Carvedilol-loaded nanocapsules : physicochemical characterization and in vitro drug release

Carvedilol (CV) has been used for the management of heart failure, hypertension and coronary artery diseases. However, it presents low oral bioavailability (25-35%). The objective of this study was to develop carvedilol-loaded nanocapsules (NC) in order to achieve a controlled drug release aiming the development of dosage forms to be administered by alternative routes. Poly(ε-caprolactone) (PCL) and Eudragit RS100 (EUD) were evaluated as polymeric wall. Nanocapsules (CV-PCL-NC and CV-EUD-NC) were prepared by interfacial deposition of preformed polymer method and characterized according to particle size and polydispersity, zeta potential, pH, drug content, encapsulation efficiency, morphology, backscattering analysis, presence of nanocrystals and drug release profile. Thermal analysis was performed to evaluate compatibility between CV and excipients. All formulations showed nanometric diameters with low polydispersity and pH slightly acid The zeta potential was positive and negative for CV-EUD-NC and CV-PCL-NC, respectively. The drug content was close to theoretical value (0.5 mg.mL-1) for both formulations and the encapsulation efficiency was higher than 87% and 99% for CV-EUD-NC and CV-PCL-NC, respectively. Nanocapsules were spherical-shaped and their suspensions showed no significant phenomena of physical instability. Drug release was controlled by both developed formulations. However, CV-PCL-NC showed phase separation during storage and an interaction between the drug and the surfactant was evidenced by thermal analysis. This study demonstrated the feasibility to encapsulate CV in nanocapsules to achieve a controlled release rate. Further studies will be carried out to explore alternatives routes of administration using these formulations

LC-UV method to assay raloxifene hydrochloride in rat plasma and its application to a pharmacokinetic study

A specific, precise, and accurate LC-UV method was developed and validated to assay raloxifene hydrochloride in rat plasma. Raloxifene was analyzed after liquid-liquid extraction and quantified by reversed phase liquid chromatography (C18 column) using acetonitrile and ammonium acetate buffer 0.05 M (pH 4.0) as mobile phase at a flow rate of 1 mL.min-1 and UV detection at 287 nm. Retention times of raloxifene and internal standard (dexamethasone) were approximately 11 min and 14 min, respectively. Linearity was checked for a concentration range between 25 ng.mL-1 and 1000 ng.mL-1. Intra- and inter-day precision had relative standard deviation lower than 10% and 15%, respectively. Recovery from plasma was higher than 90%. Accuracy values were 98.21%, 99.70%, and 102.70% for lower, medium, and upper limits of quantification, respectively. Limit of quantification was 25 ng.mL-1. Drug stability was analyzed at room temperature using plasma kept in a freezer at -80 °C for 45 days after processing for 6 h and three freeze-thaw cycles. The advantages of the method developed include stability under different conditions and low limit of quantification. Its applicability was confirmed by the analysis of raloxifene levels in plasma samples in a designed pharmacokinetic study in rats after intravenous administration (5 mg.kg-1)

Variables Pedagógicas Que Causan E Influyen El Absentismo Estudiantil En Las Clases De Matemática De La Escuela Superior Pedagógica De Namibe-Angola

The article aims to comparatively analyse the pedagogical variables that cause and influence the absenteeism of the students in math classes Pedagogical School of Namibe (Angola); the perception of teachers (population 44, sample 41) and students (population 131, sample 99) are contrasted, all of them of the second and the third level in the Degree of Physics and Chemistry. To achieve this objective a type questionnaire Likert scale are applied, it has four levels of agreement and fourteen pedagogical variables related with absenteeism. Descriptive and inferential statistics are applied on the data, also correlation analysis with Pearson coefficient, variance analysis using Mann-Whitney and Kruskal-Wallis tests, and multivariate analysis Factorial Kaiser-Meyer-Olkin are performed with Varimax rotation. As a result is obtained that the student disinterest and lack of ability of teachers to develop effective and motivating teaching are variables that cause and explain absenteeism in math classes. The analysis results show that some ways to reduce absenteeism are achieve stability of teachers in courses, increase opportunities for teachers to meet their students and achieve an environment of respect, solidarity and support for students

COMPOSTOS FENÓLICOS, CAROTENOIDES E ATIVIDADE ANTIOXIDANTE EM FRUTOS DE CAJÁ-MANGA

O presente trabalho teve como objetivo quantificar os compostos fenólicos, carotenoides e atividade antioxidante de frutos de cajá-mangueira de diferentes genótipos de ocorrência espontânea no Estado da Paraíba. O delineamento experimental utilizado foi o inteiramente casualizado (DIC), com 3 genótipos (G1, G2 e G3), em três repetições. Os frutos foram analisados quanto ao conteúdo de ácido ascórbico, carotenoides totais, flavonoides amarelos, antocianinas, polifenóis extraíveis totais e atividade antioxidante. Os genótipos diferiram significativamente quanto ao conteúdo de ácido ascórbico, carotenoides totais, flavonoides amarelos e antocianinas. Os resultados demonstraram que o cajá-manga possui quantidades significativas de ácido ascórbico (46,49 mg.100 g-1). Considerando os baixos teores de flavonoides amarelos e antocianinas em polpa de cajá-manga, é possível inferir que a ação antioxidante exibida decorra, principalmente, da presença de ácido ascórbico e polifenóis extraíveis totais. O conteúdo de ácido ascórbico foi superior ao de frutas usualmente consumidas e atividade antioxidante próxima ao de frutas com um potencial antioxidante conhecido. A atividade antioxidante foi fortemente correlacionada com o conteúdo de ácido ascórbico. O conteúdo de ácido ascórbico, carotenoides totais, flavonoides amarelos e antocianinas contribuirão para a variabilidade entre genótipos, com ácido ascórbico inferindo a maior contribuição para esta variação

Fatty acid synthase as a potential new therapeutic target for cervical cancer

Fatty acid synthase (FASN) is the rate-limiting enzyme for the de novo synthesis of fatty acids in the cytoplasm of tumour cells. Many tumour cells express high levels of FASN, and its expression is associated with a poorer prognosis. Cervical cancer is a major public health problem, representing the fourth most common cancer affecting women worldwide. To date, only a few in silico studies have correlated FASN expression with cervical cancer. This study aimed to investigate in vitro FASN expression in premalignant lesions and cervical cancer samples and the effects of a FASN inhibitor on cervical cancer cells. FASN expression was observed in all cervical cancer samples with increased expression at more advanced cervical cancer stages. The FASN inhibitor (orlistat) reduced the in vitro cell viability of cervical cancer cells (C-33A, ME-180, HeLa and SiHa) in a time-dependent manner and triggered apoptosis. FASN inhibitor also led to cell cycle arrest and autophagy. FASN may be a potential therapeutic target for cervical cancer, and medicinal chemists, pharmaceutical researchers and formulators should consider this fi nding in the development of new treatment approaches for this cancer type

EVALUACIÓN DE LA PRESENCIA DE LOS FACTORES DE RIESGO CARDIOVASCULAR EN ESTUDIANTES UNIVERSITARIOS DE PAÍSES LUSÓFONOS

Objetivo: avaliar a presença de fatores de risco cardiovascular em estudantes universitários de paíseslusófonos. Metodologia: estudo transversal, realizado de janeiro a julho de 2017, com 334 estudantes de umauniversidade pública federal no estado do Ceará, com idade igual ou superior a 18 anos, dos seguintes países: Brasil,Angola, Cabo Verde, Guiné-Bissau, Moçambique, São Tomé e Príncipe e Timor-Leste. Efetuou-se a análise estatísticados dados por meio do programa Epi Info versão 7.1.2.0. Resultados: dos 334 participantes, 75,7% encontravam-se nafaixa etária entre 18 e 24 anos, 56,9% eram brasileiros, 51,8% do sexo feminino, 47,3% de cor parda e 47,6% solteiroscom parceria eventual. Quanto aos fatores de risco para doenças cardiovasculares, destacaram-se a história familiar dedoenças cardiovasculares (81,1%), o sedentarismo (44,3%) e o uso do álcool (36,2%). Conclusão: a identificação dosprincipais fatores de risco modificáveis e hereditários nos estudantes universitários poderão nortear ações voltadas paraa promoção da saúde cardiovascular.Objective: to evaluate the presence of cardiovascular risk factors in university students from Portuguese-speaking countries. Methodology:cross-sectional study, carried out from January to July 2017, with 334 students from a federal public university in the state of Ceará, aged 18 yearsand over, from the following countries: Brazil, Angola, Cape Verde, Guinea-Bissau, Mozambique, Sao Tome and Principe and East Timor. Data wasanalyzed with the Epi Info version 7.1.2.0 statistical software. Results: of the 334 participants, 75.7% were aged 18-24 years old, 56.9% were Brazilian,51.8% were female, 47.3% were brown and 47.6% were single individuals with an occasional partner. Risk factors for cardiovascular diseasesincluded a family history of cardiovascular disease (81.1%), sedentary lifestyle (44.3%) and alcohol use (36.2%). Conclusion: identification of themain modifiable and hereditary risk factors in university students could guide actions aimed at promoting cardiovascular health.Objetivo: evaluar la presencia de factores de riesgo cardiovascular en estudiantes universitarios de países lusófonos. Metodología:estudio transversal, realizado de enero a julio de 2017, con 334 estudiantes de una universidad pública federal en el estado de Ceará, con edad igualo superior a 18 años, de los siguientes países: Brasil, Angola, Cabo Verde, Guinea-Bissau, Mozambique, San Tomé y Príncipe y Timor-Leste. Se hizoanálisis estadístico de los datos por medio del programa Epi Info versión 7.1.2.0. Resultados: de los 334 participantes, 75,7% estaban en edad entre18 y 24 años, 56,9% eran brasileños, 51,8% del sexo femenino, 47,3% de color pardo y 47,6% solteros con pareja eventual. Acerca de los factores deriesgo para enfermedades cardiovasculares, se destacaron la historia familiar de enfermedades cardiovasculares (81,1%), el sedentarismo (44,3%) y eluso de alcohol (36,2%). Conclusión: la identificación de los principales factores de riesgo modificables y hereditarios en los estudiantes universitariospodrán nortear acciones de promoción de salud cardiovascular

QUALIDADE DE FRUTOS DE ACESSOS DE CAJÁ-MANGUEIRA DURANTE A MATURAÇÃO

Este estudo teve como objetivo avaliar as mudanças nas características físicas e físico-químicas ocorridas durante a maturação de frutos de genótipos de cajá-mangueira (Spondias cytherea Sonn.). Os frutos foram oriundos de cinco plantas de cajá-mangueira, de ocorrência espontânea, em cinco estádios de maturação (TV: totalmente verde; IP: início de pigmentação amarela; AE: amarelo esverdeado e PA: predominantemente amarelo), e posteriormente selecionados quanto à uniformidade da maturação. O delineamento experimental utilizado foi o inteiramente casualizado, em esquema bifatorial 5 x 4, sendo cinco genótipos, quatro estádios de maturação. Os frutos foram avaliados quanto a Acidez Titulavel (AT), teor de sólidos solúveis (SS) e relação SS/AT. Constatou-se que com o avanço da maturação os frutos de todos os genótipos apresentam um aumento no diâmetro e comprimento, na massa fresca, e um aumento na luminosidade e na intensidade da coloração da casca, em paralelo a transição da cor verde para uma cor em tons de amarelo intenso. De modo geral os frutos da cajá-mangueira apresentam rendimento de polpa superior a 70%, sendo esta porcentagem superior ao mínimo aceito para industrialização. Os frutos dos genótipos P1, P2 e P5 destacam-se dupla finalidade, tanto para o consumo fresco como para a industrialização, por apresentarem rendimento de polpa, teor de SS superior e AT, superior ao mínimo aceitável pelo padrão de identidade e qualidade (PIQ). Além de elevado conteúdo de ácido ascórbico, destacando-se os genótipos P1 e P2 formam superiores aos demais por terem apresentado maior conteúdo de ácido ascórbico

Salivary characteristics may be associated with burning mouth syndrome?

Burning mouth syndrome (BMS) it is characterized by burning and uncomfortable sensations with no clinical alterations or laboratory findings. The evaluation of the salivary characteristics of people with BMS can help the understanding of the pathogenesi

Energetic metabolic profile of ewes presenting low body condition score induced to subclinical hypocalcemia in early postpartum

The aim of the present study is to assess plasma concentrations of metabolites related to energy balance in ewes showing low body condition score (BCS) induced to subclinical hypocalcemia in early postpartum. Sixteen crossbred ewes (Ideal x Corriedale) presenting BCS 0.05), whereas the mean concentrations of these marks after five days were lower in the hypocalcemia group (P0.05) level. These results evidence that, despite the subclinical hypocalcemia induction at early postpartum, ewes presenting low body condition do not change the concentrations of energy balance-related metabolites in the following five days