Sistemas microemulsionados como carreador lipídico para fármacos insolúveis

Several pharmaceutical products have been developed in recent years aiming to enhance the treatment of diseases by increasing the effectiveness of drugs. Many of these new products are based on new drug delivery systems. Among these, microemulsions, which were first studied in 1943 by Hoar and Schulman, is of great interest. Microemulsion can be defined as a thermodynamically stable, isotropic, translucent and transparent system of two immiscible liquids stabilized by a surfactant film located in the oil / water interface. The aim os this work was the incorporation of Amphotericin B and Simvasatin to a microemulsion system and analyzes its physicochemical properties and their therapeutical activity when incorporated into this system. Some very promising results were achieved as the reduction of the toxicity and maintenance of the efficacy of the Amphotericin B incorpored into a microemulsion, which was demonstrated in the in vitro pharmacotoxicological study. As for the incorporation of Simvastatin in microemulsion, it was observed a significant improvement in the potential antiinflammatory and anti-infective properties when the system was use to treat infected wounds (simvastatin pleiotropic effects). Therefore, it can be concluded that the incorporation of these drugs into microemulsion system reveal the potential of microemulsions as a promising and novel dosage form, qualifying them for future trials in order to make them available in the pharmaceutical market

Alterações no metabolismo de zinco relacionadas ao envelhecimento

Although many studies point to alterations in the organic concentrations of zinc in elderly patients, the mechanisms by which aging might cause changes in the metabolism of this nutrient remain unclear. Thus, we assessed the changes in plasma zinc, Zinc Binding Capacity to Plasma Protein (ZnBCPP) and Saturation Index (SI), comparing elderly individuals and young adults. The zinc analyses were performed by atomic absorption spectrophotometry. A statistically significant difference (p < 0.001) was found between the two groups, in relation to plasma zinc and SI, but the ZnBCPP did not differ between the younger and older subjects. In agreement with this result, it was shown in the young group that 76% (R2 = 0.760) of the ZnBCPP variations are explained by the variations in plasma zinc and SI. In the elderly group this measure decreased to 30.5% (R2 = 0.305). We conclude, therefore, that aging may be a factor associated to changes in control mechanisms and in zinc homeostasis, and could even alter ZnBCPP response patterns and other zinc-related indicators of nutritional status.

Estado nutricional antropométrico, perfil lipídico e consumo alimentar como fatores de risco para doença cardiovascular em adolescentes

The dyslipidemia and excess weight in adolescents, when combined, suggest a progression of risk factors for cardiovascular disease (CVD). Besides these, the dietary habits and lifestyle have also been considered unsuitable impacting the development of chronic diseases. The study objectives were: (1) estimate the prevalence of lipid profile and correlate with body mass index (BMI), waist circumference (WC) and waist / height ratio (WHR) in adolescents, considering the maturation sexual, (2) know the sources of variance in the diet and the number of days needed to estimate the usual diet of adolescents and (3) describe the dietary patterns and lifestyle of adolescents, family history of CVD and age correlates them with the patterns of risk for CVD, adjusted for sexual maturation. A cross-sectional study was performed with 432 adolescents, aged 10-19 years from public schools of the Natal city, Brazil. The dyslipidemias were evaluated considering the lipid profile, the index of I Castelli (TC / HDL) and II (LDL / HDL) and non-HDL cholesterol. Anthropometric indicators were BMI, WC and WHR. The intake of energy, nutrients including fiber, fatty acids and cholesterol was estimated from two 24-hour recalls (24HR). The variables of lipid profile, anthropometric and clinical data were used in the models of Pearson correlation and linear regression, considering the sexual maturation. The variance ratio of the diet was calculated from the component-person variance, determined by analysis of variance (ANOVA). The definition of the number of days to estimate the usual intake of each nutrient was obtained by taking the hypothetical correlation (r) ≥ 0.9, between nutrient intake and the true observed. We used the principal component analysis as a method of extracting factors that 129 accounted for the dependent variables and known cardiovascular risk obtained from the lipid profile, the index for Castelli I and II, non-HDL cholesterol, BMI, and WC the WHR. Dietary patterns and lifestyle were obtained from the independent variables, based on nutrients consumed and physical activity weekly. In the study of principal component analysis (PCA) was investigated associations between the patterns of cardiovascular risk factors in dietary patterns and lifestyle, age and positive family history of CVD, through bivariate and multiple logistic regression adjusted for sexual maturation. The low HDL-C dyslipidemia was most prevalent (50.5%) for adolescents. Significant correlations were observed between hypercholesterolemia and positive family history of CVD (r = 0.19, p <0.01) and hypertriglyceridemia with BMI (r = 0.30, p <0.01), with the CC (r = 0.32, p <0.01) and WHR (r = 0.33, p <0.01). The linear model constructed with sexual maturation, age and BMI explained about 1 to 10.4% of the variation in the lipid profile. The sources of variance between individuals were greater for all nutrients in both sexes. The reasons for variances were  1 for all nutrients were higher in females. The results suggest that to assess the diet of adolescents with greater precision, 2 days would be enough to R24h consumption of energy, carbohydrates, fiber, saturated and monounsaturated fatty acids. In contrast, 3 days would be recommended for protein, lipid, polyunsaturated fatty acids and cholesterol. Two cardiovascular risk factors as have been extracted in the ACP, referring to the dependent variables: the standard lipid profile (HDL-C and non-HDL cholesterol) and "standard anthropometric index (BMI, WC, WHR) with a power explaining 75% of the variance of the original data. The factors are representative of two independent variables led to dietary patterns, "pattern 130 western diet" and "pattern protein diet", and one on the lifestyle, "pattern energy balance". Together, these patterns provide an explanation power of 67%. Made adjustment for sexual maturation in males remained significant variables: the associations between puberty and be pattern anthropometric indicator (OR = 3.32, CI 1.34 to 8.17%), and between family history of CVD and the pattern lipid profile (OR = 2.62, CI 1.20 to 5.72%). In females adolescents, associations were identified between age after the first stage of puberty with anthropometric pattern (OR = 3.59, CI 1.58 to 8.17%) and lipid profile (OR = 0.33, CI 0.15 to 0.75%). Conclusions: The low HDL-C was the most prevalent dyslipidemia independent of sex and nutritional status of adolescents. Hypercholesterolemia was influenced by family history of CVD and sexual maturation, in turn, hypertriglyceridemia was closely associated with anthropometric indicators. The variance between the diets was greater for all nutrients. This fact reflected in a variance ratio less than 1 and consequently in a lower number of days requerid to estimate the usual diet of adolescents considering gender. The two dietary patterns were extracted and the pattern considered unhealthy lifestyle as healthy. The associations were found between the patterns of CVD risk with age and family history of CVD in the studied adolescents

Análise do óxido nítrico, perfil lipídico, resistência arterial e capacidade funcional de idosas submetidas a um treinamento aquático

A prática regular de exercício físico possibilita redução dos efeitos das disfunções hormonais e envelhecimento biológico natural que promovem desajustes hemodinâmicos, vasculares e músculo-esqueléticos, principalmente na população feminina no período pós-menopausa. Nesta fase da vida, o exercício aquático representa mais do que uma forma de ajuste funcional, é uma forma de manutenção de independência para as atividades da vida diária (AVD s) e melhoria na qualidade de vida. Este estudo teve como objetivo avaliar as modificações adquiridas pela prática regular de um programa de exercício aquático concorrente de intensidade moderada no nível de óxido nítrico (ON), no índice de resistividade arterial (IR), no perfil lipídico, na capacidade funcional e na qualidade de vida de idosas. A amostra foi formada por idosas (60 a 80 anos) selecionadas por randomização, por sorteio simples divididas em grupo controle e grupo de intervenção as quais foram submetidas a um programa de exercícios aquáticos proposto inicialmente em projeto piloto, por 12 semanas (n=34) e o ensaio clínico teve duração de 16 semanas (n=40). Foi coletada amostra sanguínea das idosas e avaliado o perfil lipídico pelo método enzimático com kit Labtest e o ON por medida indireta a partir da concentração de nitrito no sobrenadante das células em cultura em leitor de ELISA. A avaliação das artérias carótidas e vertebrais foi feita utilizando o método de ultra-som Doopler. A capacidade funcional foi avaliada por quatro testes que simulam atividades da vida diária que são: caminhar 10 metros (C10m), levantar da posição sentada (LPS), levantar da cadeira e locomover-se pela casa (LCLC) e o de levantar-se da posição decúbito ventral (LPDV). No estudo piloto foi avaliado o índice geral de autonomia funcional (IG) e a qualidade de vida através do questionário WHOQOL-100. Empregou-se a análise de variância (ANOVA) com medidas repetidas nos fatores grupo (GH e GC) e tempo (pré e pós-teste) para as comparações intra e intergrupos nas variáveis seguida do post hoc de Scheffé. Utilizou-se o teste de correlação de Pearson e adotado o valor de p<0,05 para a significância estatística. Houve aumento do ON circulante, redução nos índices de resistividade arterial, melhoria significativa nos níveis de colesterol e triglicérides e ganho na capacidade funcional das idosas após a intervenção. Existiu correlação inversa entre a resistividade da artéria vertebral direita (VERTD) e níveis de ON e entre a VERTD e os níveis plasmáticos de HDL, assim como entre estes e o teste C10m nas idosas em estudo. Não houve modificações significativas na qualidade de vida das idosas. Em conclusão, o programa de exercício proposto foi capaz de oferecer melhorias funcionais, aumentar o nível de óxido nítrico circulante, diminuindo a resistência arterial promovendo modificações no perfil lipídico de idosas

Segurança e eficácia da tibolona na transição menopausal: um ensaio clínico randomizado, duplo-cego e controlado com placebo

Conselho Nacional de Desenvolvimento Científico e Tecnológico

Consequências da colectomia associada à hepatectomia no metabolismo hepático e na forma e função de hemácias em ratos

This study investigated the influence of partial colectomy associated with hepatectomy on the biodistribution of the 99mTc-phytate, on metabolic parameters, as well as labeling and morphology of red blood cells. Wistar rats were distributed into three groups (each with 6), nominated as colectomy, colectomy+hepatectomy and sham. In the 30th postoperative day all rats were injected with 99mTc-phytate 0.1mL i.v. (radioactivity 0.66 MBq). After 15 minutes, liver sample was harvested and weighed. Percentage radioactivity per gram of tissue (%ATI/g) was determined using an automatic gamma-counter. Serum AST, ALT, alkaline phosphatase and red blood cells labeling were determined. The liver %ATI/g and red blood cells labeling were lower in colectomy and colectomy+hepatectomy rats than in sham rats (p <0.05), and no difference was detected comparing the colectomy and colectomy+hepatectomy groups. Red blood cells morphology did not differ among groups. Serum levels of AST, ALT and alkaline fosfatase were significantly higher in colectomy+hepatectomy than in colectomy rats (p<0.001). Hepatectomy associated with colectomy lowered the uptake of radiopharmaceutical in liver and in red blood cells in rats, coinciding with changes in liver enzymatic activity

Medidas antropométricas e avaliação do perfil lipídico de indivíduos obesos e com sobrepeso residentes no Estado do RN

Overweight and obesity are defined as abnormal or excessive fat accumulation that may impair health. Obesity significantly increases the risk of developing numerous medical conditions, besides is associated with shortened life span. The objective of this study was to evaluate the anthropometric measurements and lipid profile in adult overweight and obese subjects residents in the state of Rio Grande do Norte. The methodology was the analysis of certain biochemical parameters in serum of individuals and a physical evaluation that consisted of measurements of blood pressure and anthropometric data. In addition, the volunteers of the research answered a questionnaire about personal, social and clinical data. 1741 samples were collected, of which 432 (24,8%) were obese. Of these, 280 were selected to participate in the study, including 118 (42,1%) men and 162 (57,9%) women. Of the remaining 1309 individuals, 731 (55,8%) were overweight. Among them, 179 (24.5%) were analyzed in this study, with 56,4% female. Of the remaining 578 normal individuals, 143 were selected as controls in the research. Amid the obese, overweight and eutrophic, there were respectively 10% vs 5% vs 5,6% of diabetics, 92,1% vs 85,5% vs 68,7% of dyslipidemics and 38,6% vs 22,3% vs 15,6% of hypertensive patients. The degree of obesity presented by the participants was varied, with the majority (72,8%) fall into grade I obese, 22,9% (64) in grade II and only 4,3% (12) in grade III. Mean anthropometric participants showed statistically significant differences between groups eutrophic, overweight and obese on the BMI, WC, WHR and %BF and between sexes in CC, WHR and %BF. As the mean serum biochemical parameters to evaluate the lipid profile showed significant differences between groups eutrophic, overweight and obese, unless the exception of HDL among overweight and obese. The significance level was 5% (p <0.05)

Estudo de polimorfismos em genes relacionados ao metabolismo do ácido fólico e sua associação com o desenvolvimento de fendas orais não-sindrômicas

The congenital facial clefts are characterized by incomplete formation of the structures that separate the oral and nasal cavity. It is known that several environmental and genetic factors are involved in its development, among these, polymorphisms associated with folic acid metabolism have been investigated. In this sense, the objective was to observe the frequency of polymorphisms C677T and A1298C methylenetetrahydrofolate reductase gene (MTHFR), methionine synthase A2756G of (MTR), A66G of methionine synthase reductase (MTRR) A80G and the reduced folate carrier (RFC1) in patients with non-syndromic oral clefts, trying to match them with their development. Methods: We studied 140 patients with non-syndromic oral clefts and their mothers and 175 control subjects with their mothers, who underwent a questionnaire to obtain family information. Were collecting blood for DNA extraction from patients and their mothers to identify the genotypes of both by PCRRFLP, in addition to carrying out the determination of glucose, AST, ALT and serum creatinine, folic acid and vitamin B12 Serum and plasma homocysteine, and the hemogram. Results: Most patients have cleft lip and palate (55.8%), followed by isolated cleft palate (24.2%) and cleft lip (20%). Regarding gender, 62% of patients were male and 48% female and, after subdivision of the type of screwdriver according to sex was found a prevalence of males in the cracks of the type lip and palate (69 %) and lip (69.2%) and in the case of cleft palate was a female predominance (59%). The average concentration of serum folate in the group of mothers of cleft patients was significantly lower (13.8 ± 2.4 ng / mL) compared with the group of mothers of control subjects (18.8 ± 3.4 ng / mL) This was also observed for the group of cleft children as compared to controls, the dosage of folic acid had a significant difference with values of 15.6 ± 0.6 (ng / mL) and 17.9 ± 0.6 (ng / mL), respectively. For the biochemical measurements of glucose, AST, ALT and creatinine were not statistically different, nor was observed for haematological parameters performed. In assessing the frequency of polymorphisms C677T and A1298C MTHFR, A2756G MTR, MTRR A66G and A80G of the RFC1 there was no statistically significant difference in genotype distribution between cases and controls both for mothers and in the cleft. Conclusion: Although not observed association of polymorphisms with the development of cracks, the decrease in serum folate in the group of cleft patients and their mothers may reflect a disturbance in the metabolism of this metabolite, necessitating further studies such as studies methylation and expression to further elucidate the involvement of folate in the development of oral clefts

Digestibilidade das dietas e metabolismo de suínos alimentados com dietas contendo bentonita sódica em diferentes programas alimentares

Foi realizado um experimento para avaliar a digestibilidade aparente de dietas e o metabolismo de suínos alimentados com dietas contendo bentonita sódica submetidos a diferentes programas alimentares. Foram utilizados 24 suínos machos castrados, meio irmãos paternos, com peso vivo médio inicial de 42,2kg, alojados em gaiolas metabólicas. O delineamento experimental foi o inteiramente casualizado com três níveis de bentonita sódica (0,0; 0,3 e 0,5%) e dois programas alimentares (restrito e à vontade), com oito repetições cada. A adição de bentonita sódica não alterou (P>0,05) o consumo de ração e os balanços da energia e do nitrogênio. O consumo de ração diferiu (P<0,01) entre a alimentação restrita e à vontade (1,17 vs. 2,19kg d-1). O programa alimentar alterou (P<0,05) o balanço do N, mas não afetou (P>0,05) a retenção de N pelos animais. A alimentação à vontade alterou (P<0,05) o balanço da energia, sobretudo a energia retida (3.825 vs. 3.013kcal d-1). A adição de 0,5% de bentonita sódica nas dietas reduziu em 9% (P<0,01) a excreção fecal de fósforo. A adição de bentonita sódica nas dietas de suínos não altera os balanços da energia e do N nem as digestibilidades aparentes do Ca, Mg, Zn, Cu e Mn. A adição de bentonita sódica reduz a excreção fecal de fósforo. Não há interação entre o programa alimentar e a adição de bentonita sódica nas dietas.

Complexo enzimático para suínos: digestão, metabolismo, desempenho e impacto ambiental

Foram conduzidos dois experimentos para avaliar a suplementação enzimática (amilase, pentosanase, celulase, protease e a-galactosidase) em rações à base de milho e farelo de soja para suínos. No Exp 1, foram determinadas as digestibilidades aparentes da energia, matéria seca, proteína e das fibras das rações, com ou sem o complexo enzimático, para suínos machos castrados, com 19,96 ± 2,90 kg de peso vivo. Foi utilizado o método da coleta total de fezes e as rações foram formuladas com níveis reduzidos de energia, proteína e aminoácidos. No Exp 2, foram mensurados o desempenho, a excreção de sólidos totais e voláteis, matéria mineral, nitrogênio, macro e microminerais nas fezes, em relação ao desempenho, de suínos machos castrados dos 50 aos 151 dias de idade, com peso médio inicial de 18,34 ± 1,35 kg. Foram utilizadas três dietas, sendo uma ração formulada para atender ou exceder as exigências nutricionais dos animais, de acordo com o NRC (1998), e outras duas com níveis reduzidos de energia, proteína e aminoácidos, suplementadas ou não com o complexo enzimático. Foi utilizado o delineamento em blocos casualizados. A suplementação enzimática em rações contendo milho e farelo de soja não promoveu incrementos na digestibilidade de nutrientes, não melhorou o desempenho dos animais e também não reduziu a excreção de resíduos pelas fezes. Mais estudos são necessários para testar novas matrizes e diferentes níveis do complexo enzimático.

Alterações no metabolismo da cana-de-açúcar em função da aplicação de maturadores

O objetivo deste trabalho foi avaliar as alterações nos níveis de ácido chiquímico e ácido salicílico em plantas de cana-de-açúcar submetidas à aplicação de maturadores. Aplicou-se glyphosate nas doses de 400 e 200 mL ha-1 e na dose de 150 mL ha-1 em mistura com sulfumeturon-methyl a 12 e 20 g ha-1 e sulfumeturon-methyl a 20 g ha-1. As avaliações foram realizadas aos 15 e 30 dias após a aplicação (DAA) e aos 30, 60, 90, 120 e 150 dias após a colheita da cana-de-açúcar. Os teores de ácido chiquímico e salicílico nas plantas de canade-açúcar foram determinados por cromatografia líquida e espectrometria de massas. Os resultados mostraram que as doses de glyphosate correlacionaram-se diretamente com as concentrações de ácido chiquímico na planta, sendo superiores à da testemunha. Aos 30 DAA, houve aumento na concentração de ácido salicílico em todos os tratamentos estudados, revelando um processo de senescência da planta. Maiores doses de glyphosate promoveram aumento na concentração de ácido chiquímico e ácido salicílico antes da colheita da canade-açúcar. No período de crescimento da planta, aumentos nos teores dos ácidos chiquímico e salicílico revelaram dependência da aplicação dos produtos e também dos fatores abióticos e bióticos a que a cultura foi exposta.

Validação de método analítico por espectrofotometria UV para sistema emulsionado lipídico contendo benznidazol

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Teor lipídico da dieta, lipídios séricos e peso corporal em ratos exercitados

OBJETIVO: Analisar os efeitos de diferentes níveis de triglicerídeos fornecidos pela dieta sobre os parâmetros séricos triglicerídeos e lipoproteínas de alta densidade e o peso corporal de ratos sedentários e exercitados. MÉTODOS: Foram utilizados ratos Wistar, alimentados com dietas controle (7%peso/peso) e hiperlipídica (14% peso/peso) e subdivididos em sedentários e exercitados, por um período de 8 semanas. RESULTADOS: Verificou-se que o peso não diferiu entre os grupos, embora o consumo tenha sido reduzido nos grupos com dieta hiperlipídica. Os níveis de triglicerídeos não foram aumentados com a dieta rica em gordura e o HDL-colesterol se elevou apenas entre os animais exercitados que tiveram dieta normolipídica. CONCLUSÃO: A intensidade e o tempo de exercício físico influenciam de maneira mais aguda os níveis de HDL-colesterol em comparação aos níveis de triglicérides. Sugere-se que a dieta hiperlipídica deveria sobrepor (14%peso/peso) de gordura para que houvesse alterações relevantes nos parâmetros lipídicos e supostamente um aumento da performance física.

Metabolismo mitocondrial, radicais livres e envelhecimento

O envelhecimento pode estar associado ao maior acúmulo de lesões celulares decorrentes das espécies reativas do oxigênio e do nitrogênio derivadas do metabolismo mitocondrial. Com a progressão da idade, há acúmulo de proteínas, lipídeos, carboidratos e DNA oxidados em relação a organismos jovens, de acordo com a teoria dos radicais livres. Entretanto, nem sempre os idosos ou animais envelhecidos apresentam maior estresse oxidativo que os jovens. Este artigo discute o paradoxo da teoria dos radicais livres de acordo com a teoria da biogênese da manutenção adequada do metabolismo mitocondrial. Diversos fatores podem contribuir para a redução do estresse oxidativo, como a hormese induzida pela prática regular de exercícios físicos, a restrição calórica, a ingestão de antioxidantes nutricionais e o aumento da produção de antioxidantes celulares que. em conjunto, estes promovem a expressão das sirtuínas e das proteínas do choque térmico, protegendo a integridade e funcionalidade mitocondriais, reduzindo o estresse oxidativo e nitrosativo, o que está associado à redução do envelhecimento e aumento da longevidade.

Avaliação do cortisol, dehidroepiandrosterona sulfato e dos perfis lipídico e imunológico e suas correlações com a sensibilidade dolorosa, depressão e funcionalidade em mulheres com fibromialgia na pós-menopausa

Fibromyalgia (FM) is a non-inflammatory rheumatic syndrome characterized by widespread musculoskeletal pain with palpable tender points, muscle stiffness, fatigue, and sleep disturbances. Patients with FM have hormonal changes that are directly correlated with symptoms of the syndrome. The neuroendocrine regulation may be impaired, with abnormalities in the hypothalamus-pituitary-adrenal (HPA) axis with various hormones showing changes in their levels. In women in fertile period, various gonadal hormones are associated with symptoms of the syndrome, but studies focusing only a population of women in post-menopausal period who do not use hormone replacement are rare. We developed an analytical cross sectional study to assess the plasma levels of cortisol and dehidroepiandrosterona sulfate (DHEA-S) with quimioluminescence method in a group of 17 women with FM and 19 healthy women in post-menopause who do not use hormone replacement and observe the correlation with the symptoms of pain through algometry, depression and physical functional capacity measured from the Beck Depression Index (BDI) and the Fibromyalgia Impact Questionnaire (FIQ). Three blood samples were collected in the morning (between 8:00 9:30) with an interval of 24 hours for the measurements of hormonal levels and biochemical profile. There were no immunological or lipid changes in patients with FM. Comparing the two groups, there is no difference in levels of cortisol and a tangential effect for DHEA-S (p=0,094) with the lowest levels in the FM. DHEA-S also correlated with pain threshold (r=0,7) and tolerance (r=0,65) in group FM. We found the presence of depressive state and low physical functional capacity in FM. It was also evident that women in post-menopausal period, DHEA-S should influence the symptoms of increased sensitivity to pain, but not the presence of depressive status and low physical functional