Counterfeit steroids are available on the black market, ultimately to consumers who believe they are buying a legitimate pharmaceutical item from the labeled company. In many cases, counterfeit steroids can contain lower doses or some products can be overdosed. This can unwittingly expose users to a significant health risks. The mixture of testosterone propionate, phenylpropionate, isocaproate and decanoate in an oil-based injectable dosage form belongs to the one of the most misused illicit drugs by a variety of athletes. This study developed a new, fast, simple and reliable HPLC method combined with a simple sample preparation step to determine testosterone propionate, phenylpropionate, isocaproate and decanoate in an oil-based injectable dosage form without the use of sophisticated and expensive instrumentation. The developed analytical procedure provides high throughput of samples where LC analysis takes only 6min and sample preparation of oil matrix in one step takes approximately 10min with precision ranging from 1.03 to 3.38% (RSD), and accuracy (relative error %) within ±2.01%. This method was found to be precise, linear, accurate, sensitive, selective and robust for routine application in screening of commercial pharmaceutical products based on content of mentioned testosterone esters in their oil-based injectable dosage form for counterfeit drugs. This method was successfully applied to the analysis of nine samples of commercial testosterone mixtures purchased from various sources and will be further used as an effective screening method for determination of previously mentioned testosterone esters in samples confiscated by Institute of Forensic Science (Slovakia) during the illegal trade.

• MeSH
• kongenery testosteronu analýza   MeSH
• lidé MeSH
• odhalování abúzu drog metody   MeSH
• padělané léky analýza   MeSH
• reprodukovatelnost výsledků MeSH
• teplota MeSH
• testosteron analýza   MeSH
• vysokoúčinná kapalinová chromatografie metody   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH

Over the past decade, the use of anabolic androgenic steroids (AAS) by recreational bodybuilders and regular gym members has been increasing exponentially. However, there is a lack of knowledge on AAS products sold in the Czech Republic and Slovakia. The aim of this study was to assess the quantity of active substances in AAS products obtained from AAS users in the Czech Republic and Slovakia. In addition, the study also examines the current trends in counterfeit AAS products used by recreational bodybuilders and regular gym members. For this purpose, the authors developed and validated a universal ultra-high performance liquid chromatography with tandem mass spectrometry method to determine the most popular doping substances in different pharmaceutical formulations (oil-based injectables, tablets, and capsules). This method was successfully utilized for the analysis of 358 AAS products. Our results showed that 58.9% AAS products analyzed contained the declared active substances at the declared concentrations, 15.9% contained no active substance, 16.8% were under-concentrated, 4.5% contained active substances different from those declared on the label, and 3.6% products were over-concentrated. Alarmingly, the results demonstrated that over 40% of the AAS analyzed failed to meet label claims and therefore may pose serious health risks to consumers. This study also highlighted that the availability of AAS should be more rigorously restricted and their quality closely monitored in order to protect AAS users. In conclusion, the authors have developed a precise, accurate, sensitive, selective, and robust method for the routine screening of products containing anabolic androgenic steroids.

• MeSH
• injekce statistika a číselné údaje   MeSH
• kongenery testosteronu analýza   ekonomika   MeSH
• lidé MeSH
• tablety MeSH
• tandemová hmotnostní spektrometrie metody   MeSH
• tobolky MeSH
• vysokoúčinná kapalinová chromatografie metody   MeSH
• zločin ekonomika   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Geografické názvy
• Česká republika MeSH
• Slovenská republika MeSH

Systemic administration of bisphosphonates, e.g. sodium alendronate (Aln) is characterized by extremely low bioavailability and high toxicity. To omit aforementioned drawbacks an injectable system for the intra-bone delivery of Aln based on Aln-loaded nanoparticles (NPs-Aln) suspended in a hydrogel matrix (gellan gum, GG) was developed. Aln was encapsulated in poly(lactide-co-glycolide) (PLGA 85:15) by solid-oil-water emulsification. Drug release tests showed that within 25 days all the encapsulated drug was released from NPs-Aln and the release rate was highest at the beginning and decreased with time. In contrast, by suspending NPs-Aln in a GG matrix, the release rate was significantly lower and more constant in time. The GG-NPs-Aln system was engineered to be easily injectable and was able to reassemble its structure after extrusion as shown by rheological measurements. Invitro studies showed that the GG-NPs-Aln was cytocompatible with MG-63 osteoblast-like cells and it inhibited RANKL-mediated osteoclastic differentiation of RAW 264.7 cells. The injectability, the sustained local delivery of small doses of Aln and the biological activity render the GG-NPs-Aln system promising for the local treatment of osteoporosis and other bone tissue disorders.

• MeSH
• alendronát aplikace a dávkování   chemie   MeSH
• bakteriální polysacharidy chemie   MeSH
• buněčná diferenciace účinky léků   MeSH
• farmaceutická chemie MeSH
• farmaceutická technologie metody   MeSH
• hydrogely MeSH
• inhibitory kostní resorpce aplikace a dávkování   chemie   MeSH
• injekce MeSH
• kinetika MeSH
• kyselina mléčná chemie   MeSH
• kyselina polyglykolová chemie   MeSH
• lidé MeSH
• ligand RANK farmakologie   MeSH
• myši MeSH
• nádorové buněčné linie MeSH
• nanočástice * MeSH
• nanotechnologie MeSH
• nosiče léků * MeSH
• osteoblasty účinky léků   metabolismus   MeSH
• osteoklasty účinky léků   metabolismus   MeSH
• RAW 264.7 buňky MeSH
• reologie MeSH
• rozpustnost MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• myši MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH

Intradermal (i.d.) application of vaccine is promising way how to induce specific immune response against particular pathogens. Adjuvants, substances added into vaccination dose with the aim to increase immunogenicity, play important role in activation of dendritic cells with subsequent activation of lymphocytes. They can, however, induce unwanted local reactions. The aim of the study was to determine the effect of i.d. administration of model antigen keyhole limped hemocyanine alone or with different adjuvants-aluminium hydroxide and oil-based adjuvants-on local histopathological reaction as well as dendritic cell activation at the site of administration and local cytokine and chemokine response. This was assessed at 4 and 24 hours after application. Selection of the adjuvants was based on the fact, that they differently enhance antibody or cell-mediated immunity. The results showed activation of dendritic cells and both Th1 and Th2 response stimulated by oil-based adjuvants. It was associated with higher expression of set of genes, incl. chemokine receptor CCR7 or Th1-associated chemokine CXCL10 and cytokine IFNγ. Application of the antigen with aluminium hydroxide induced higher expression of Th2-associated IL4 or IL13. On the other hand, both complete and incomplete Freund´s adjuvants provoked strong local reaction associated with influx of neutrophils. This was accompanied with high expression of proinflammatory IL1 or neutrophil chemoattractant CXCL8. Surprisingly, similarly strong local reaction was detected also after application of aluminium hydroxide-based adjuvant. The best balanced local reaction with sufficient activation of immune cells was detected after application of oil-based adjuvants Montanide and Emulsigen.

• MeSH
• adjuvancia imunologická farmakologie   MeSH
• cytokiny imunologie   MeSH
• dendritické buňky cytologie   imunologie   MeSH
• imunizace * MeSH
• injekce intradermální MeSH
• prasata MeSH
• Th1 buňky cytologie   imunologie   MeSH
• Th2 buňky cytologie   imunologie   MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH

The ability of different adjuvants to enhance immune responses to intradermal (ID) immunisation with a model antigen was studied in pigs. Immune responses were evaluated with respect to the intensity of systemic and mucosal antibody formation, their isotype characterisation and rate of cell-mediated immunity. These findings were compared with the intensity of adverse local reactions. Six groups of piglets were immunised with keyhole limpet haemocyanin (KLH) antigen alone or in combination with aluminium hydroxide or selected oil-based adjuvants (complete and incomplete Freund's adjuvants, Montanide ISA 206 and Emulsigen). Systemic specific antibody responses were significantly increased following ID administration of antigen together with any of the adjuvants used. IgG antibody responses were most pronounced after the first administration of antigen, being stimulated with both Freund's and Montanide ISA 206 adjuvants. The oil adjuvants also enhanced the cell-mediated immune responses and the levels of local IgA antibodies in the respiratory mucosa. On the other hand, they elicited more pronounced adverse local reactions.

• MeSH
• adjuvancia imunologická farmakologie   MeSH
• antigeny aplikace a dávkování   imunologie   farmakologie   MeSH
• Freundovo adjuvans farmakologie   MeSH
• hemokyanin imunologie   MeSH
• humorální imunita účinky léků   imunologie   MeSH
• imunoglobulin G imunologie   MeSH
• injekce intradermální veterinární   MeSH
• prasata imunologie   MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH

BACKGROUND: Long-chain n-3 polyunsaturated fatty acids (LC n-3 PUFA) of marine origin exert multiple beneficial effects on health. Our previous study in mice showed that reduction of adiposity by LC n-3 PUFA was associated with both, a shift in adipose tissue metabolism and a decrease in tissue cellularity. The aim of this study was to further characterize the effects of LC n-3 PUFA on fat cell proliferation and differentiation in obese mice. METHODS: A model of inducible and reversible lipoatrophy (aP2-Cre-ERT2 PPARγL2/L2 mice) was used, in which the death of mature adipocytes could be achieved by a selective ablation of peroxisome proliferator-activated receptor γ in response to i.p. injection of tamoxifen. Before the injection, obesity was induced in male mice by 8-week-feeding a corn oil-based high-fat diet (cHF) and, subsequently, mice were randomly assigned (day 0) to one of the following groups: (i) mice injected by corn-oil-vehicle only, i.e."control" mice, and fed cHF; (ii) mice injected by tamoxifen in corn oil, i.e. "mutant" mice, fed cHF; (iii) control mice fed cHF diet with15% of dietary lipids replaced by LC n-3 PUFA concentrate (cHF+F); and (iv) mutant mice fed cHF+F. Blood and tissue samples were collected at days 14 and 42. RESULTS: Mutant mice achieved a maximum weight loss within 10 days post-injection, followed by a compensatory body weight gain, which was significantly faster in the cHF as compared with the cHF+F mutant mice. Also in control mice, body weight gain was depressed in response to dietary LC n-3 PUFA. At day 42, body weights in all groups stabilized, with no significant differences in adipocyte size between the groups, although body weight and adiposity was lower in the cHF+F as compared with the cHF mice, with a stronger effect in the mutant than in control mice. Gene expression analysis documented depression of adipocyte maturation during the reconstitution of adipose tissue in the cHF+F mutant mice. CONCLUSION: Dietary LC n-3 PUFA could reduce both hypertrophy and hyperplasia of fat cells in vivo. Results are in agreement with the involvement of fat cell turnover in control of adiposity.

• MeSH
• cyklooxygenasy genetika   metabolismus   MeSH
• epididymis metabolismus   patologie   MeSH
• exprese genu MeSH
• genový knockout MeSH
• kukuřičný olej škodlivé účinky   MeSH
• myši transgenní MeSH
• myši MeSH
• obezita chemicky indukované   prevence a kontrola   MeSH
• omega-3 mastné kyseliny farmakologie   MeSH
• PPAR alfa genetika   metabolismus   MeSH
• PPAR gama genetika   MeSH
• preklinické hodnocení léčiv MeSH
• proliferace buněk účinky léků   MeSH
• proteiny genetika   metabolismus   MeSH
• stearyl-CoA-desaturasa genetika   metabolismus   MeSH
• trans-aktivátory genetika   metabolismus   MeSH
• tukové buňky účinky léků   patologie   MeSH
• zvířata MeSH
• Check Tag
• mužské pohlaví MeSH
• myši MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH

• MeSH
• fyziologie výživy MeSH
• nutriční nároky MeSH
• stopové prvky normy   metabolismus   MeSH

• Konspekt
• Fyziologie člověka a srovnávací fyziologie
• NLK Obory
• nutriční terapie, dietoterapie a výživa
• vnitřní lékařství
• NLK Publikační typ
• publikace WHO

• Publikační typ
• příručky MeSH

• Konspekt
• Chemie. Mineralogické vědy
• NLK Obory
• chemie, klinická chemie