside 5 as a promising enhancer. Furthermore, this amino sugar 5 increased epidermal concentration of a highly hydrophilic antiviral cidofovir by a factor of 7. The effect of compound 5 on skin electrical impedance suggested its direct interaction with the skin barrier. Infrared spectroscopy of isolated stratum corneum revealed no effect of enhancer 5 on the stratum corneum proteins but an overall decrease in the lipid chain order. The enhancer showed acceptable toxicity on HaCaT keratinocyte and 3T3 fibroblast cell lines. Finally, transepidermal water loss returned to baseline values after enhancer 5 had been removed from the skin. CONCLUSIONS: Compound 5, a dodecyl amino glucoside, is a promising enhancer that acts through a reversible interaction with the stratum corneum lipids.

• Klíčová slova
• penetration enhancers, sugar, topical drug delivery, transdermal drug delivery,
• MeSH
• antivirové látky aplikace a dávkování   metabolismus   MeSH
• aplikace kožní MeSH
• aplikace lokální MeSH
• buněčné linie MeSH
• cidofovir MeSH
• cytosin aplikace a dávkování   analogy a deriváty   metabolismus   MeSH
• epidermis účinky léků   metabolismus   MeSH
• farmaceutická chemie MeSH
• glukosidy chemická syntéza   farmakologie   MeSH
• hexosy farmakologie   MeSH
• hydrofobní a hydrofilní interakce MeSH
• keratinocyty účinky léků   metabolismus   MeSH
• kožní absorpce MeSH
• kůže účinky léků   metabolismus   MeSH
• lékové transportní systémy MeSH
• lidé MeSH
• lipidy fyziologie   MeSH
• organofosfonáty aplikace a dávkování   metabolismus   MeSH
• permeabilita MeSH
• theofylin aplikace a dávkování   metabolismus   MeSH
• viabilita buněk MeSH
• vztahy mezi strukturou a aktivitou MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• antivirové látky MeSH
• cidofovir MeSH
• cytosin MeSH
• glukosidy MeSH
• hexosy MeSH
• lipidy MeSH
• organofosfonáty MeSH
• sorbitan monolaurate MeSH Prohlížeč
• theofylin MeSH

The microbial biotransformation using low-cost feedstock to produce biopolymers (degradable), an alternative to petrochemical-based synthesis plastics (non-degradable), can be a beneficial approach towards sustainable development. In this study, the dairy industry processes waste (whey) is used in polyhydroxyalkanoate (PHA) copolymer production. Initial screening suggested that Ralstonia eutropha produced higher PHA as compared to Bacillus megaterium. A central composite rotatable design-based optimization using two process variables (amino acid and tween-80) concentration remarkably influenced PHA co-polymer production under physiological conditions of pH (7), temperature (37 °C), and agitation rate of 150 rpm. High polyhydroxybutyrate (PHB) mass fraction yield of 69.3% was observed as compared to predicted yield of 62.8% from deproteinized whey as feed. The combination of tryptophan (50 mg L-1) and tween-80 (3 mL-1) enhanced R. eutropha mass gain to 6.80 g L-1 with PHB contents of 4.71 g L-1. Further, characterization of PHA and its copolymers was done by ESI-MS, FTIR, and TEM. On upscaling up to 3.0 L, the PHA contents and yields were noted as quite similar by R. eutropha. This study demonstrates that dairy waste processing waste can be potentially utilized as inexpensive feed for producing high content of biopolymers to develop a sustainable system of waste management.

• MeSH
• aminokyseliny MeSH
• biopolymery MeSH
• plastické hmoty MeSH
• polyhydroxyalkanoáty * chemie   MeSH
• polysorbáty * MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• aminokyseliny MeSH
• biopolymery MeSH
• plastické hmoty MeSH
• polyhydroxyalkanoáty * MeSH
• polysorbáty * MeSH

Unknown impurities were identified in ibuprofen (IBU) soft gelatin capsules (SGCs) during long-term stability testing by a UHPLC method with UV detection and its chemical formula was determined using high resolution/accurate mass (HRAM) LC-MS. Reference standards of the impurities were subsequently synthesized, isolated by semi-preparative HPLC and characterized using HRAM LC-MS, NMR and IR. Two impurities were formed by esterification of IBU with polyethylene glycol (PEG), which is used as a fill of the SGCs, and were identified as IBU-PEG monoester and IBU-PEG diester. Two other degradants arised from reaction of IBU with sorbitol and sorbitan, which are components of the shell and serves as plasticizers. Thus, IBU sorbitol monoester (IBU-sorbitol) and IBU sorbitan monoester (IBU-sorbitan ester) were identified. An UHPLC method was further optimized in order to separate, selectively detect and quantify the degradation products in IBU SGCs.

• MeSH
• esterifikace MeSH
• ibuprofen analýza   chemie   izolace a purifikace   MeSH
• polysorbáty MeSH
• referenční standardy MeSH
• sorbitol MeSH
• stabilita léku MeSH
• tobolky MeSH
• vysokoúčinná kapalinová chromatografie metody   MeSH
• želatina MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• ibuprofen MeSH
• polysorbáty MeSH
• sorbitol MeSH
• tobolky MeSH
• želatina MeSH

• MeSH
• Clostridium perfringens účinky léků   enzymologie   MeSH
• fosfolipasy biosyntéza   MeSH
• kultivační média MeSH
• polyethylenglykoly farmakologie   MeSH
• polysorbáty farmakologie   MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• fosfolipasy MeSH
• kultivační média MeSH
• polyethylenglykoly MeSH
• polysorbáty MeSH

By using dimethyl sulfoxide or Tween 80 (1 or 0.2%), the production of L-lysine was increased by 20-28 and 23-25%, respectively, in regulatory mutant strains of Corynebacterium glutamicum. The stimulation observed is supposed to be caused by influencing cellular surface structures.

• MeSH
• Corynebacterium účinky léků   genetika   metabolismus   MeSH
• dimethylsulfoxid farmakologie   MeSH
• lysin biosyntéza   MeSH
• mutace MeSH
• polysorbáty farmakologie   MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• dimethylsulfoxid MeSH
• lysin MeSH
• polysorbáty MeSH

A bacterium isolated from Assam (India) soil was found to accumulate L-valine in the growth medium and was identified as Micrococcus varians. The strain grew and accumulated valine in a purely synthetic medium, but supplementation with either casamino acids or yeast extract or with both, improved the yield. The entire fermentation period could be divided into a growth phase and a production (phase which could be prolonged by adjustment of pH to neutral range. Among the different hydrocarbon and nitrogen sources tested straight run gas-oil and ammonium sulphate, respectively, were found most suitable. Antibiotics inhibited growth but stimulated extracellular valine accumulation. Vitamins stimulated growth and valine yield and an inoculum level of 10% was found to be optimal. The yield of L-valine under optimal conditions was 2.95 g/L.

• MeSH
• antibakteriální látky farmakologie   MeSH
• kultivační média MeSH
• Micrococcus účinky léků   růst a vývoj   metabolismus   MeSH
• polysorbáty farmakologie   MeSH
• uhlovodíky metabolismus   MeSH
• valin analýza   biosyntéza   MeSH
• vitaminy farmakologie   MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• antibakteriální látky MeSH
• kultivační média MeSH
• polysorbáty MeSH
• uhlovodíky MeSH
• valin MeSH
• vitaminy MeSH

Serum esterase activity was estimated in 148 patients with bronchogenic carcinoma and in 19 patients with pulmonary tuberculosis before operation, 1 week and 3 weeks after operation. We failed to prove significant differences between the patients with malignant and nonmalignant lung diseases. We failed also to prove significant differences between the mean esterase activity findings regarding to the extent of surgery. They were identical even of the performed thoracotomy was radical, palliative or explorative. The course of changes in esterase activity findings is quite individual. From the esterase activity we cannot conclude, if the tumor tissue was completely removed or not.

• MeSH
• bronchogenní karcinom enzymologie   chirurgie   MeSH
• esterasy krev   MeSH
• lidé MeSH
• nádory plic enzymologie   chirurgie   MeSH
• plicní tuberkulóza enzymologie   chirurgie   MeSH
• polysorbáty MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• esterasy MeSH
• polysorbáty MeSH

Dye decolorization capacity of two white-rot fungi, Irpex lacteus and Phanerochaete chrysosporium, was compared in N-limited liquid cultures. The agitated cultures showed lower ability to decolorize azo dyes Reactive Orange 16 and Naphthol Blue Black than static cultures. Similar effect was also observed with other structurally different synthetic dyes. The effect of surfactants on the decolorization process is discussed. A significant increase in the Reactive Orange 16 decolorization by the agitated I. lacteus cultures was observed after adding 0.1% Tween 80, following a higher Mn-dependent peroxidase production. The in vitro dye decolorization using the purified enzyme proved its decolorization ability.

• MeSH
• azosloučeniny metabolismus   MeSH
• barvicí látky metabolismus   MeSH
• Basidiomycota účinky léků   enzymologie   metabolismus   MeSH
• enzymová indukce MeSH
• peroxidasy metabolismus   MeSH
• Phanerochaete enzymologie   metabolismus   MeSH
• polysorbáty farmakologie   MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• srovnávací studie MeSH
• Názvy látek
• azosloučeniny MeSH
• barvicí látky MeSH
• manganese peroxidase MeSH Prohlížeč
• peroxidasy MeSH
• polysorbáty MeSH
• reactive orange 16 MeSH Prohlížeč

• MeSH
• fixní kombinace léků MeSH
• lidé MeSH
• nemoci úst farmakoterapie   MeSH
• oxid křemičitý terapeutické užití   MeSH
• parabeny terapeutické užití   MeSH
• pektiny terapeutické užití   MeSH
• polysorbáty terapeutické užití   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• fixní kombinace léků MeSH
• oxid křemičitý MeSH
• parabeny MeSH
• pektiny MeSH
• polysorbáty MeSH

Tween-ether toxoplasma antigen for the complement fixation test was verified on a more extensive clinical material. From a series of 949 patient's sera, positive reaction was obtained in 44% of samples with the tween-ether antigen and in only 33.5% of samples with the FT antigen. All sera, giving positive results only with the tween-ether antigen, were also positive in the Sabin-Feldman test. The authors believe that by using this type of more sensitive antigen, containing also the cell-wall components of Toxoplasma gondii, it would be possible to standardize serological examination by the complement fixation test on the basis of an international standard serum.

• MeSH
• antigeny * MeSH
• ether MeSH
• komplement fixační testy * MeSH
• lidé MeSH
• polysorbáty MeSH
• Toxoplasma imunologie   MeSH
• toxoplazmóza diagnóza   imunologie   MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• antigeny * MeSH
• ether MeSH
• polysorbáty MeSH