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[PMID]:29367483
[Au] Autor:Matsuura T; Ogawa A; Ohara Y; Nishina S; Nakanishi M; Gohtani S
[Ad] Endereço:Department of Applied Biological Science, Kagawa University.
[Ti] Título:Effect of Alcohols on the Phase Behavior and Emulsification of a Sucrose Fatty Acid Ester/Water/Edible Oil System.
[So] Source:J Oleo Sci;67(2):167-176, 2018 Feb 01.
[Is] ISSN:1347-3352
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:The effect of alcohols (ethanol, 1-propanol, propylene glycol, glycerin, sucrose) on the phase behavior and emulsification of sucrose stearic acid ester (SSE)/water/edible vegetable oil (EVO) systems was investigated. Adding sucrose, propylene glycol, and glycerin narrowed the oil-separated two-phase region in the phase diagram of the SSE/water/EVO systems, whereas adding ethanol and 1-propanol expanded the oil-separated two-phase region. Changing the course of emulsification in the phase diagram showed that the size of the oil-droplet particle typically decreased in a system with a narrowed oil-separated region. The emulsification properties of the systems varied with respect to changes in the phase diagram. The microstructure of the systems was examined using small-angle X-ray scattering, and the ability to retain the oil in the lamellar structure of the SSEs was suggested as an important role in emulsification, because the mechanism of the systems was the same as that for the liquid crystal emulsification method.
[Mh] Termos MeSH primário: Álcoois/química
Ésteres/química
Ácidos Graxos/química
Transição de Fase
Óleos Vegetais/química
Ácidos Esteáricos/química
Sacarose/química
Água/química
[Mh] Termos MeSH secundário: Emulsões
Glicerol/química
Propilenoglicol/química
Espalhamento a Baixo Ângulo
Difração de Raios X
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alcohols); 0 (Emulsions); 0 (Esters); 0 (Fatty Acids); 0 (Plant Oils); 0 (Stearic Acids); 059QF0KO0R (Water); 4ELV7Z65AP (stearic acid); 57-50-1 (Sucrose); 6DC9Q167V3 (Propylene Glycol); PDC6A3C0OX (Glycerol)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180126
[St] Status:MEDLINE
[do] DOI:10.5650/jos.ess17146


  2 / 1605 MEDLINE  
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[PMID]:29422755
[Au] Autor:Maharana PK; Raghuwanshi S; Chauhan AK; Rai VG; Pattebahadur R
[Ad] Endereço:Department of Ophthalmology, All India Institute of Medical Sciences, Bhopal, Madhya Pradesh, India.
[Ti] Título:Comparison of the Efficacy of Carboxymethylcellulose 0.5%, Hydroxypropyl-guar Containing Polyethylene Glycol 400/Propylene Glycol, and Hydroxypropyl Methyl Cellulose 0.3% Tear Substitutes in Improving Ocular Surface Disease Index in Cases of Dry Eye.
[So] Source:Middle East Afr J Ophthalmol;24(4):202-206, 2017 Oct-Dec.
[Is] ISSN:0975-1599
[Cp] País de publicação:India
[La] Idioma:eng
[Ab] Resumo:PURPOSE: To compare the efficacy of carboxymethylcellulose 0.5% (CMC), hydroxypropyl-guar containing polyethylene glycol 400/propylene glycol (PEG/PG), and hydroxypropyl methylcellulose 0.3% (HPMC) as tear substitutes in patients with dry eye. METHODS: A retrospective evaluation of cases presenting with symptoms of dry eye from July 2014 to June 2015 was done. Patients with Ocular Surface Disease Index (OSDI) scoring >12 were included in the study. Parameters such as age, gender, Schirmer test (ST), and tear film breakup time (TBUT) were recorded on day 0, week 1, and week 4. For analysis, cases were divided into three groups; Group 1 - CMC, Group 2 - PEG/PG, and Group 3 - HPMC. RESULTS: Overall, 120 patients were included in the study. Demographic data and baseline characteristics were comparable among the groups. Group 2 had significant improvement in percentage change in OSDI (weeks 0-1, 0-4, and 1-4, = 0.00), TBUT (weeks 0-1, = 0.01; 0-4, = 0.006; and 1-4, = 0.007), and in ST (weeks 0-1, = 0.02; 0-4, = 0.002; and 1-4, = 0.008) compared to Group 1 at all follow-ups. Group 3 had improvements similar to Group 2, but it was not at all follow-ups (improvement in percentage change OSDI [weeks 0-1, 0-4, and 1-4, = 0.00], TBUT [weeks 0-1, = 0.10; 0-4, = 0.03; and 1-4, = 0.04], and in ST [weeks 0-1, = 0.007; 0-4, = 0.03; and 1-4, = 0.12]). No significant difference was found between Groups 2 and 3. CONCLUSIONS: Hydroxypropyl-guar containing PEG/PG and HPMC as tear substitutes are better than CMC. While HPMC was comparable to PEG/PG in subjective improvement, the objective improvement was not consistent.
[Mh] Termos MeSH primário: Carboximetilcelulose Sódica/administração & dosagem
Síndromes do Olho Seco/tratamento farmacológico
Derivados da Hipromelose/administração & dosagem
Lubrificantes Oftálmicos/administração & dosagem
Polissacarídeos/administração & dosagem
[Mh] Termos MeSH secundário: Administração Oftálmica
Adulto
Combinação de Medicamentos
Síndromes do Olho Seco/fisiopatologia
Feminino
Seres Humanos
Masculino
Meia-Idade
Soluções Oftálmicas
Polietilenoglicóis/química
Polissacarídeos/química
Propilenoglicol/química
Estudos Retrospectivos
Lágrimas/fisiologia
Resultado do Tratamento
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Drug Combinations); 0 (Lubricant Eye Drops); 0 (Ophthalmic Solutions); 0 (Polysaccharides); 0 (hydroxypropyl guar); 30IQX730WE (Polyethylene Glycols); 3NXW29V3WO (Hypromellose Derivatives); 6DC9Q167V3 (Propylene Glycol); B697894SGQ (polyethylene glycol 400); K679OBS311 (Carboxymethylcellulose Sodium)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180223
[Lr] Data última revisão:
180223
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180210
[St] Status:MEDLINE
[do] DOI:10.4103/meajo.MEAJO_165_15


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[PMID]:29304068
[Au] Autor:Drake AC; Lee Y; Burgess EM; Karlsson JOM; Eroglu A; Higgins AZ
[Ad] Endereço:School of Chemical, Biological and Environmental Engineering, Oregon State University, Corvallis, Oregon, United States of America.
[Ti] Título:Effect of water content on the glass transition temperature of mixtures of sugars, polymers, and penetrating cryoprotectants in physiological buffer.
[So] Source:PLoS One;13(1):e0190713, 2018.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Long-term storage of viable mammalian cells is important for applications ranging from in vitro fertilization to cell therapy. Cryopreservation is currently the most common approach, but storage in liquid nitrogen is relatively costly and the requirement for low temperatures during shipping is inconvenient. Desiccation is an alternative strategy with the potential to enable viable cell preservation at more convenient storage temperatures without the need for liquid nitrogen. To achieve stability during storage in the dried state it is necessary to remove enough water that the remaining matrix forms a non-crystalline glassy solid. Thus, the glass transition temperature is a key parameter for design of cell desiccation procedures. In this study, we have investigated the effects of moisture content on the glass transition temperature (Tg) of mixtures of sugars (trehalose or raffinose), polymers (polyvinylpyrrolidone or Ficoll), penetrating cryoprotectants (ethylene glycol, propylene glycol, or dimethyl sulfoxide), and phosphate buffered saline (PBS) solutes. Aqueous solutions were dried to different moisture contents by equilibration with saturated salt solutions, or by baking at 95°C. The glass transition temperatures of the dehydrated samples were then measured by differential scanning calorimetry. As expected, Tg increased with decreasing moisture content. For example, in a desiccation medium containing 0.1 M trehalose in PBS, Tg ranged from about 360 K for a completely dry sample to about 220 K at a water mass fraction of 0.4. Addition of polymers to the solutions increased Tg, while addition of penetrating cryoprotectants decreased Tg. Our results provide insight into the relationship between relative humidity, moisture content and glass transition temperature for cell desiccation solutions containing sugars, polymers and penetrating cryoprotectants.
[Mh] Termos MeSH primário: Crioprotetores/química
Polímeros/química
Açúcares/química
Temperatura de Transição
Água/química
[Mh] Termos MeSH secundário: Tampões (Química)
Varredura Diferencial de Calorimetria
Criopreservação/métodos
Dessecação/métodos
Dimetil Sulfóxido/química
Etilenoglicol/química
Ficoll/química
Vidro/química
Modelos Teóricos
Povidona/química
Propilenoglicol/química
Rafinose/química
Soluções/química
Trealose/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL
[Nm] Nome de substância:
0 (Buffers); 0 (Cryoprotective Agents); 0 (Polymers); 0 (Solutions); 0 (Sugars); 059QF0KO0R (Water); 25702-74-3 (Ficoll); 6DC9Q167V3 (Propylene Glycol); B8WCK70T7I (Trehalose); FC72KVT52F (Ethylene Glycol); FZ989GH94E (Povidone); N5O3QU595M (Raffinose); YOW8V9698H (Dimethyl Sulfoxide)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180205
[Lr] Data última revisão:
180205
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180106
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0190713


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[PMID]:28957438
[Au] Autor:Kennedy AE; Kandalam S; Olivares-Navarrete R; Dickinson AJG
[Ad] Endereço:Virginia Commonwealth University, Department of Biology, Richmond, VA, United States of America.
[Ti] Título:E-cigarette aerosol exposure can cause craniofacial defects in Xenopus laevis embryos and mammalian neural crest cells.
[So] Source:PLoS One;12(9):e0185729, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Since electronic cigarette (ECIG) introduction to American markets in 2007, vaping has surged in popularity. Many, including women of reproductive age, also believe that ECIG use is safer than traditional tobacco cigarettes and is not hazardous when pregnant. However, there are few studies investigating the effects of ECIG exposure on the developing embryo and nothing is known about potential effects on craniofacial development. Therefore, we have tested the effects of several aerosolized e-cigarette liquids (e-cigAM) in an in vivo craniofacial model, Xenopus laevis, as well as a mammalian neural crest cell line. Results demonstrate that e-cigAM exposure during embryonic development induces a variety of defects, including median facial clefts and midface hypoplasia in two of e-cigAMs tested e-cigAMs. Detailed quantitative analyses of the facial morphology revealed that nicotine is not the main factor in inducing craniofacial defects, but can exacerbate the effects of the other e-liquid components. Additionally, while two different e-cigAMs can have very similar consequences on facial appearances, there are subtle differences that could be due to the differences in e-cigAM components. Further assessment of embryos exposed to these particular e-cigAMs revealed cranial cartilage and muscle defects and a reduction in the blood supply to the face. Finally, the expression of markers for vascular and cartilage differentiation was reduced in a mammalian neural crest cell line corroborating the in vivo effects. Our work is the first to show that ECIG use could pose a potential hazard to the developing embryo and cause craniofacial birth defects. This emphasizes the need for more testing and regulation of this new popular product.
[Mh] Termos MeSH primário: Aerossóis/toxicidade
Anormalidades Craniofaciais/induzido quimicamente
Sistemas Eletrônicos de Liberação de Nicotina
Crista Neural/efeitos dos fármacos
Xenopus laevis/embriologia
[Mh] Termos MeSH secundário: Animais
Regulação da Expressão Gênica no Desenvolvimento/efeitos dos fármacos
Glicerol/toxicidade
Mamíferos
Crista Neural/citologia
Nicotina/toxicidade
Propilenoglicol/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Aerosols); 6DC9Q167V3 (Propylene Glycol); 6M3C89ZY6R (Nicotine); PDC6A3C0OX (Glycerol)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170929
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0185729


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[PMID]:28719877
[Au] Autor:Guan M; Zhang X
[Ad] Endereço:State Key Laboratory of Pollution Control & Resource Reuse, School of the Environment, Nanjing University, Nanjing, 210023, PR China.
[Ti] Título:Functional genomic assessment of 2, 2-bis (bromomethyl)-1, 3-propanediol induced cytotoxicity in a single-gene knockout library of E. coli.
[So] Source:Chemosphere;185:582-588, 2017 Oct.
[Is] ISSN:1879-1298
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Functional gene fingerprinting of chemicals could be used to understand the direct gene-chemical interaction in the process of toxification from a genome-wide scale. 2, 2-bis (bromomethyl)-1, 3-propanediol (BMP) is a brominated flame retardant with widespread production but with very limited toxicological data. Here the cytotoxicity of BMP was assessed by Escherichia coli (E. coli) functional genome-wide knockout mutants screening and the underlying molecular mechanism was investigated. The median inhibition concentration (IC50) of BMP was 1.608 ± 0.078 mg/ml after 24 h exposure. 119 initial, including 66 sensitive and 53 resistant single gene mutants, were identified by a full library screening of BMP at the concentration of IC50. The resistant genes were significantly enriched in nucleobase-containing compound biosynthetic process (GO: 0034654) by gene ontology (GO) biological process analyses, which suggested that the pathway of DNA repair is a critical cellular process in the survival of cells exposed to BMP. Meanwhile, function annotation of all BMP responsive genes suggested the mechanism of BMP was associated with DNA damage, oxidative stress and cellular transmembrane transport process. Many genes were exclusively responsive to BMP comparing with other chemicals that has been assessed by E. coli mutant screening approach, which indicated that BMP has a distinct mode of toxic action. Overall, the functional genomic screening approach presented here provides a great tool to assess the cellular toxicological mechanism of environmental chemicals.
[Mh] Termos MeSH primário: Escherichia coli/efeitos dos fármacos
Retardadores de Chama/toxicidade
Propilenoglicóis/toxicidade
[Mh] Termos MeSH secundário: Dano ao DNA
Escherichia coli/genética
Técnicas de Inativação de Genes
Genômica
Estresse Oxidativo
Propilenoglicol
Testes de Toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Flame Retardants); 0 (Propylene Glycols); 3296-90-0 (2,2-bis(bromomethyl)-1,3-propanediol); 6DC9Q167V3 (Propylene Glycol)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171017
[Lr] Data última revisão:
171017
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170719
[St] Status:MEDLINE


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[PMID]:28678965
[Au] Autor:Valentim D; Bueno CRE; Marques VAS; Vasques AMV; Cury MTS; Cintra LTA; Dezan E
[Ad] Endereço:Centro Universitário do Distrito Federal - UDF, School of Dentistry, Department of Endodontics, Brasilia, DF, Brazil.
[Ti] Título:Calcium hydroxide associated with a new vehicle: Psidium cattleianum leaf extracts. Tissue response evaluation.
[So] Source:Braz Oral Res;31:e43, 2017 Jul 03.
[Is] ISSN:1807-3107
[Cp] País de publicação:Brazil
[La] Idioma:eng
[Ab] Resumo:The aim of this study was to evaluate edemogenic activity and subcutaneous inflammatory reaction induced by Psidium cattleianum leaf extracts associated with Ca(OH)2. Thirty male Wistar rats, split equally into three groups [aqueous extract + Ca(OH)2; ethanolic extract + Ca(OH)2; and propylene glycol + Ca(OH)2], were assessed every 3 h or 6 h (five animals in each period). Under general anesthesia, 0.2 mL of 1% Evans blue per 100 g of body weight was injected into the penile vein and each combination to be evaluated was subcutaneously injected into the dorsal region 30 min thereafter. Edemogenic activity was analyzed by spectrophotometry (λ=630 nm). For inflammatory reaction analysis, 50 rats received four polyethylene tubes (three experimental groups) and an empty tube (control group). The assessments were made at 7, 15, 30, 60, and 90 days, followed by hematoxylin-eosin staining and by the assignment of scores for evaluation of tissue response intensity. Ethanolic extract + Ca(OH)2 yielded the largest edemogenic activity at 3 h. Intergroup differences at 6 h were not significant. The histological analysis showed progressive repair over time (p<0.05) and aqueous and ethanolic extracts produced similar responses to those of the control and Ca(OH)2 + propylene glycol groups. Psidium cattleianum leaf extracts used as Ca(OH)2 vehicles evoked similar tissue response when compared to Ca(OH)2 associated with propylene glycol.
[Mh] Termos MeSH primário: Hidróxido de Cálcio/farmacologia
Extratos Vegetais/farmacologia
Psidium/química
Tela Subcutânea/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Anti-Infecciosos/farmacologia
Portadores de Fármacos
Avaliação Pré-Clínica de Medicamentos
Etanol/farmacologia
Inflamação/tratamento farmacológico
Inflamação/patologia
Masculino
Teste de Materiais
Veículos Farmacêuticos/química
Veículos Farmacêuticos/farmacologia
Folhas de Planta/química
Propilenoglicol/farmacologia
Ratos Wistar
Reprodutibilidade dos Testes
Tela Subcutânea/patologia
Fatores de Tempo
Água/química
[Pt] Tipo de publicação:EVALUATION STUDIES; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Infective Agents); 0 (Drug Carriers); 0 (Pharmaceutical Vehicles); 0 (Plant Extracts); 059QF0KO0R (Water); 3K9958V90M (Ethanol); 6DC9Q167V3 (Propylene Glycol); PF5DZW74VN (Calcium Hydroxide)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170822
[Lr] Data última revisão:
170822
[Sb] Subgrupo de revista:D; IM
[Da] Data de entrada para processamento:170706
[St] Status:MEDLINE


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[PMID]:28609737
[Au] Autor:Lv T; Carvalho PN; Casas ME; Bollmann UE; Arias CA; Brix H; Bester K
[Ad] Endereço:Department of Bioscience, Aarhus University, Aarhus 8000C, Denmark. Electronic address: lvtao@bios.au.dk.
[Ti] Título:Enantioselective uptake, translocation and degradation of the chiral pesticides tebuconazole and imazalil by Phragmites australis.
[So] Source:Environ Pollut;229:362-370, 2017 Oct.
[Is] ISSN:1873-6424
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Phytoremediation of realistic environmental concentrations (10 µg L ) of the chiral pesticides tebuconazole and imazalil by Phragmites australis was investigated. This study focussed on removal dynamics, enantioselective mechanisms and transformation products (TPs) in both hydroponic growth solutions and plant tissues. For the first time, we documented uptake, translocation and metabolisation of these pesticides inside wetland plants, using enantioselective analysis. Tebuconazole and imazalil removal efficiencies from water reached 96.1% and 99.8%, respectively, by the end of the experiment (day 24). Removal from the solutions could be described by first-order removal kinetics with removal rate constants of 0.14 d for tebuconazole and 0.31 d for imazalil. Removal of the pesticides from the hydroponic solution, plant uptake, within plant translocation and degradation occurred simultaneously. Tebuconazole and imazalil concentrations inside Phragmites peaked at day 10 and 5d, respectively, and decreased thereafter. TPs of tebuconazole i.e., (5-(4-Chlorophenyl)-2,2-dimethyl-3-(1H-1,2,4-triazol-1-ylmethyl)-1,3-pentanediol and 5-(3-((1H-1,2,4-Triazol-1-yl)methyl)-3-hydroxy-4,4-dimethylpentyl)-2-chlorophenol) were quantified in solution, while the imazalil TPs (α-(2,4-Dichlorophenyl)-1H-imidazole-1-ethanol and 3-[1-(2,4-Dichlorophenyl)-2-(1H-imidazol-1-yl)ethoxy]-1,2-propanediol) were quantified in both solution and plant tissue. Pesticide uptake by Phragmites was positively correlated with evapotranspiration. Pesticide removal from the hydroponic solution was not enantioselective. However, tebuconazole was degraded enantioselectively both in the roots and shoots. Imazalil translocation and degradation inside Phragmites were also enantioselective: R-imazalil translocated faster than S-imazalil.
[Mh] Termos MeSH primário: Imidazóis/metabolismo
Praguicidas/metabolismo
Poaceae/metabolismo
Triazóis/metabolismo
[Mh] Termos MeSH secundário: Biodegradação Ambiental
Clorofenóis
Hidroponia
Imidazóis/química
Praguicidas/química
Raízes de Plantas/metabolismo
Propilenoglicol/metabolismo
Triazóis/química
Zonas Úmidas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Chlorophenols); 0 (Imidazoles); 0 (Pesticides); 0 (Triazoles); 401ATW8TRW (tebuconazole); 6DC9Q167V3 (Propylene Glycol); 6K0NOF3XQ6 (enilconazole); 7GBN705NH1 (imidazole); K9KAV4K6BN (2-chlorophenol)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171103
[Lr] Data última revisão:
171103
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170614
[St] Status:MEDLINE


  8 / 1605 MEDLINE  
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[PMID]:28589736
[Au] Autor:Zupancic O; Rohrer J; Thanh Lam H; Grießinger JA; Bernkop-Schnürch A
[Ad] Endereço:a Department of Pharmaceutical Technology, Institute of Pharmacy , Leopold-Franzens-University Innsbruck , Innsbruck , Austria.
[Ti] Título:Development and in vitro characterization of self-emulsifying drug delivery system (SEDDS) for oral opioid peptide delivery.
[So] Source:Drug Dev Ind Pharm;43(10):1694-1702, 2017 Oct.
[Is] ISSN:1520-5762
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:AIM: In this study, self-emulsifying drug delivery system (SEDDS) for oral delivery of opioid peptide dalargin were developed and characterized in vitro. METHODS: Dalargin lipophilicity was increased by O-esterification of tyrosine OH group, hydrophobic ion pairing, or a combination thereof. Distribution coefficients (log D) of lipidized dalargin derivatives were determined. Then, dalargin was incorporated in chosen SEDDS, namely SEDDS-1, composed of 50% Capmul 907, 40% Cremophor EL, and 10% propylene glycol and comparatively more lipophilic SEDDS-2 composed of 30% Captex 8000, 30% Capmul MCM, 30% Cremophor EL, and 10% propylene glycol. Additionally, SEDDS were characterized regarding droplet size, polydispersity index (PDI), cloudy point, physical stability and stability against pancreatic lipase. Furthermore, mucus permeating properties of SEDDS and their ability to protect the incorporated dalargin against proteolysis by trypsin, α-chymotrypsin, elastase, simulated gastric fluid (SGF), and simulated intestinal fluid (SIF) were evaluated. RESULTS: The highest dalargin drug payload of 4.57% in SEDDS-2 was achieved when dalargin palmitate (pDAL) was ion paired with sodium dodecyl sulfate (SDS) in molar ratio 1:1. Moreover, SEDDS-1 and SEDDS-2 had a narrow droplet size distribution with average droplet sizes of 42.1 and 33.1 nm with PDI of 0.042 and 0.034, respectively. Lipolysis study showed that within 30 min 78.5% of SEDDS-1 and 92.1% of SEDDS-2 were digested. In addition, both SEDDS exhibited mucus permeating properties as well as a protective effect against enzymatic degradation by trypsin, α-chymotrypsin, elastase, SGF and SIF. CONCLUSION: The results of this study suggest that the developed SEDDS could be considered for oral opioid peptide delivery.
[Mh] Termos MeSH primário: Caprilatos/química
Quimotripsina/química
Sistemas de Liberação de Medicamentos/métodos
Emulsões/química
Glicerídeos/química
Lipídeos/química
Muco/química
Peptídeos Opioides/química
Polietilenoglicóis/química
Propilenoglicol/química
[Mh] Termos MeSH secundário: Administração Oral
Disponibilidade Biológica
Peptídeos Opioides/administração & dosagem
Peptídeos Opioides/farmacologia
Solubilidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Caprylates); 0 (Emulsions); 0 (Glycerides); 0 (Lipids); 0 (Opioid Peptides); 30IQX730WE (Polyethylene Glycols); 39279-69-1 (cremophor); 6DC9Q167V3 (Propylene Glycol); EC 3.4.21.1 (Chymotrypsin); EC 3.4.21.1 (alpha-chymotrypsin); VFU0OU98LO (monooctanoin)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171020
[Lr] Data última revisão:
171020
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170608
[St] Status:MEDLINE
[do] DOI:10.1080/03639045.2017.1338722


  9 / 1605 MEDLINE  
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[PMID]:28475631
[Au] Autor:Jakobson CM; Tullman-Ercek D; Slininger MF; Mangan NM
[Ad] Endereço:Department of Chemical and Biological Engineering, Northwestern University, Evanston, IL, USA.
[Ti] Título:A systems-level model reveals that 1,2-Propanediol utilization microcompartments enhance pathway flux through intermediate sequestration.
[So] Source:PLoS Comput Biol;13(5):e1005525, 2017 May.
[Is] ISSN:1553-7358
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The spatial organization of metabolism is common to all domains of life. Enteric and other bacteria use subcellular organelles known as bacterial microcompartments to spatially organize the metabolism of pathogenicity-relevant carbon sources, such as 1,2-propanediol. The organelles are thought to sequester a private cofactor pool, minimize the effects of toxic intermediates, and enhance flux through the encapsulated metabolic pathways. We develop a mathematical model of the function of the 1,2-propanediol utilization microcompartment of Salmonella enterica and use it to analyze the function of the microcompartment organelles in detail. Our model makes accurate estimates of doubling times based on an optimized compartment shell permeability determined by maximizing metabolic flux in the model. The compartments function primarily to decouple cytosolic intermediate concentrations from the concentrations in the microcompartment, allowing significant enhancement in pathway flux by the generation of large concentration gradients across the microcompartment shell. We find that selective permeability of the microcompartment shell is not absolutely necessary, but is often beneficial in establishing this intermediate-trapping function. Our findings also implicate active transport of the 1,2-propanediol substrate under conditions of low external substrate concentration, and we present a mathematical bound, in terms of external 1,2-propanediol substrate concentration and diffusive rates, on when active transport of the substrate is advantageous. By allowing us to predict experimentally inaccessible aspects of microcompartment function, such as intra-microcompartment metabolite concentrations, our model presents avenues for future research and underscores the importance of carefully considering changes in external metabolite concentrations and other conditions during batch cultures. Our results also suggest that the encapsulation of heterologous pathways in bacterial microcompartments might yield significant benefits for pathway flux, as well as for toxicity mitigation.
[Mh] Termos MeSH primário: Microambiente Celular/fisiologia
Espaço Intracelular/metabolismo
Redes e Vias Metabólicas/fisiologia
Modelos Biológicos
Propilenoglicol/metabolismo
[Mh] Termos MeSH secundário: Salmonella enterica/metabolismo
Biologia de Sistemas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
6DC9Q167V3 (Propylene Glycol)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170627
[Lr] Data última revisão:
170627
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170506
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pcbi.1005525


  10 / 1605 MEDLINE  
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[PMID]:28344173
[Au] Autor:Liu KS; Huang TH; Aljuffali IA; Chen EL; Wang JJ; Fang JY
[Ad] Endereço:Department of Pharmacy, Chia Nan University of Pharmacy and Science, Tainan, Taiwan.
[Ti] Título:Exploring the structure-permeation relationship of topical tricyclic antidepressants used for skin analgesia.
[So] Source:Int J Pharm;523(1):386-397, 2017 May 15.
[Is] ISSN:1873-3476
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The purpose of this study was to evaluate the skin permeation of tricyclic antidepressants (TCAs) with propamine moiety to select candidates for the development of topical analgesics to treat cutaneous pain. We sought to establish the structure-permeation relationship (SPR) of topical TCAs. The lipophilicity, melting point, and aqueous solubility were determined to develop the physicochemical characterization. The TCA permeation into pig and nude mouse skins was estimated using Franz diffusion cell. TCAs and lidocaine were comparatively examined for cutaneous analgesia by pinprick assay. Cutaneous tolerance to TCAs was assessed using nude mouse skin. The skin deposition increased following the increase of lipophilicity after excluding the effect of solubility, with clomipramine exhibiting the highest skin retention. A contrary result was observed for TCA penetration into the receptor. Of the permeants tested, clomipramine demonstrated the best skin-targeting ability. Nortriptyline and clomipramine demonstrated selective uptake into the hair follicles, exhibiting a 2.5-fold higher follicular accumulation than desipramine. Replacement of nitrogen with carbon in the seven-member ring increased skin absorption. The tertiary amine TCAs demonstrated higher absorption than the secondary amine TCAs. The position of the double bond also affected skin transport. Topical clomipramine had a longer duration of analgesic action than lidocaine (240min versus 60min). Exploring the SPR revealed that clomipramine could be an analgesic candidate drug for future development.
[Mh] Termos MeSH primário: Analgésicos
Antidepressivos Tricíclicos
Neuralgia/tratamento farmacológico
Absorção Cutânea
[Mh] Termos MeSH secundário: 1-Octanol/química
Administração Cutânea
Analgesia
Analgésicos/administração & dosagem
Analgésicos/química
Analgésicos/farmacocinética
Analgésicos/uso terapêutico
Animais
Antidepressivos Tricíclicos/administração & dosagem
Antidepressivos Tricíclicos/química
Antidepressivos Tricíclicos/farmacocinética
Antidepressivos Tricíclicos/uso terapêutico
Técnicas In Vitro
Camundongos Nus
Simulação de Acoplamento Molecular
Estrutura Molecular
Propilenoglicol/química
Pele/metabolismo
Suínos
Água/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Analgesics); 0 (Antidepressive Agents, Tricyclic); 059QF0KO0R (Water); 6DC9Q167V3 (Propylene Glycol); NV1779205D (1-Octanol)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170807
[Lr] Data última revisão:
170807
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170328
[St] Status:MEDLINE



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