Base de dados : MEDLINE
Pesquisa : D02.092.471.302 [Categoria DeCS]
Referências encontradas : 658 [refinar]
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[PMID]:27769669
[Au] Autor:Stallivieri A; Colombeau L; Jetpisbayeva G; Moussaron A; Myrzakhmetov B; Arnoux P; Acherar S; Vanderesse R; Frochot C
[Ad] Endereço:Laboratoire Réactions et Génie des Procédés, UMR-CNRS 7274, Lorraine-Université, 1 rue Grandville, BP 20451, 54001 Nancy Cedex, France.
[Ti] Título:Folic acid conjugates with photosensitizers for cancer targeting in photodynamic therapy: Synthesis and photophysical properties.
[So] Source:Bioorg Med Chem;25(1):1-10, 2017 Jan 01.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Recent researches in photodynamic therapy have focused on novel techniques to enhance tumour targeting of anticancer drugs and photosensitizers. Coupling a photosensitizer with folic acid could allow more effective targeting of folate receptors which are over-expressed on the surface of many tumour cells. In this study, different folic acid-OEG-conjugated photosensitizers were synthesized, characterized and their photophysical properties were evaluated. The introduction of an OEG does not significantly improve the hydrophilicity of the FA-porphyrin. All the FA-targeted photosensitizers present good to very good photophysical properties. The best one appears to be Ce6. Molar extinction coefficient, fluorescence and singlet oxygen quantum yields were determined and were compared to the corresponding photosensitizer alone.
[Mh] Termos MeSH primário: Dietilaminas/química
Ácido Fólico/análogos & derivados
Fármacos Fotossensibilizantes/química
Porfirinas/química
[Mh] Termos MeSH secundário: Técnicas de Química Sintética
Dietilaminas/síntese química
Ácido Fólico/síntese química
Seres Humanos
Neoplasias/tratamento farmacológico
Fotoquimioterapia
Fármacos Fotossensibilizantes/síntese química
Porfirinas/síntese química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (2,2'-(ethylenedioxy)diethylamine); 0 (Diethylamines); 0 (Photosensitizing Agents); 0 (Porphyrins); 5S2CCF3T1Z (phytochlorin); 935E97BOY8 (Folic Acid)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170726
[Lr] Data última revisão:
170726
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161023
[St] Status:MEDLINE


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[PMID]:27769530
[Au] Autor:van Hengel J; Van den Broeke C; Pieters T; Libbrecht L; Hofmann I; van Roy F
[Ad] Endereço:Molecular Cell Biology Unit, Inflammation Research Center, VIB, Ghent, Belgium; Department of Biomedical Molecular Biology, Faculty of Sciences, Ghent University, Ghent, Belgium; Department of Basic Medical Sciences, Faculty of Medicine and Health Sciences, Ghent University, Ghent, Belgium. Electron
[Ti] Título:Inactivation of p120 catenin in mice disturbs intrahepatic bile duct development and aggravates liver carcinogenesis.
[So] Source:Eur J Cell Biol;95(12):574-584, 2016 Dec.
[Is] ISSN:1618-1298
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:p120 catenin (p120ctn) is required for the stability of classic cadherins at the cell surface and is thought to play a central role in modulating cell-cell adhesion. Cytoplasmic p120ctn promotes cell motility, and probably other activities, by modulating the activities of RhoA, Rac and Cdc42. E-cadherin is expressed in periportal but not in perivenous hepatocytes. In contrast, all hepatocytes of normal mouse liver express N-cadherin. Cholangiocytes express exclusively E-cadherin. Mice with p120ctn ablation in hepatocytes and cholangiocytes (p120LiKO mice) were generated by Cre-loxP technology. Livers were examined by histological, immunohistochemical, ultrastructural and serum analysis to determine the effect of the p120ctn ablation on liver structure and function. Mouse hepatocyte differentiation and homeostasis were not impaired. However, hepatoblasts differentiated abnormally into hybrid hepato-biliary cells, ductal plate structures were irregular in p120LiKO newborns, and further development of intrahepatic bile ducts was severely impaired. In adults, enrichment of ductular structures was accompanied by portal inflammation and fibrosis. p120LiKO mice did not spontaneously develop hepatocellular carcinoma but initiation of hepatocarcinogenesis by diethylnitrosamine was accelerated. In summary: p120ctn has a critical role in biliary differentiation and is a potent suppressor of liver tumor growth.
[Mh] Termos MeSH primário: Ductos Biliares Intra-Hepáticos/metabolismo
Carcinoma Hepatocelular/metabolismo
Cateninas/metabolismo
Diferenciação Celular
Transformação Celular Neoplásica/metabolismo
Neoplasias Hepáticas/metabolismo
Proteínas de Neoplasias/metabolismo
[Mh] Termos MeSH secundário: Animais
Carcinoma Hepatocelular/induzido quimicamente
Carcinoma Hepatocelular/genética
Cateninas/genética
Transformação Celular Neoplásica/induzido quimicamente
Transformação Celular Neoplásica/genética
Dietilaminas/toxicidade
Hepatócitos/metabolismo
Neoplasias Hepáticas/genética
Camundongos
Camundongos Knockout
Proteínas de Neoplasias/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Catenins); 0 (Diethylamines); 0 (Neoplasm Proteins); 0 (delta catenin); D7TJ0C6RJO (N-nitrodiethylamine)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170209
[Lr] Data última revisão:
170209
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161023
[St] Status:MEDLINE


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[PMID]:27439356
[Au] Autor:Servais AC; Janicot B; Takam A; Crommen J; Fillet M
[Ad] Endereço:Laboratory for the Analysis of Medicines, Dept. of Pharmacy, CIRM, University of Liège, CHU, B36, B-4000 Liege, Belgium. Electronic address: acservais@ulg.ac.be.
[Ti] Título:Liquid chromatography separation of the chiral prodrug eslicarbazepine acetate and its main metabolites in polar organic mode. Application to their analysis after in vitro metabolism.
[So] Source:J Chromatogr A;1467:306-311, 2016 Oct 07.
[Is] ISSN:1873-3778
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:A LC method using a chiral stationary phase (CSP) with cellulose tris(3-chloro-4-methylphenylcarbamate) as chiral selector in polar organic mode (POM) was developed for the separation of the biopharmaceutic classification system (BCS) class II chiral prodrug eslicarbazepine acetate (ESL) and its main metabolites, namely eslicarbazepine, its optical antipode, (R)-licarbazepine, and the achiral oxcarbazepine (OXC). The percentage of methanol (MeOH) in the mobile phase containing acetonitrile (ACN) as the main solvent was found to significantly influence analyte retention and resolution. A reversal of elution order of OXC and (R)-licarbazepine was observed, depending on the MeOH percentage in the mobile phase. The optimized mobile phase consisted of ACN/MeOH/acetic acid/diethylamine (95/5/0.2/0.07; v/v/v/v). The potential of this chemo- and enantioselective LC method combined with solid-phase extraction (SPE) was then evaluated for in vitro metabolism studies using ESL as a model case. Only eslicarbazepine could be detected after incubation of ESL in human liver microsome systems.
[Mh] Termos MeSH primário: Dibenzazepinas/isolamento & purificação
Pró-Fármacos/isolamento & purificação
[Mh] Termos MeSH secundário: Ácido Acético
Acetonitrilos
Carbamazepina/análogos & derivados
Carbamazepina/química
Carbamazepina/isolamento & purificação
Celulose/análogos & derivados
Celulose/química
Celulose/isolamento & purificação
Cromatografia Líquida/métodos
Dibenzazepinas/química
Dibenzazepinas/metabolismo
Dietilaminas
Seres Humanos
Microssomos Hepáticos/química
Fenilcarbamatos/química
Fenilcarbamatos/isolamento & purificação
Pró-Fármacos/metabolismo
Extração em Fase Sólida
Solventes
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (10,11-dihydro-10-hydroxy-5H-dibenz(b,f)azepine-5-carboxamide); 0 (Acetonitriles); 0 (Dibenzazepines); 0 (Diethylamines); 0 (Phenylcarbamates); 0 (Prodrugs); 0 (Solvents); 0 (cellulose tris(3-chloro-4-methylphenylcarbamate)); 33CM23913M (Carbamazepine); 9004-34-6 (Cellulose); B035PIS86W (diethylamine); BEA68ZVB2K (eslicarbazepine acetate); Q40Q9N063P (Acetic Acid); S5VXA428R4 (eslicarbazepine); VZI5B1W380 (oxcarbazepine); Z072SB282N (acetonitrile)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:171008
[Lr] Data última revisão:
171008
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160722
[St] Status:MEDLINE


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[PMID]:27438252
[Au] Autor:Citraningrum HM; Liu JC
[Ad] Endereço:Department of Chemical Engineering, National Taiwan University of Science and Technology, 43 Keelung Road, Section 4, Taipei 10607, Taiwan E-mail: liu1958@mail.ntust.edu.tw.
[Ti] Título:Effect of competing amines on the removal of tetramethylammonium hydroxide from solution using ion exchange.
[So] Source:Water Sci Technol;74(2):466-72, 2016.
[Is] ISSN:0273-1223
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Tetramethylammonium hydroxide (TMAH, TMA(+)) has been widely used as the photoresist developer in semiconductor and thin film transistor liquid crystal display manufacturing. In this study, TMAH-containing wastewater was treated by ion exchange method. Strong acid cation exchange resin was used. A kinetics study revealed that the ion exchange reaction reached equilibrium within 20 min and it could be described by a pseudo-second-order model. To assess the effects of competing ions, wastewater was spiked with three different amines, namely ethylamine (EA(+)), diethylamine (DEA(+)), and triethylamine (TEA(+)). TMAH uptake decreased when in the presence of amines, and it decreased in the order EA(+) < DEA(+) < TEA(+). It could be attributed to different proton affinity (PA) and the strength of affinity between amine molecules and resin matrix, as found from the ab initio calculation values and Langmuir isotherm parameters. However, the interaction energy between sulphonic acid groups and interfering amines in solution using density functional theory (DFT) calculation resulted in a different trend compared with that of PA. The difference might be caused by stabilization of amines by resin matrix and different molecular structures.
[Mh] Termos MeSH primário: Aminas/química
Resinas de Troca de Cátion/química
Resíduo Eletrônico/análise
Compostos de Amônio Quaternário/química
Eliminação de Resíduos Líquidos/métodos
[Mh] Termos MeSH secundário: Dietilaminas/química
Etilaminas/química
Águas Residuais/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amines); 0 (Cation Exchange Resins); 0 (Diethylamines); 0 (Ethylamines); 0 (Quaternary Ammonium Compounds); 0 (Waste Water); B035PIS86W (diethylamine); H0W55235FC (tetramethylammonium); VOU728O6AY (triethylamine); YG6MGA6AT5 (ethylamine)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:170117
[Lr] Data última revisão:
170117
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160721
[St] Status:MEDLINE
[do] DOI:10.2166/wst.2016.167


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[PMID]:27083367
[Au] Autor:Dias SF; Nogueira SS; de França Dourado F; Guimarães MA; de Oliveira Pitombeira NA; Gobbo GG; Primo FL; de Paula RC; Feitosa JP; Tedesco AC; Nunes LC; Leite JR; da Silva DA
[Ad] Endereço:UFPI, Research Center in Biodiversity and Biotechnology - Biotech Campus Parnaíba, Federal University of Piauí, Av São Sebastian 2819, 64202-020 Parnaíba, Piauí, Brazil.
[Ti] Título:Acetylated cashew gum-based nanoparticles for transdermal delivery of diclofenac diethyl amine.
[So] Source:Carbohydr Polym;143:254-61, 2016 Jun 05.
[Is] ISSN:1879-1344
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Nanoprecipitation and dialysis methods were employed to obtain nanoparticles (NPs) of acetylated cashew gum (ACG). NPs synthesized by dialysis showed greater average size compared to those synthesized by nanoprecipitation, but they presented improved stability and yield. NPs were loaded with diclofenac diethylamine and the efficiency of the drug incorporation was over 60% for both methods, for an ACG:NP a weight ratio of 10:1. The cytotoxicity assay demonstrated that the NPs had no significant effect on the cell viability, verifying their biocompatibility. The release profile for the diclofenac diethylamine associated with the ACG-NPs showed a more controlled release compared to the free drug and a Fickian diffusion mechanism was observed. Transdermal permeation reached 90% penetration of the drug.
[Mh] Termos MeSH primário: Diclofenaco/análogos & derivados
Diclofenaco/administração & dosagem
Dietilaminas/administração & dosagem
Nanopartículas/química
Gomas Vegetais/síntese química
[Mh] Termos MeSH secundário: Acetilação
Administração Cutânea
Anacardium
Linhagem Celular
Diclofenaco/química
Dietilaminas/química
Composição de Medicamentos
Liberação Controlada de Fármacos
Nanopartículas/toxicidade
Tamanho da Partícula
Gomas Vegetais/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Diethylamines); 0 (Plant Gums); 0 (diclofenac diethylamine); 144O8QL0L1 (Diclofenac)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170213
[Lr] Data última revisão:
170213
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160417
[St] Status:MEDLINE


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[PMID]:27018187
[Au] Autor:Wang Q; Yu L; Sun Y
[Ad] Endereço:Department of Biochemical Engineering and Key Laboratory of Systems Bioengineering of Ministry of Education, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China.
[Ti] Título:Grafting glycidyl methacrylate to Sepharose gel for fabricating high-capacity protein anion exchangers.
[So] Source:J Chromatogr A;1443:118-25, 2016 Apr 22.
[Is] ISSN:1873-3778
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:To develop ion exchangers of high protein adsorption capacity, we have herein introduced atom transfer radical polymerization (ATRP) method to graft glycidyl methacrylate (GMA) onto Sepharose FF gel. GMA-grafted Sepharose FF resins of four grafting densities and different grafting chain lengths were obtained by adjusting reaction conditions. The epoxy groups on the grafted chains were functionalized by modification with diethylamine (DEA), leading to the fabrication of Sepharose-based anion exchangers of 14 different grafting densities and/or grafting chain lengths. The resins were first characterized for the effects of grafting density, chain length and ionic strength on pore sizes by inverse size exclusion chromatography. Then, the resins were evaluated by adsorption equilibria of bovine serum albumin (BSA) as a function of ionic capacity (IC) (chain length) at individual grafting densities. It was observed that at each grafting density there was a specific IC value (chain length) that offered the maximum equilibrium capacity. Of the resins with maximum values at individual grafting densities, the resin of the second grafting density with an IC value of 330 mmol/L (denoted as FF-Br2-pG-D330) showed the highest capacity, 264 mg/mL, about two times higher than that of the traditional ungrafted resin Q Sepharose FF (137 mg/mL). This resin also showed the most favorable uptake kinetics among the resins of similar IC values but different grafting densities, or of the same grafting density but different IC values. Effects of ionic strength showed that the capacities of FF-Br2-pG-D330 were much higher than Q Sepharose FF at a wide range of NaCl concentrations (0-200 mmol/L), and the uptake rates of the two resins were similar in the ionic strength range. Therefore, the dynamic binding capacity values of BSA on FF-Br2-pG-D330 were much higher than Q Sepharose FF as demonstrated at different residence times and ionic strengths. Taken together, the research has proved the success in the fabrication of high-capacity protein anion exchangers by grafting GMA onto Sepharose gel.
[Mh] Termos MeSH primário: Técnicas de Química Analítica/métodos
Compostos de Epóxi/química
Metacrilatos/química
Sefarose/química
[Mh] Termos MeSH secundário: Adsorção
Ânions
Cromatografia em Gel
Dietilaminas/química
Cinética
Concentração Osmolar
Soroalbumina Bovina/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anions); 0 (Diethylamines); 0 (Epoxy Compounds); 0 (Methacrylates); 27432CM55Q (Serum Albumin, Bovine); 9012-36-6 (Sepharose); B035PIS86W (diethylamine); R8WN29J8VF (glycidyl methacrylate)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160329
[St] Status:MEDLINE


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[PMID]:26921388
[Au] Autor:Obach RS; Walker GS; Brodney MA
[Ad] Endereço:Pharmacokinetics, Pharmacodynamics, and Drug Metabolism (R.S.O., G.S.W.) and Worldwide Medicinal Chemistry (M.A.B.), Pfizer Inc., Groton, Connecticut and Cambridge, Massachusetts r.scott.obach@pfizer.com.
[Ti] Título:Biosynthesis of Fluorinated Analogs of Drugs Using Human Cytochrome P450 Enzymes Followed by Deoxyfluorination and Quantitative Nuclear Magnetic Resonance Spectroscopy to Improve Metabolic Stability.
[So] Source:Drug Metab Dispos;44(5):634-46, 2016 May.
[Is] ISSN:1521-009X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Replacement of hydrogen with fluorine is a useful drug design strategy when decreases in cytochrome P450 (P450) metabolic lability are needed. In this paper, a facile two-step method of inserting fluorine into metabolically labile sites of drug molecules is described that utilizes less than 1 mg of starting material and quantitative NMR spectroscopy to ascertain the structures and concentrations of products. In the first step, hydroxyl metabolites are biosynthesized using human P450 enzymes, and in the second step these metabolites are subjected to deoxyfluorination using diethylaminosulfur trifluoride (DAST). The method is demonstrated using midazolam, celecoxib, ramelteon, and risperidone as examples and CYP3A5, 2C9, 1A2, and 2D6 to catalyze the hydroxylations. The drugs and their fluoro analogs were tested for metabolic lability. 9-Fluororisperidone and 4'-fluorocelecoxib were 16 and 4 times more metabolically stable than risperidone and celecoxib, respectively, and 2-fluororamelteon and ramelteon were metabolized at the same rate. 1'-Fluoromidazolam was metabolized at the same rate as midazolam by CYP3A4 but was more stable in CYP3A5 incubations. The P450-catalyzed sites of metabolism of the fluorine-containing analogs were determined. Some of the metabolites arose via metabolism at the fluorine-substituted carbon, wherein the fluorine was lost to yield aldehydes. In summary, this method offers an approach whereby fluorine can be substituted in metabolically labile sites, and the products can be tested to determine whether an enhancement in metabolic stability was obtained.
[Mh] Termos MeSH primário: Sistema Enzimático do Citocromo P-450/metabolismo
Flúor/química
Preparações Farmacêuticas/química
[Mh] Termos MeSH secundário: Aldeídos/química
Celecoxib/química
Dietilaminas/química
Halogenação
Seres Humanos
Hidroxilação
Indenos/química
Espectroscopia de Ressonância Magnética/métodos
Microssomos Hepáticos/metabolismo
Midazolam/química
Risperidona/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Aldehydes); 0 (Diethylamines); 0 (Indenes); 0 (Pharmaceutical Preparations); 284SYP0193 (Fluorine); 78622BV6IJ (diethylaminosulfur trifluoride); 901AS54I69 (ramelteon); 9035-51-2 (Cytochrome P-450 Enzyme System); JCX84Q7J1L (Celecoxib); L6UH7ZF8HC (Risperidone); R60L0SM5BC (Midazolam)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160228
[St] Status:MEDLINE
[do] DOI:10.1124/dmd.116.069310


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[PMID]:26888602
[Au] Autor:Ambade A; Satishchandran A; Szabo G
[Ad] Endereço:Department of Medicine, University of Massachusetts Medical School, Worcester, MA 01604 United States.
[Ti] Título:Alcoholic hepatitis accelerates early hepatobiliary cancer by increasing stemness and miR-122-mediated HIF-1α activation.
[So] Source:Sci Rep;6:21340, 2016 Feb 18.
[Is] ISSN:2045-2322
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Alcohol-related hepatocellular carcinoma (HCC) develops with advanced alcoholic liver disease and liver fibrosis. Using adult mice, we evaluate the effect of alcoholic steatohepatitis on early hepatobiliary carcinoma after initiation by diethyl-nitrosamine (DEN). Here we show that alcohol-fed DEN-injected mice have higher ALT and liver-to-body weight ratio compared to pair-fed DEN-injected mice. Alcohol feeding results in steatohepatitis indicated by increased pro-inflammatory cytokines and fibrotic genes. MRI and liver histology of alcohol+DEN mice shows hepatobiliary cysts, early hepatic neoplasia and increase in serum alpha-fetoprotein. Proliferation makers (BrdU, cyclin D1, p53) and cancer stem cell markers (CD133 and nanog) are significantly up-regulated in livers of alcohol-fed DEN-injected mice compared to controls. In livers with tumors, loss of miR-122 expression with a significant up-regulation of miR-122 target HIF-1α is seen. We conclude that alcoholic steatohepatitis accelerates hepatobiliary tumors with characteristic molecular features of HCC by up-regulating inflammation, cell proliferation, stemness, and miR-122 loss.
[Mh] Termos MeSH primário: Regulação Neoplásica da Expressão Gênica
Hepatite Alcoólica/metabolismo
Subunidade alfa do Fator 1 Induzível por Hipóxia/biossíntese
Neoplasias Hepáticas Experimentais/metabolismo
MicroRNAs/biossíntese
Proteínas de Neoplasias/biossíntese
RNA Neoplásico/biossíntese
Regulação para Cima
[Mh] Termos MeSH secundário: Animais
Dietilaminas/toxicidade
Etanol/toxicidade
Hepatite Alcoólica/patologia
Neoplasias Hepáticas Experimentais/induzido quimicamente
Neoplasias Hepáticas Experimentais/patologia
Masculino
Camundongos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL
[Nm] Nome de substância:
0 (Diethylamines); 0 (Hif1a protein, mouse); 0 (Hypoxia-Inducible Factor 1, alpha Subunit); 0 (MicroRNAs); 0 (Mirn122 microRNA, mouse); 0 (Neoplasm Proteins); 0 (RNA, Neoplasm); 3K9958V90M (Ethanol); D7TJ0C6RJO (N-nitrodiethylamine)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160219
[St] Status:MEDLINE
[do] DOI:10.1038/srep21340


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[PMID]:26369621
[Au] Autor:Hamed R; Basil M; AlBaraghthi T; Sunoqrot S; Tarawneh O
[Ad] Endereço:a Department of Pharmacy, Faculty of Pharmacy , Al-Zaytoonah University of Jordan , Amman , Jordan.
[Ti] Título:Nanoemulsion-based gel formulation of diclofenac diethylamine: design, optimization, rheological behavior and in vitro diffusion studies.
[So] Source:Pharm Dev Technol;21(8):980-989, 2016 Dec.
[Is] ISSN:1097-9867
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Chronic oral administration of the non-steroidal anti-inflammatory drug, diclofenac diethylamine (DDEA), is often associated with gastrointestinal ulcers and bleeding. As an alternative to oral administration, a nanoemulsion-based gel (NE gel) formulation of DDEA was developed for topical administration. An optimized formulation for the o/w nanoemulsion of oil, surfactant and cosurfactant was selected based on nanoemulsion mean droplet size, clarity, stability, and flowability, and incorporated into the gelling agent Carbopol® 971P. Rheological studies of the DDEA NE gel were conducted and compared to those of conventional DDEA gel and emulgel. The three gels exhibited an elastic behavior, where G' dominated G″ at all frequencies, indicating the formation of strong gels. NE gel exhibited higher G' values than conventional gel and emulgel, which indicated the formation of a stronger gel network. Strat-M® membrane, a synthetic membrane with diffusion characteristics that are well correlated to human skin, was used for the in vitro diffusion studies. The release of DDEA from conventional gel, emulgel and NE gel showed a controlled release pattern over 12 h, which was consistent with the rheological properties of the gels. DDEA release kinetics from the three gels followed super case II transport as fitted by Korsmeyer-Peppas model.
[Mh] Termos MeSH primário: Diclofenaco/análogos & derivados
Dietilaminas/química
Emulsões/química
Géis/química
Nanopartículas/química
[Mh] Termos MeSH secundário: Administração Tópica
Anti-Inflamatórios não Esteroides/química
Química Farmacêutica/métodos
Diclofenaco/química
Difusão
Membranas Artificiais
Tamanho da Partícula
Reologia
Solubilidade
Tensoativos/química
Viscosidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Diethylamines); 0 (Emulsions); 0 (Gels); 0 (Membranes, Artificial); 0 (Surface-Active Agents); 0 (diclofenac diethylamine); 144O8QL0L1 (Diclofenac)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170314
[Lr] Data última revisão:
170314
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150916
[St] Status:MEDLINE


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[PMID]:26089167
[Au] Autor:Sengupta S; Banerjee S; Sinha B; Mukherjee B
[Ad] Endereço:Department of Pharmaceutical Technology, Jadavpur University, Kolkata, 700 032, India.
[Ti] Título:Improved Skin Penetration Using In Situ Nanoparticulate Diclofenac Diethylamine in Hydrogel Systems: In Vitro and In Vivo Studies.
[So] Source:AAPS PharmSciTech;17(2):307-17, 2016 Apr.
[Is] ISSN:1530-9932
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Delivering diclofenac diethylamine transdermally by means of a hydrogel is an approach to reduce or avoid systemic toxicity of the drug while providing local action for a prolonged period. In the present investigation, a process was developed to produce nanosize particles (about 10 nm) of diclofenac diethylamine in situ during the development of hydrogel, using simple mixing technique. Hydrogel was developed with polyvinyl alcohol (PVA) (5.8% w/w) and carbopol 71G (1.5% w/w). The formulations were evaluated on the basis of field emission scanning electron microscopy, texture analysis, and the assessment of various physiochemical properties. Viscosity (163-165 cps for hydrogel containing microsize drug particles and 171-173 cps for hydrogel containing nanosize drug particles, respectively) and swelling index (varied between 0.62 and 0.68) data favor the hydrogels for satisfactory topical applications. The measured hardness of the different hydrogels was uniform indicating a uniform spreadability. Data of in vitro skin (cadaver) permeation for 10 h showed that the enhancement ratios of the flux of the formulation containing nanosize drug (without the permeation enhancer) were 9.72 and 1.30 compared to the formulation containing microsized drug and the marketed formulations, respectively. In vivo plasma level of the drug increased predominantly for the hydrogel containing nanosize drug-clusters. The study depicts a simple technique for preparing hydrogel containing nanosize diclofenac diethylamine particles in situ, which can be commercially viable. The study also shows the advantage of the experimental transdermal hydrogel with nanosize drug particles over the hydrogel with microsize drug particles.
[Mh] Termos MeSH primário: Diclofenaco/química
Dietilaminas/química
Hidrogel de Polietilenoglicol-Dimetacrilato/química
Nanopartículas/química
Pele/metabolismo
[Mh] Termos MeSH secundário: Acrilatos/química
Administração Cutânea
Adulto
Animais
Química Farmacêutica/métodos
Diclofenaco/administração & dosagem
Dietilaminas/administração & dosagem
Excipientes/química
Feminino
Seres Humanos
Hidrogel de Polietilenoglicol-Dimetacrilato/administração & dosagem
Masculino
Microscopia Eletrônica de Varredura/métodos
Nanopartículas/administração & dosagem
Tamanho da Partícula
Álcool de Polivinil/química
Ratos
Ratos Sprague-Dawley
Absorção Cutânea
Viscosidade
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Acrylates); 0 (Diethylamines); 0 (Excipients); 0 (carbopol 71G); 144O8QL0L1 (Diclofenac); 25852-47-5 (Hydrogel, Polyethylene Glycol Dimethacrylate); 9002-89-5 (Polyvinyl Alcohol)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150620
[St] Status:MEDLINE
[do] DOI:10.1208/s12249-015-0347-4



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