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1.
Basic Clin Pharmacol Toxicol ; 112(6): 385-91, 2013 Jun.
Article in English | MEDLINE | ID: mdl-23331460

ABSTRACT

Non-alcoholic steatohepatitis (NASH) is a frequent condition in obese patients that may progress to end-stage liver disease. This study was designed to evaluate the modulation of this condition by use of quercetin (Q), a flavonoid largely found in vegetable foods, with known anti-inflammatory and antioxidant properties, in the experimental model of non-alcoholic steatohepatitis (NASH) using a diet deficient in methionine and choline (MCD). Male C57BL6 mice were divided into four groups (n = 16): (i) Control plus vehicle (control ration plus carboxymethylcellulose 1% used as vehicle, CO + V); (ii) Control ration plus Q 50 mg/kg (CO + Q); (iii) MCD diet plus vehicle (NASH + V); and (iv) MCD diet plus Q (NASH + Q). Diets were administered for 4 weeks. At the end of the experimental period, liver alterations, bioindicators of oxidative stress and DNA damage were assessed. NASH was diagnosed in 100% of the mice that were fed the MCD diet. In addition, a significant increase in DNA damage in liver tissue from NASH + V group was observed in comparison with CO + V. The group NASH + Q showed a significant decrease in hepatic damage enzymes, lipoperoxidation, DNA damage and a lower degree of macrovesicular steatosis, ballooning and inflammatory process. These findings suggest that Q may have protective effects by improving liver integrity in NASH.


Subject(s)
Antioxidants/therapeutic use , DNA Damage , Fatty Liver/prevention & control , Quercetin/therapeutic use , Animals , Antioxidants/administration & dosage , Choline Deficiency , Comet Assay , DNA Damage/drug effects , Diet , Disease Models, Animal , Fatty Liver/etiology , Fatty Liver/metabolism , Fatty Liver/pathology , Lipid Peroxidation/drug effects , Liver Function Tests , Male , Methionine/deficiency , Mice , Mice, Inbred C57BL , Molecular Structure , Oxidative Stress/drug effects , Quercetin/administration & dosage
2.
Drug Dev Ind Pharm ; 37(8): 886-93, 2011 Aug.
Article in English | MEDLINE | ID: mdl-21247375

ABSTRACT

OBJECTIVE: To evaluate the effect of different cyclodextrins (ß-cyclodextrin [ß-CD], methyl-ß-cyclodextrin [Mß-CD], or hydroxypropyl-ß-cyclodextrin [HPß-CD]) and/or hydrophilic polymers (carboxymethylcellulose, hydroxypropylmethylcellulose [HPMC], polyethyleneglycol, or polyvinylpyrrolidone [PVP]) on daidzein solubility in water. MATERIALS AND METHODS: The corresponding associations were characterized in aqueous media using phase-solubility studies. The morphology of daidzein/cyclodextrin freeze-dried complexes was characterized using scanning electron microscopy, and their spatial configuration was proposed by means of nuclear magnetic resonance spectroscopy. RESULTS AND DISCUSSION: In the presence of 6 mM of cyclodextrins, the solubility of daidzein in water was significantly enhanced: 5.7-fold (ß-CD), 7.2-fold (Mß-CD), and 9.4-fold (HPß-CD). The analysis of the three solid complexes proved that the formation of inclusion complexes occurred through the insertion of the B and C rings of daidzein molecule into the cyclodextrins cavity. The association of daidzein/cyclodextrin complexes to the hydrophilic polymers HPMC or PVP (1%, w/w) was able to improve the solubility of daidzein even further. CONCLUSION: The highest solubilizing effect was obtained for daidzein/HPß-CD/PVP ternary system (12.7-fold).


Subject(s)
Cyclodextrins/chemistry , Isoflavones/chemistry , Phytoestrogens/chemistry , Polymers/chemistry , Chemistry, Pharmaceutical , Hydrophobic and Hydrophilic Interactions , Magnetic Resonance Spectroscopy/methods , Solubility , Water/chemistry
3.
RBCF, Rev. bras. ciênc. farm. (Impr.) ; 42(4): 531-537, out.-dez. 2006. tab, graf
Article in Portuguese | LILACS | ID: lil-446374

ABSTRACT

Os objetivos deste estudo foram desenvolver e avaliar a estabilidade física de loções do tipo O/A contendo 6 por cento (p/p) do filtro solar octilmetoxicinamato (OMC) ou metilbenzilidenocânfora (MBC). As formulações foram armazenadas em temperatura ambiente durante seis meses e durante este período foram avaliadas com relação às suas características macroscópicas, viscosidade, comportamento reológico, índice de óleo, espalhabilidade e Fator de Proteção Solar (FPS). Os resultados demonstram que as formulações foram estáveis por seis meses. Os valores de FPS foram significativamente (P < 0,05) maiores para a formulação MBC. Em contrapartida, a formulação OMC apresentou valores de espalhabilidade significativamente (P < 0,05) superiores e valores de viscosidade significativamente (P < 0,05) inferiores durante todo o período de armazenamento.


The objectives of this study were to develop and to evaluate the physical stability of O/W lotions containing 6 percent (w/w) of the sunscreen octylmethoxycinnamate (OMC) or methyl benzylidene camphor (MBC). The formulations were stored at room temperature, for six months and during this period its macroscopic characteristics, viscosity and rheological behavior, oil indexes, spreading properties and Sun Protection Factor (SPF) were evaluated. The results demonstrate that both formulations were stable for six months. The SPF values were significantly (P < 0.05) higher for MBC formulation. On the other hand, the OMC formulation presented significantly (P < 0.05) higher spreading and lower viscosity values during the storage period.


Subject(s)
Beauty Lotions , Cosmetic Stability , Sunscreening Agents , Chemistry, Pharmaceutical , Cosmetics
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