932 resultados para HP-polymeeri


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Hydroxymethylnitrofurazone (NFOH) is a prodrug that is active against Trypanosoma cruzi. It however presents low solubility and high toxicity. Hydroxypropyl-beta-cyclodextrin (HP-beta-CD) can be used as a drug-delivery system for NFOH modifying its physico-chemical properties. The aim of this work is to characterize the inclusion complex between NFOH and HP-beta-CD. The rate of NFOH release decreases after complexation and thermodynamic parameters from the solubility isotherm studies revealed that a stable complex is formed (deltaGº= 1.7 kJ/mol). This study focuses on the physico-chemical characterization of a drug-delivery formulation that comes out as a potentially new therapeutic option for Chagas disease treatment.

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Ropivacaine (RVC) is an enantiomerically pure local anesthetic (LA) largely used in surgical procedures, which presents physico-chemical and therapeutic properties similar to those of bupivacaine (BPV), but associated to less systemic toxicity This study focuses on the development and pharmacological evaluation of a RVC in 2-hydroxypropyl-beta-cyclodextrin (HP-P-CD) inclusion complex. Phase-solubility diagrams allowed the determination of the association constant between RVC and HP-beta-CD (9.46 M-1) and showed an increase on RVC solubility upon complexation. Release kinetics revealed a decrease on RVC release rate and reduced hemolytic effects after complexation. (onset at 3.7 mM and 11.2 mM for RVC and RVCHP-beta-CD, respectively) were observed. Differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and X-ray analysis (X-ray) showed the formation and the morphology of the complex. Nuclear magnetic resonance (NMR) and job-plot experiments afforded data regarding inclusion complex stoichiometry (1:1) and topology. Sciatic nerve blockade studies showed that RVCHP-beta-CD was able to reduce the latency without increasing the duration of motor blockade, but prolonging the duration and intensity of the sensory blockade (p < 0.001) induced by the LA in mice. These results identify the RVCHP-beta-CD complex as an effective novel approach to enhance the pharmacological effects of RVC, presenting it as a promising new anesthetic formulation. (c) 2007 Elsevier B.V All rights reserved.

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Objectives To investigate the molecular interaction between beta-cyclodextrin (beta CD) or hydroxypropyl-beta-cyclodextrin (HP beta CD) and riboflavin (RF), and to test the anticancer potential of these formulations. Methods The physicochemical characterization of the association between RF and CDs was performed by UV-vis absorption, fluorescence, differential scanning calorimetry and NMR techniques. Molecular dynamics simulation was used to shed light on the mechanism of interaction of RF and CDs. Additionally, in-vitro cell culture tests were performed to evaluate the cytotoxicity of the RFCD complexes against prostate cancer cells. Key findings Neither beta CD nor HP beta CD led to substantial changes in the physicochemical properties of RF (with the exception of solubility). Additionally, rotating frame Overhauser effect spectroscopy experiments detected no spatial correlations between hydrogens from the internal cavity of CDs and RF, while molecular dynamics simulations revealed out-of-ring RFCD interactions. Notwithstanding, both RF beta CD and RFHP beta CD complexes were cytotoxic to PC3 prostate cancer cells. Conclusions The interaction between RF and either beta CD or HP beta CD, at low concentrations, seems to be made through hydrogen bonding between the flavonoid and the external rim of both CDs. Regardless of the mechanism of complexation, our findings indicate that RFCD complexes significantly increase RF solubility and potentiate its antitumour effect.

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The interaction of 4-nerolidylcatechol (4-NRC), a potent antioxidant agent, and 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CD) was investigated by the solubility method using Fourier transform infrared (FTIR) methods in addition to UV-Vis, (1)H-nuclear magnetic resonance (NMR) spectroscopy and molecular modeling. The inclusion complexes were prepared using grinding, kneading and freeze-drying methods. According to phase solubility studies in water a B(S)-type diagram was found, displaying a stoichiometry complexation of 2:1 (drug:host) and stability constant of 6494 +/- A 837 M(-1). Stoichiometry was established by the UV spectrophotometer using Job's plot method and, also confirmed by molecular modeling. Data from (1)H-NMR, and FTIR, experiments also provided formation evidence of an inclusion complex between 4-NRC and HP-beta-CD. 4-NRC complexation indeed led to higher drug solubility and stability which could probably be useful to improve its biological properties and make it available to oral administration and topical formulations.

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Background: The increased prevalence of foot and ankle pathologies in Rheumatic and Musculoskeletal diseases (RMDs) is well documented1, however the provision of foot & ankle (F&A) healthcare services for people with RMDs in Europe has not been evaluated. Objectives: To assess the current healthcare systems for providing foot & ankle healthcare services for people with RMDs in Europe. Methods: A survey was undertaken to evaluate current provision of F&A health care services for people with RMDs across Europe. A questionnaire was distributed to all 22 country presidents representing HP associations within EULAR. The questionnaire used was developed and piloted (in 7 countries) by the EULAR F&A Study Group, and structured to capture the provision and type of F&A services for people with RMDs. When the HP presidents felt unable to answer specific questions they were encouraged to consult a colleague who may be better placed to provide the answers. Results: Sixteen questionnaires were completed (Norway, Ireland, Sweden, Hungary, Netherlands, UK, Denmark, Portugal, Italy, Switzerland, Austria, France, Czech Republic, Spain, Belgium, Malta). Of the 16, 13 respondents indicated provision of F&A health care services in their country, but only three countries had services specialising in RMD-related F&A problems (Netherlands, UK, Malta). The professions providing the care for patients with RMD-related F&A problems were different depending on the pathology and the country (Table1). Podiatrists provided care for F&A pain and deformity problems in 11 countries, but provided F&A ulcer care in only 8 countriesConclusions: Only 3 countries have F&A health care services specialised to the needs of people with RMDs. The professions providing the care varied between countries, and also depended on the F&A pathology. Interestingly, F&A healthcare services were provided by professions that do not solely specialised in F&A care. Further research is needed to assess the variation of F&A healthcare services between and within European countries and the impact on healthcare of various F&A healthcare service designs. References: Woodburn, J. & Helliwell, P. Foot problems in rheumatology. Rheumatology 36, 932-934 (1997).

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OBJETIVOS: Avaliar a prevalência de problemas músculo-esqueléticos (PM-E) em atletas praticantes de Hóquei em Patins (HP); comparar e correlacionar o estado de saúde (ES), o grau de dificuldade sentida no desempenho do HP e a intensidade da dor com os PM-E; estimar as diferentes contribuições dos PM-E para a variação no ES, grau de dificuldade sentida no desempenho do HP e a intensidade da dor. MATERIAIS E MÉTODOS: Foram inquiridos 289 atletas, a competir nos campeonatos nacionais e locais de HP em Portugal na época 2011/2012. Foi registada a prevalência de PM-E e o seu impacto no ES dos atletas nos últimos 12 meses. Todos os participantes responderam a um Questionário de PM-E relativo a 10 regiões anatómicas e ao Short Form-36 Health Survey Questionnaire. RESULTADOS: As áreas com maior prevalência de PM-E são o punho/mãos (31.1%), ancas/coxas (24.6%) e região lombar (24.2%). Grande parte dos atletas que reportaram problemas, apesar de experienciarem dor e limitação durante a sua participação, não interromperam a prática desportiva. As queixas físicas são prevalentes entre os atletas que reportaram PM-E e, predominantemente, resultantes de lesões por sobrecarga. Os PM-E afetaram as subescalas mais relacionadas com a dimensão física da saúde (p ≤ 0.05), diminuíndo, na generalidade, o ES dos atletas. Esta diminuição foi acompanhada de um aumento da dificuldade sentida no desempenho do HP e da intensidade de dor. A análise de regressão múltipla stepwise revelou que os PM-E explicam 1.4% a 28% da variância dos resultados das subescalas do ES. Quanto ao grau médio de dificuldade no desempenho do HP, os PM-E explicam 27.1% da variância dos resultados, assim como, explicam 21.3% da variância dos resultados da intensidade média de dor. CONCLUSÃO: Os PM-E são prevalentes em atletas praticantes de HP e estão associados a um menor ES, a um aumento da dificuldade no desempenho do HP e uma maior intensidade de dor; estes explicam uma proporção moderada da variação no ES, grau de dificuldade sentida no desempenho do HP e intensidade de dor. A ocorrência de problemas ao longo da época, diminuíu o rendimento e a participação desportiva, estendendo-se, estas limitações, para além do terreno de jogo, interferindo com as atividades diárias dos atletas.

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A construção social do gênero feminino em Moçambique está baseada na submissão ao homem, influenciando a vulnerabilidade de gênero à infecção pelo HIV. Objetivou-se analisar a percepção de pessoas vivendo com HIV/aids (PVHA) e de profissionais de saúde (PS), da cidade de Maputo, em relação à vulnerabilidade de gênero e infecção pelo HIV. Participaram 33 PVHA e 15 PS, selecionados por conveniência, mediante a realização de grupos focais e de entrevistas semiestruturadas. Dois eixos temáticos nortearam a análise: vulnerabilidade de gênero e práticas culturais tradicionais. A análise de conteúdo dos relatos verbais permitiu concluir que a vulnerabilidade feminina é maior, segundo a quase totalidade dos participantes, delineando categorias como submissão da mulher, dificuldade para negociar o uso do preservativo e influência das práticas culturais. O estudo possibilitou compreender melhor o contexto de vulnerabilidades que afetam cidadãos de Maputo, em especial as mulheres, em um país de prevalência elevada da epidemia. ____________________________________________________________________________________ ABSTRACT

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This lecture course covers the theory of so-called duality-based a posteriori error estimation of DG finite element methods. In particular, we formulate consistent and adjoint consistent DG methods for the numerical approximation of both the compressible Euler and Navier-Stokes equations; in the latter case, the viscous terms are discretized based on employing an interior penalty method. By exploiting a duality argument, adjoint-based a posteriori error indicators will be established. Moreover, application of these computable bounds within automatic adaptive finite element algorithms will be developed. Here, a variety of isotropic and anisotropic adaptive strategies, as well as $hp$-mesh refinement will be investigated.

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We shall consider the weak formulation of a linear elliptic model problem with discontinuous Dirichlet boundary conditions. Since such problems are typically not well-defined in the standard H^1-H^1 setting, we will introduce a suitable saddle point formulation in terms of weighted Sobolev spaces. Furthermore, we will discuss the numerical solution of such problems. Specifically, we employ an hp-discontinuous Galerkin method and derive an L^2-norm a posteriori error estimate. Numerical experiments demonstrate the effectiveness of the proposed error indicator in both the h- and hp-version setting. Indeed, in the latter case exponential convergence of the error is attained as the mesh is adaptively refined.

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Aim: To evaluate the effect of different in-office bleaching agents on the permeability, roughness and surface microhardness of human enamel. Methods: For evaluation of roughness and microhardness, 40 hemi-faces of 20 premolars were subjected to initial roughness (Ra parameter) and microhardness (VHN) measurements. Thirty-two premolar’s crowns were used for permeability test. Then, all specimens were randomly divided into four groups: C - without bleaching (control), HP35 - bleaching with 35% hydrogen peroxide (HP), HPF38 - 38% HP+fluoride, HPC35 - 35% HP+calcium. Final roughness (FR) and microhardness (FM) measurements were evaluated. For permeability, the 32 crowns were immersed in 1% sodium hypochlorite (20 min) and silver nitrate solutions (2 h) and subjected to developing solution under fluorescent light (16 h). Three sections from the crowns were analyzed in light microscope (100x) to evaluate the scores of permeability: Score 0 - no tracer agent penetration; Score 1 - less than half the thickness of enamel penetration; Score 2 - tracer agent reaching half the enamel thickness; Score 3 - entire enamel depth penetration, without reaching dentin and Score 4 - tracer agent reaching dentin. For roughness and microhardness evaluation were used one-way ANOVA and Dunnet post-test for independent samples, and t test for paired samples. For permeability, the data were analyzed by Kruskal Wallis and Dunn tests. Results: A significantly higher permeability and surface roughness were observed in groups HP35, HPF38 and HPC35 compared to the C group, as well as decreased microhardness (p<0.05). Conclusions: All bleaching agents increased permeability and surface roughness, and decreased microhardness of human enamel; thus, the addition of fluoride or calcium was not beneficial.

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Background: Harpalycin 2 (HP-2) is an isoflavone isolated from the leaves of Harpalyce brasiliana Benth., a snakeroot found in northeast region of Brazil and used in folk medicine to treat snakebite. Its leaves are said to be anti-inflammatory. Secretory phospholipases A(2) are important toxins found in snake venom and are structurally related to those found in inflammatory conditions in mammals, as in arthritis and atherosclerosis, and for this reason can be valuable tools for searching new anti-phospholipase A(2) drugs.Methods: HP-2 and piratoxin-III (PrTX-III) were purified through chromatographic techniques. The effect of HP-2 in the enzymatic activity of PrTX-III was carried out using 4-nitro-3-octanoyloxy-benzoic acid as the substrate. PrTX-III induced platelet aggregation was inhibited by HP-2 when compared to aristolochic acid and p-bromophenacyl bromide (p-BPB). In an attempt to elucidate how HP-2 interacts with PrTX-III, mass spectrometry, circular dichroism and intrinsic fluorescence analysis were performed. Docking scores of the ligands (HP-2, aristolochic acid and p-BPB) using PrTX-III as target were also calculated.Results: HP-2 inhibited the enzymatic activity of PrTX-III (IC50 11.34 +/- 0.28 mu g/mL) although it did not form a stable chemical complex in the active site, since mass spectrometry measurements showed no difference between native (13,837.34 Da) and HP-2 treated PrTX-III (13,856.12 Da). A structural analysis of PrTX-III after treatment with HP-2 showed a decrease in dimerization and a slight protein unfolding. In the platelet aggregation assay, HP-2 previously incubated with PrTX-III inhibited the aggregation when compared with untreated protein. PrTX-III chemical treated with aristolochic acid and p-BPB, two standard PLA(2) inhibitors, showed low inhibitory effects when compared with the HP-2 treatment. Docking scores corroborated these results, showing higher affinity of HP-2 for the PrTX-III target (PDB code: 1GMZ) than aristolochic acid and p-BPB. HP-2 previous incubated with the platelets inhibits the aggregation induced by untreated PrTX-III as well as arachidonic acid.Conclusion: HP-2 changes the structure of PrTX-III, inhibiting the enzymatic activity of this enzyme. In addition, PrTX-III platelet aggregant activity was inhibited by treatment with HP-2, p-BPB and aristolochic acid, and these results were corroborated by docking scores.

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Background: Mutation analysis has identified a G-> A transition in the promoter region of TNF-alpha gene at position -308 (rs1800629). Objective: The aim of our study was to investigate the influence of polymorphism in -308 GA promoter variant of the TNF alpha gene on metabolic response and weight loss secondary to two hypocaloric diets. Method: A sample of 283 obese subjects was enrolled in a consecutive prospective way. In the basal visit, patients were randomly allocated during 9 months to diet HP (high protein/low carbohydrate hypocaloric diet) and diet S (standard hypocaloric diet). Results: There were no significant differences between the positive effects on weight loss in either genotype group with both diets. With both diets and only in wild genotype (diet HP vs. diet S), total cholesterol (-9.1 ± 3.4 mg/dL vs. -6.9 ± 2.0 mg/dL; p > 0.05), LDL cholesterol (-9.0 ± 2.9 mg/dL vs. -6.5 ± 2.1 mg/dL; p > 0.05) and triglycerides (-23.1 ± 5.1 mg/dL vs. -12.3 ± 4.8 mg/dL; p < 0.05) decreased. The improvement in triglycerides was higher in subjects without A allele. With diet HP and only in wild genotype, insulin levels (-3.1 ± 1.8 UI/L; p < 0.05) and HOMA-R (-0.8 ± 0.1 units; p < 0.05) decreased. Conclusion: Carriers of -308 GG promoter variant of TNF-alpha gene have a better metabolic response than -308 GA obese with a high protein hypocaloric diet.

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Vegetation plays a fundamental role in soil conservation, so it is common to consider an increase in vegetation cover as one of the techniques to mitigate the effects of desertification in Mediterranean forest environments. There are two factors limiting the establishment and growth of seedlings in dry environments: (i) an excessive radiation and, (ii) the limited availability of water during the summer drought. During an afforestation plan, soil preparation is always necessary to reduce sapling mortality. The goal of this study was to analyze the effect of various organic amendments on soil according to chemical and hydrological properties, and to assess the effects of these parameters on an afforestal proposal under Mediterranean climate conditions. Five amendments were applied in an experimental set of plots: straw mulching (SM); mulch with chipped branches of Aleppo Pine (PM); TerraCotten hydroabsobent polymers (HP); sewage sludge (RU); sheep manure (SH) and control (C). Plots were afforested following the same spatial pattern, and amendments were mixed with the soil at the rate 10 Mg ha -1 . Under bare soil conditions (C), most of mortalities occurred during the summer period of the first year. A substantial positive effect of SM, PM and HP on the survival rates have been clearly observed. Conversely, when the soil was amended with SH, the survival rate quickly decreased or remained more or less constant regarding to C. In this study, the lack of differences on chemical properties indicates that there may exist other reasons to justify the differences that were found in the pattern of vegetation. However, regarding to the hydrological properties some differences have been found. In C, soils were registered below the wilting point during 4 months a year, and therefore, in the area of water unusable by plants. These months were coinciding with the summer Mediterranean drought and can justify the high mortality found on plants. Conversely, in SM, PM and HP, soil moisture remained below the wilting point less period than C and, the plant available water was also higher. In these treatments, the survival sapling rates measured were the highest. SH showed water holding capacity slightly more limited than C. For this treatment, the survival sapling rates measured were the lowest. In conclusion, from a land management standpoint, the PM, SM and HP have been proved as a significant method to reduce sapling mortality rates during the Mediterranean summer drought.