Obtenção e caracterização de complexos de inclusão binários e ternários com praziquantel

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior

Extração, caracterização e atividades biológicas de proteínas da espécie cnidoscolus urens (L.) Arthur

The extraction, chemical and structural characterization of a wide variety of compounds derived from plants has been a major source of bioactive molecules. Several proteases have been isolated in the plant kingdom, with numerous pharmacological and biotechnological applications. Among the proteases isolated from plants, are the fibrinogenolytic, with relevant application in the treatment of disorders in the coagulation cascade, in addition to potential use as a tool in clinical laboratories. In this study, in addition to evaluating the effects of the protein extract of Cnidoscolus urens (L.) Arthur (Euphorbiaceae) in the coagulation cascade also investigates the presence of antimicrobial activity and characterizes the proteolytic activity detected in this extract, aiming to determine their potential pharmacological and biotechnological application. In this way, crude protein extracts obtained from the leaves of C. urens in Tris-HCl 0.05M, NaCl 0.15M, pH 7.5, were precipitated in different concentrations of acetone, and assessed for the presence of proteolytic activity in azocaseína and fibrinogen. The most active fraction (F1.0) in these tests was chosen for assessment of biological activity and biochemical characterization. The Aα chain and Bβ of fibrinogen were completely cleaved at a concentration of 0.18 μg/μL of protein fraction in 4 minutes. Fibrinogenolytic activity presented total inhibition in the presence of E-64 and partial in the presence of EDTA. The fraction demonstrated coagulant activity in plasm and reduced the APTT, demonstrating acting on the factors coagulation of the intrinsic pathway and common, not exerting effects on the PT. Fibrinolytic activity on plasma clot was detected only in SDS-PAGE in high concentrations of fraction, and there were no defibrinating. Although several proteases isolated from plants and venomous animals are classically toxic, the fraction F1.0 of C. urens not expressed hemorrhagic nor hemolytic activities. Fraction F1.0 also showed no antimicrobial activity. In proteolytic activity on the azocasein, the optimal pH was 5.0 and optimum temperature of 60ºC. The enzyme activity has been shown to be sensitive to the presence of salts tested, with inhibition for all compounds. The surfactant triton did not influence the enzyme activity, but the tween-20 and SDS inhibited the activity. In the presence of reducing agents increase in enzyme activity occurred, a typical feature of enzymes belonging to the class of cysteine proteases. Several bands with proteolytic activity were detected in zymogram, in the region of high-molecular-weight, which were inhibited by E-64. In this study, we found that C. urens presents in its constitution cysteine proteases with fibrinogenolytic and procoagulant activity, which may be isolated, with potential application in treatment of bleeding disorders, thrombolytic and clinical laboratory

Preparação e caracterização de sistemas emulsionados lipidicos contendo praziquantel

Praziquantel (PRZ) is the main drug used for treatment of schistosomiasis in Brazil. It is administered by oral rout as tablets. However, has low aqueous solubility which limits this therapeutic success dosage form and availability of liquid forms. The emulsion systems have great potential and represent an interesting strategy to increase the solubility of drugs. The aim of study was the development and characterization of lipid-emulsified liquid systems of the type oil in water (O / W), the base of soybean oil as the internal phase stabilized by surfactants pair Tween® 80 and Span® 80, for improving the phase biopharmaceutical of PRZ. After selecting the best value of Hydrophilic-Lipophilic Balance (HLB = 11), the parameters of the preparation of the formulations were optimized emulsification technique. The emulsions were successfully obtained; the liquid forms provided exhibited Newtonian behavior and an increase in solubility of PRZ higher than 20 times. The accelerated stability study demonstrated the stability of the emulsions and the effect of cosurfactants investigated. The study of the dynamics of interaction between components in the diagram showed pseudoternary phase regions to obtain O/W emulsions, whereas the study of the interaction of the components and their effect on system structure and the efficiency of incorporation of the drug led to systems with an amount of soluble drug even higher (about 1.5%), which demonstrates the potential of this new input mainly for the treatment of schistosomiasis, which resulted in the filing of patent BR 10 2013 0004 55 3

Preparação e caracterização de complexos multicomponentes contendo ciclodextrinas com metotrexato

Conselho Nacional de Desenvolvimento Científico e Tecnológico

Caracterização dos marcadores químicos e avaliação de atividades biológicas do extrato de Spondias mombim

Spondias mombin is a fruitful species dispersed in tropical regions of America, Africa and Asia. In Brazil, the species can be found mainly in the northern and northeastern regions. Scarce chemical and pharmacological studies have been reported for S. mombin and until this moment studies about chemical markers were not developed. In this context, the aims of this study were to characterize the chemical markers from S. mombin leaves and evaluate their anti-inflammatory, antioxidant and antiproliferative potentials. The chemical profile of the hydroethanolic extract from S. mombin leaves analyzed by HPLC-DAD, through a validated method, allowed the identification and quantification of ellagic acid and chlorogenic acid. This extract showed anti-inflammatory potential in acute peritonitis model induced by carrageenan. The hydroethanolic extract from S. mombin leaves was subjected to a liquid-liquid partition with the solvents: n-hexane, dichloromethane, ethyl acetate and n-butanol. Regarding the anti-inflammatory potential of the fractions obtained they were active; however, ethyl acetate fraction at 200 mg/kg showed highlighted results. The compounds ellagic acid and chlorogenic acid also inhibited the leukocyte migration to the site of inflammation at 2.5, 5 and 10 mg/kg. The hydroethanolic extract, fractions and the chemical markers showed significant antioxidant potential when evaluated in different assays: DPPH Free-Radical Scavenging, Superoxide Radical Scavenging, Hydroxyl Radicals Scavenging and Reducing Power. Taken together our results showed that hydroethanolic extract of S. mombin leaves has ellagic acid and chlorogenic acid as bioactive markers and it demonstrated antiinflammatory and antioxidant properties besides no cytotoxicity against 3T3 cells. It enables us to suggest S. mombin as an important species to develop herbal drugs

Utilização intracoágulo de espuma fibrinolítica - preparação, caracterização e atividade in vitro de uma espuma de estreptoquinase e proposta de uma nova abordagem terapêutica

Foam was developed as a novel vehicle for streptokinase with the purpose of increasing the contact time and area between the fibrinolytic and the target thrombus, which would lead to a greater therapeutic efficacy at lower doses, decreasing the drug s potential to cause bleeding. Fibrinolytic foams were prepared using CO2 and human albumin (at different v:v ratios), as the gas and liquid phases, respectively, and streptokinase at a low total dose (100,000 IU) was used as fibrinolytic agent conveyed in 1 mL of foam and in isotonic saline solution. The foams were characterized as foam stability and apparent viscosity. The thrombolytic effect of the streptokinase foam was determined in vitro as thrombus lysis and the results were compared to those of a fibrinolytic solution (prepared using the same dose of streptokinase) and foam without the fibrinolytic. In vitro tests were conducted using fresh clots were weighed and placed in test tubes kept at 37 ° C. All the samples were injected intrathrombus using a multiperforated catheter. The results showed that both foam stability and apparent viscosity increased with the increase in the CO2:albumin solution ratio and therefore, the ratio of 3:1 was used for the incorporation of streptokinase. The results of thrombus lysis showed that the streptokinase foam presented the highest thrombolytic activity (44.78 ± 9.97%) when compared to those of the streptokinase solution (32.07 ± 3.41%) and the foam without the drug (19.2 ± 7.19%). We conclude that fibrinolytic foam showed statistically significant results regarding the enhancement of the lytic activity of streptokinase compared to the effect of the prepared saline solution, thus it can be a promising alternative in the treatment of thrombosis. However, in vivo studies are needed in order to corroborate the results obtained in vitro

Dispersões sólidas de sinvastatina: preparação, caracterização, no estado sólido utilizando técnicas emergentes e estudo de estabilidade

This thesis aimed to assess the increase in solubility of simvastatin (SINV) with solid dispersions using techniques such as kneading (MA), co-solvent evaporation (ES), melting carrier (FC) and spray dryer (SD). Soluplus (SOL), PEG 6000 (PEG), PVP K-30 (PVP) e sodium lauryl sulphate (LSS) were used as carriers. The solid dispersions containing PEG [PEG-2(SD)], Soluplus [SOL-2(MA)] and sodium lauryl sulphate [LSS-2(ES)] were presented with a greater increase in solubility (5.02, 5.60 and 5.43 times respectively); analyses by ANOVA between the three groups did not present significant difference (p<0.05). In the phase solubility study, the calculation of the Gibbs free energy (ΔG) revealed that the spontaneity of solubilisation of SINV occurred in the order SOL>PEG >PVP 75%>LSS, always 80%. The phase diagrams of PEG and LSS presented solubilization stoichiometry of type 1:1 (type AL). The diagrams with PVP and SOL tend to 1:2 stoichiometry (type AL + AP). The stability coefficients (Ks) of the phase diagrams revealed that the most stable reactions occurred with LSS and PVP. The solid dispersions were characterized by Fourier transform infrared (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), particle size distribution (PSD), near-infrared spectroscopy imaging (NIR-CI) and X-ray diffraction of the powder using the Topas software (PDRX-TOPAS). The solid dispersion PEG-2(SD) presented the greatest homogeneity and the lowest degree of crystallinity (18.2%). The accelerated stability study revealed that the solid dispersions are less stable than SINV, with PEG-2(SD) being the least stable, confirmed by FTIR and DSC. The analyses by PDRX-TOPAS revealed the amorphous character of the dispersions and the mechanism of increasing solubility

Caracterização do nicho alimentar do polvo octopus insularis (cephalopoda: octopodidae): da população ao indivíduo

Octopus insularis, target species in this study, is the dominant benthic octopus of the North and Northeast Brazil. Studies on behavior and ecology of the species have been conducted primarily on oceanic islands, with little information on the continental populations. In this study, two regions of the coast of RN, Rio do Fogo and Pirangi, were chosen for the characterization of the niche by O. insularis populations. The dietary niche, habitat and distribution of O. insularis of oceanic islands and the mainland, were compared. In addition, individual characteristics of feeding behavior in a population at Atol das Rocas was studied, taking into account the size of individuals, the proximity of the dens and characteristics of their "personality". The diet of the Rio do Fogo population was composed mainly of bivalve molluscs (82%), unlike Pirangi population that has a diet consisting mainly of crustaceans Decapoda (68%), similar to that described for the populations of the islands. Consequently, the feeding niches of the island populations were more similar, with greater overlap, but the niche breadth of the continent was larger. The habitats of occurrence on the coast includes reefs, rocks, gravel and an environment called Restinga, a plateau composed of biogenic gravel, sand, sponges and algae, showed a high density of animals. Similarly to that found in the islands, O. insularis in the continent, had a clumped distribution, and a bathymetric segregation between small and large individuals. The differences in diet composition among populations were explained by differences in habitat and coverage of the substrate, which may be directly influencing the diversity and prey availability in these environments. The individual analyzes of the population at Atol das Rocas, showed no relationship between the degree of individual specialization and the different personalities, or the distance between dens. The results suggest that the foraging strategy with greater availability of prey in the environment has an influence on diet octopuses over preferences or personalities

Caracterização ecofisiológica de sementes de espécies lenhosas da Caatinga

Dormancy is an inherent property of the seeds that define the environmental conditions in which they are able to germinate and their presence is an adaptive trait common in species inhabiting semiarid regions. Moreover, the ability of seedling establishment in these environments has been related to the size, strength and chemical characteristics of the seeds. This study investigated patterns of dormancy and germination speed in tree species of the Caatinga, exploring how the seed size influence the processes of germination, seedling size and biomass allocation. In addition, we aim to investigate the chemical characteristics of the reserves, to verify a possible relationship between nutritional content and the process of seed germination. Therefore, seeds were collected from ten species of woody Caatinga for tests of breaking dormancy, germination and biochemical characterization. Overall, the results show that the scarification treatments mechanical and chemical, and thermal shock influenced the percentage and speed of germination in 50 % of the species, suggesting that they have some level of physical dormancy in the seeds. Biochemical characterization showed the existence of large amounts of carbohydrates in the seeds of all species, low proportion of protein and low amounts of neutral lipids. Using linear regression, we demonstrated the existence of a significant relationship between seed size and the ratio of root/shoot where the largest seeds invested a greater amount of resources for shoot growth. The relationship between germination speed and non-reducing sugar content was also significant, so these compounds is related to the maintenance of physiological seed quality. These results confirm some relationships discussed in the literature for cultivated species, but can be applied to the species native to the Caatinga

Caracterização do acidente de trânsito e gravidade do trauma: um estudo em vítimas de um hospital de emergência de Natal

Descriptive exploratory study, with quantitative approach and prospective data performed on the Monsenhor Walfredo Gurgel Hospital Complex (MWGH), in Natal/RN, aiming to classify the type of motor vehicle involved in the accident, the public roadway s user quality and the more frequent injuries; to evaluate the severity of trauma in traffic accident victims; characterized the severity of the injuries and the trauma, and the type of motor vehicle involved. The population comprises 605 traffic accident victims, with data collected between October and December 2007. We used as a support for the evaluation of severity of injuries and trauma the Glasgow Coma Scale (GCSl), the Condensed Abbreviated Injury Scale (CAIS) and the Injury Severity Score (ISS). The results show that 82.8% of the victims were male; 78.4% were aged 18 to 38; the victims originating from the State s Countryside prevailed (43.1%); 24.3% of the population had completed middle-level instruction; 23.1% worked on commerce and auxiliary activities; most (79.4%) was catholic; 48.8% were married/consensual union; 76.2% earned up to two monthly minimum wages; Sunday was the day with the most accidents (25.1%); 47.4% were attended to in under an hour after the event; the motorcycle on its own was responsible for 53.2% of the accidents; 42.3% were attended to by the SAMU; 61.8% were victims of crashes; over half (53.4%) used individual protection equipment (IPE); 49.4% were helmets and 4.0% the seatbelt; 61.3% were motorcycle drivers; 43.3% of the accidents took place in the afternoon shift; from 395 drivers, 55.2% were licensed, and 50.7% among those had been licensed for 1 to 5 years; 90.7% of the victims had GCS1 between 13 and 15 points at the time of evaluation; the body area most affected was the external surface (35.9%); 38.8% of the injuries were light or moderate (AIS=1 and AIS=2); 83.2% had light trauma (ISS between 1 and 15 points). In face of the results, we can conclude that there is a risk for the elevation of injury severity and trauma resulting from traffic accidents, when these events are related to certain variables such as gender, age, weekday, the interval between the accident and the first care, ingestion of drugs, type of accident, the public roadway s user quality, the use of IPE, day shift, body regions and the type of motor vehicle involved in the accident

Argamassas do grupo escolar Augusto Severo/RN: caracterização e incidência de manifestações patológicas

The search for cultural heritage preservation should be a constant, in order to minimize the lost of historical and cultural identity of a country. As part of this cultural heritage, highlights the importance of historical buildings. For the principles of restoration are met its important to know the state of conservation and the existing materials. Given the above, this work aims to study the pathological manifestations of the mortar coating from the Grupo Escolar Augusto Severo. For this, was conducted historical survey of the building, on-site visits with visual observation, collecting samples of mortar coating and characterization through visual and laboratory analysis, XRF, XRD, TG/DTG, OM and SEM-EDS. From the observations, pathological manifestations were found as: cracks, detachment of the coating, dirt, use of inappropriate material basis of cement, efflorescence, mold and mildew and also incompatible material base of cement. It was found that the pathological manifestations were intensified due to lack of coverage in some spots and especially the abandonment of the building, that many years does not have restoration or any other type of preventive and corrective maintenance. The results of laboratory tests indicated that the mortars studied are based on lime, with calcitic nature, and siliceous aggregate, with the presence of clay in two samples. From the samples collected, two are composed of lime, sand and clay and two by lime and sand. In this regard, it is important to conduct periodic inspections and maintenance, as well as carrying out restoration with use of material compatible with the original

Caracterização de estruturas planares com substratos Iso/Anisotrópicos truncados através da técnica da ressonância transversa modificada

This work presents a theoretical and numerical analysis using the transverse resonance technique (TRT) and a proposed MTRT applied in the analysis of the dispersive characteristics of microstrip lines built on truncated isotropic and anisotropic dielectric substrates. The TRT uses the transmission lines model in the transversal section of the structure, allowing to analyze its dispersive behavior. The difference between TRT and MTRT consists basically of the resonance direction. While in the TRT the resonance is calculated in the same direction of the metallic strip normal axis, the MTRT considers the resonance in the metallic strip parallel plane. Although the application of the MTRT results in a more complex equivalent circuit, its use allows some added characterization, like longitudinal section electric mode (LSE) and longitudinal section magnetic mode (LSM), microstrips with truncated substrate, or structures with different dielectric regions. A computer program using TRT and MTRT proposed in this work is implemented for the characterization of microstrips on truncated isotropic and anisotropic substrates. In this analysis, propagating and evanescent modes are considered. Thus, it is possible to characterize both the dominant and higher order modes of the structure. Numerical results are presented for the effective permittivity, characteristic impedance and relative phase velocity for microstrip lines with different parameters and dimensions of the dielectric substrate. Agreement with the results obtained in the literature are shown, as well as experimental results. In some cases, the convergence analysis is also performed by considering the limiting conditions, like particular cases of isotropic materials or structures with dielectric of infinite size found in the literature. The numerical convergence of the formulation is also analyzed. Finally, conclusions and suggestions for the continuity of this work are presented

Caracterização numérica de antenas para aplicações RFID utilizando o método das ondas - WCIP

In recent years, the radio frequency identification technology (RFID) has gained great interest both industrial communities as scientific communities. Its ability to locate and monitor objects, animals and persons with active or passive tags allows easy development, with good cost-benefice and still presents undeniable benefits in applications ranging from logistics to healthcare, robotics, security, among others. Within this aspect what else comes excelling are RFID tags and the antennas used in RFID readers. Most tags have antennas omnidirectional and are usually manufactured as dipoles modified printed. The primary purpose of a project of antenna for tag is to achieve the required input impedance to perform a good marriage impedance with the load impedance of the chip. Already the objective principal in project of antennas for readers is to achieve reduced sizes and structures with good data transmission capacity. This work brings the numerical characterization of antennas for RFID applications, being these divided into tags RFID and antennas for RFID readers. Three tags RFID and two antennas for RFID readers, found in literature, are analyzed. The analysis of these structures is made using the Method of Waves - WCIP. Initial results found in the literature are compared with those obtained through simulations in WCIP with objective to show that the Method of Waves is able to analyze such structures. To illustrate the results obtained in simulations is presented the behavior of electric and magnetic fields. It also performed a literature review on the characteristics and principles of RFID technology. Suggestions for continuity to this work are presented

Caracterização de antenas planares com substrato metamaterial

This work presents a theoretical and numerical analysis for the radiation characteristics of rectangular microstrip antenna using metamaterial substrate. The full wave analysis is performed in the Fourier transform domain through the application of the Transverse Transmission Line - TTL method. A study on metamaterial theory was conducted to obtain the constructive parameters, which were characterized through permittivity and permeability tensors to arrive at a set of electromagnetic equations. The general equations for the electromagnetic fields of the antenna are developed using the Transverse Transmission Line - TTL method. Imposing the boundary conditions, the dyadic Green s function components are obtained relating the surface current density components at the plane of the patch to the electric field tangential components. Then, Galerkin s method is used to obtain a system of matrix equations, whose solution gives the antenna resonant frequency. From this modeling, it is possible to obtain numerical results for the resonant frequency and return loss for different configurations and substrates

Caracterização de superfícies seletivas de freqüência e de antenas fractais para aplicações em redes sem fio

This work aims to investigate the behavior of fractal elements in planar microstrip structures. In particular, microstrip antennas and frequency selective surfaces (FSSs) had changed its conventional elements to fractal shapes. For microstrip antennas, was used as the radiating element of Minkowski fractal. The feeding method used was microstrip line. Some prototypes were built and the analysis revealed the possibility of miniaturization of structures, besides the multiband behavior, provided by the fractal element. In particular, the Minkowski fractal antenna level 3 was used to exploit the multiband feature, enabling simultaneous operation of two commercial tracks (Wi-Fi and WiMAX) regulated by ANATEL. After, we investigated the effect of switches that have been placed on the at the pre-fractal edges of radiating element. For the FSSs, the fractal used to elements of FSSs was Dürer s pentagon. Some prototypes were built and measured. The results showed a multiband behavior of the structure provided by fractal geometry. Then, a parametric analysis allowed the analysis of the variation of periodicity on the electromagnetic behavior of FSS, and its bandwidth and quality factor. For numerical and experimental characterization of the structures discussed was used, respectively, the commercial software Ansoft DesignerTM and a vector network analyzer, Agilent N5230A model