Obtenção e caracterização de sistemas particulados de quitosana para liberação gástrica de amoxicilina

The infection caused by Helicobacter pylori (H. pylori) is associated with gastroduodenal inflammation can lead to the development of gastritis, gastric or duodenal ulcer and gastric cancer (type 1 carcinogen for stomach cancer). Amoxicillin is used as first-line therapy in the treatment of H. pylori associated to metronidazole or clarithromycin, and a proton pump inhibitor. However, the scheme is not fully effective due to inadequate accumulation of antibiotics in gastric tissue, inadequate efficacy of ecological niche of H. pylori, and other factors. In this context, this study aimed to obtaining and characterization of particulate systems gastrorretentivos chitosan - amoxicillin aiming its use for treatment of H. pylori infections. The particles were obtained by the coacervation method / precipitation using sodium sulfate as precipitating agent and crosslinking and two techniques: addition of amoxicillin during preparation in a single step and the sorption particles prior to amoxycillin prepared by coacervation / precipitation and spray drying. The physicochemical characterization of the particles was performed by SEM, FTIR, DSC, TG and XRD. The in vitro release profile of amoxycillin free and incorporated in the particles was obtained in 0.1 N HCl (pH = 1.2). The particles have higher encapsulation efficiency to 80% spherical shape with interconnected particles or adhered to each other, the nanometric diameter to the systems obtained by coacervation / precipitation and fine for the particles obtained by spray drying. The characterization by FTIR, DSC and XRD showed that the drug was incorporated into the nanoparticles dispersed in the polymeric matrix. Thermal analysis (TG and DSC) indicated that encapsulation provides greater heat stability to the drug. Amoxicillin encapsulated in nanoparticles had slower release compared to free drug. The particles showed release profile with a faster initial stage (burst effect) reaching a maximum at 30 minutes 35% of amoxicillin for the system in 1: 1 ratio relative to the polymer and 80% for the system in the ratio 2: 1. Although simple and provide high encapsulation efficiency of amoxicillin, the process of coacervation, precipitation in one step using sodium sulfate as precipitant / cross-linker must be optimized in order to adjust the release kinetics according to the intended application.

Materiais bionanocompósitos a base de argilominerais e hidróxidos duplos lamelares como sistemas de liberação de fármacos

Bionanocomposites systems clay base (montmorillonite and sepiolite), layered double hidroxides and biopolymers (carboxymethylcellulose and zein) were evaluated as topical delivery systems with antibacterial activity and as oral delivery systems. For this study, neomycin, a topical antibiotic, indicated mainly for open wound infections. The drug amoxicillin, an antibiotic indicated mainly for throat infections, were also used in this study. Both antibiotics were used as model drugs. Initially, drugs were incorporated directly into the biopolymer matrix, comprising the combination of carboxymethylcellulos and zein, being conformed as movies and balls and evaluated for their antibacterial activity and controlled release simulating gastrointestinal fluids. Moreover, hybrids materials have been prepared where the neomycin drug was incorporated into the lamellar inorganic solids, such as montmorillonite by ion exchange reaction, and the fibrous type, such as sepiolite by adsorption in aqueous solution. But the drug amoxicillin was incorporated into layered double hydroxides by anion exchange and montmorillonite by cation exchange. The resulting hybrids were in turn combined with the biopolymer matrix yielding bionanocomposites shaped materials such as films were tested for their antibacterial activity, and the shaped materials beads were tested for their release in the gastrointestinal fluids. Through the analysis of various physico-chemical techniques, we observed the interactions between the studied materials, the formation of hybrids materials, obtaining the bionanocomposites materials and material efficiency when applied in controlled release of drugs both topical and use oral mainly influenced by the presence of zein, are promising as topical delivery systems and oral drugs.

Nanopartículas catiônicas de poli (ácido lático) para liberação modificada de peptídios da peçonha do escorpião Tityus serrulatus

Reported accidents involving the poisoning scorpions are still frequent in Brazil, mainly caused by Tityus serrulatus, known as yellow scorpion. Although antivenom sera are produced routinely by various government laboratories, the effectiveness of its use depends on how quickly treatment is initiated and efficiency in the production of antibodies by the immunized animals. In this study, the development of cationic polymeric nanoparticles of poly(lactic acid) aimed to create a modified delivery system for peptides and proteins of T. serrulatus venom, able to enhance the production of serum antibodies against the scorpion toxins. The cationic nanoparticles were obtained by a low energy nanoprecipitation, after study of the parameters’ variations effects over the physicochemical properties of the particles. The surface functionalization of the nanoparticles with the hyperbranched polyethyleneimine was proved by zeta potential analysis and enabled the adsorption by electrostatic interaction of different types of proteins. The protein loading efficiency of 40-80 % to bovine serum albumin (BSA) and 100 % to scorpion venom peptides evaluated by spectrophotometry and polyacrylamide gel electrophoresis confirmed the success of the selected parameters established for obtainment of nanoparticles, produced with size between 100 to 250 nm. The atomic force microscopy analysis and in vitro release showed that the spherical nanoparticles provided a sustained release profile of proteins by diffusion mechanism, demonstrating the potential for application of the nanoparticles in vivo.

Nanopartículas catiônicas de poli (ácido lático) para liberação modificada de peptídios da peçonha do escorpião Tityus serrulatus

Reported accidents involving the poisoning scorpions are still frequent in Brazil, mainly caused by Tityus serrulatus, known as yellow scorpion. Although antivenom sera are produced routinely by various government laboratories, the effectiveness of its use depends on how quickly treatment is initiated and efficiency in the production of antibodies by the immunized animals. In this study, the development of cationic polymeric nanoparticles of poly(lactic acid) aimed to create a modified delivery system for peptides and proteins of T. serrulatus venom, able to enhance the production of serum antibodies against the scorpion toxins. The cationic nanoparticles were obtained by a low energy nanoprecipitation, after study of the parameters’ variations effects over the physicochemical properties of the particles. The surface functionalization of the nanoparticles with the hyperbranched polyethyleneimine was proved by zeta potential analysis and enabled the adsorption by electrostatic interaction of different types of proteins. The protein loading efficiency of 40-80 % to bovine serum albumin (BSA) and 100 % to scorpion venom peptides evaluated by spectrophotometry and polyacrylamide gel electrophoresis confirmed the success of the selected parameters established for obtainment of nanoparticles, produced with size between 100 to 250 nm. The atomic force microscopy analysis and in vitro release showed that the spherical nanoparticles provided a sustained release profile of proteins by diffusion mechanism, demonstrating the potential for application of the nanoparticles in vivo.

Obtenção de triacetato de celulose a partir do bagaço de cana-deaçúcar para revestimento de micropartículas de goma gelana e avaliação do seu perfil de liberação in vitro e da mucoadesão ex vivo

Oral route of administration is considered to be the most comfortable, safe and greater adaptation for patients. But, oral route presents some disadvantages such as drugs bioavailability and side effects on the stomach. Some technologies are studied to soften and/or resolve these problems, such as coating with polymeric films, which are able to protect the pharmaceutical form of the acid stomachic environment and to act in the drug release, and mucoadhesive systems, which allow the pharmaceutical form remains a greater time interval in the intestine, increasing the effectiveness of the drug. Cellulose triacetate (CTA) films were produced from cellulose extracted from sugar cane bagasse. The films were prepared with different morphologies (with and without water, acting as non-solvent) and concentrations (3, 6.5 and 10%) of CTA and characterized using scanning electron microscopy (SEM), water vapor permeability (WVP), puncture resistance (PR), enzymatic digestion (DE), and mucoadhesive force evaluation (MF). Microscopy showed the formation of symmetric and asymmetric morphologies. WVP data showed that more concentrated films have higher values for WVP; moreover, asymmetric films had higher values than symmetric films. PR measurements showed that symmetric membranes are more resistant than asymmetric ones. More concentrated films were also more puncture resistant, except for symmetric membranes with CTA concentrations of 6.5 and 10% that did not show significant differences. All of the films presented large mucoadhesive capacities independent of their morphology and CTA concentration. From the results of WVP and RP, a symmetric filme with 6.5% CTA showed better ability and mechanical resistance, therefore, was selected to serve as coating of gellan gum (GG) particles incorporating ketoprofen (KET), which was confirmed by SEM. The selected film presented low values in measurements of the swelling index (SI) and in a dissolution test (DT). TGA analysis showed that the CTA coating does not influence the thermal stability of the particles and there is no incompatibility evidence between CTA, GG and KET. Coated particles released 100% of the ketoprofen in 24 h, while uncoated particles released the same amount in 4 h. The results of this study highlight the potential of CTA in the development of new controlled oral delivery systems.

Desempenho de soja associado à posição do fertilizante e tamanho de sementes

The seed size used for seeding has caused doubts among soybean producers. The study aimed to determine whether there may be differences between seed size with respect to depth of fertilizer deposition. The field experiment was conducted at the Experimental Area UTFPR Campus Pato Branco, using a precision seeder for direct seeding. The design was a randomized blocks, with five repetitions. The treatments were composed by the combination of two seed sizes (large seed with 6,5 mm and 5,5 mm with small seed) and two fertilizer deposition depths in relation to the seed (fertilizer near the seed with about 3 cm away and fertilizer distant from the seeds with about 10 cm). Data were subjected to analysis of variance. When the test value F was significant at 5% probability was applied to the Duncan test for comparison of means. The shallower depth of fertilizer deposition provided larger number of pods per plant and increased number of grains per plant. Already the largest depth of fertilizer deposition provided greater plant height at 30 days after sowing and R2 stage, greater ground area mobilized, higher plant population in all periods, greater depth of deposition of seeds and a higher rate of emergency speed.

Características químicas do solo e desempenho de culturas após quatro anos de aplicações de cama de aviário em diferentes épocas e níveis

Due to the high supply and its attractive cost, the poultry litter has been used in the southwestern region of Parana to the improvement of soil fertility seeking greater production of grains and pastures. However, the use without technical knowledge can minimize the benefits of poultry litter or even cause undesirable effects on soil, environmental pollution and also productivity losses in the used crops. The objective of this study was to evaluate the influence of different times of poultry litter application, predating the winter crop, associated with increasing levels, about soil chemical properties, release of nutrients and crop performances in four consecutive years (2011-2014). In the first three years the experimental design was randomized blocks with a split plot system and four replications. In the main plots were tested four poultry litter application times preceding the wheat production: 0, 15, 30 and 45 days before sowing (DAS); in the subplots were applied four poultry litter levels (wet basis): 0, 4, 8 and 12 Mg ha-1. Last year one more subdivision of plots was done, evaluating the use or not of nitrogen in coverage in wheat, at a dose of 100 kg N ha-1. The wheat cultivar used in the four years was the BRS 220. In three years it was evaluated the residual effect on soybean production (cultivar - BMX Turbo RR) and in one year on the beans. The chemical soil attributes were evaluated at four depths 0-2,5cm, 2,5-5cm, 5-10cm and 10-20cm, and also the rate of decomposition and nutrient release of poultry litter and the crop productivity. The different times of application concerning the poultry litter had little influence on the studied variables, demonstrating that the producer does not need to have a specific date (before planting) to the application of poultry litter. Potassium was fully released 60 days after the allocation of litter bags into the field; for nitrogen and phosphorus the release was slower. The use of increasing levels of poultry litter increased the levels of various soil elements, highlighting the potassium which reached 20 cm deep in the second year of evaluation. The increase in pH and in the base saturation occurred only in the upper layers, while the phosphorus reached 10 cm deep in the third year of the study. It was observed increased pH and base saturation. The use of increasing doses of poultry litter contributed to the wheat plant nutrition, significantly increasing the weight of a thousand grains, and the grain yield of wheat in all the evaluated years; the nitrogen fertilization in coverage also had significant effect for the fourth evaluated year. Also there was a significant response from the residual effect of poultry litter for crops planted in summer for both soybeans and beans.

Estudo da influência da morfologia de nanopartículas de sílica mesoporosa na liberação do anticancerígeno indol-3-carbinol

Dissertação (mestrado)—Universidade de Brasília, Faculdade de Ceilândia, Programa de Pós-graduação em Ciências e Tecnologias em Saúde, 2015.

Cómo va la economía del mundo : la recuperación se hace más lenta y el proteccionismo golpea

Fondo Margaritainés Restrepo

Interação de microorganismos na solubilização de fósforo e potássio de rochas para produção de biofertilizantes

he present model of agriculture is based on intensive use of industrial inputs, due to its rapid response, but it brings harmful consequences to the environment, and it is necessary the use of modern inputs. And an alternative is the use of rock biofertilizers in agriculture, a product easy to use, with higher residual effect and does not harm the environment. The objective of study was to evaluate the inoculation and co-inoculation of different microorganisms in the solubilization of rock phosphate and potash ground microbial evaluating the best performance in the production of biofertilizers comparing with rocks pure in soil chemical properties and, verify effect of inoculation of the bacterium Paenibacillus polymyxa in the absorption of minerals dissolved in the development of cowpea (Vigna unguiculata [L.] Walp.). The first bioassay was conducted in Laboratory (UFRN) for 72 days in Petri dishes, where the rock powder was increased by 10% and sulfur co-inoculated and inoculated with bacterial suspension of Paenibacillus polymyxa grown in medium tryptone soy broth, Ralstonia solanacearum in medium Kelman, Cromobacterium violaceum in medium Luria-Bertani and Acidithiobacillus thiooxidans in medium Tuovinen and Kelly,and fungi Trichoderma humatum and Penicillium fellutanum in malt extract. Every 12 days, samples were removed in order to build up the release curve of minerals. The second bioassay was conducted in a greenhouse of the Agricultural Research Corporation of Rio Grande do Norte in experimental delineation in randomized block designs, was used 10 kg of an Yellow Argissolo Dystrophic per pot with the addition of treatments super phosphate simple (SS), potassium chloride (KCl), pure rock, biofertilizers in doses 40, 70, 100 and 200% of the recommendation for SS and KCl, and a control, or not inoculated with bacteria P. polymyxa. Were used seeds of cowpea BRS Potiguar and co-inoculated with the bacterial suspension of Bradyrhizobium japonicum and P. polymyxa. The first crop was harvested 45 days after planting, were evaluated in the dry matter (ADM), macronutrients (N, P, K, Ca, Mg) and micronutrients (Zn, Fe, Mn) in ADM. And the second at 75 days assessing levels of macro end micronutrients in plants and soil, and the maximum adsorption capacity of P in soil. The results showed synergism in co-inoculations with P. polymyxa+R. solanacearum and, P. polymyxa+C. violaceum solubilizations providing higher P and K, respectively, and better solubilization time at 36 days. The pH was lower in biofertilizers higher doses, but there was better with their addition to P at the highest dose. Significant reduction of maximum adsorption capacity of phosphorus with increasing dose of biofertilizer. For K and Ca was better with SS+KCl, and Mg to pure rock. There was an effect of fertilization on the absorption, with better results for P, K and ADM with SS+KCL, and N, Ca and Mg for biofertilizers. Generally, the P. polymyxa not influence the absorption of the elements in the plant. In treatments with the uninoculated P. polymyxa chemical fertilizer had an average significantly higher for weight and number of grains. And in the presence of the bacteria, biofertilizers and chemical fertilizers had positive values in relation to rock and control. The data show that the rocks and biofertilizers could meet the need of nutrients the plants revealed as potential for sustainable agriculture

Nanopartículas de alginato como sistema de liberação para o herbicida clomazone

In this paper, we describe the preparation of alginate nanoparticles as a delivery system for the herbicide clomazone. Two different methods were investigated and characterized by size distribution, zeta potencial, pH and in vitro release. The alginate/AOT nanoparticles had higher rates of association of the herbicide clomazone than alginate/chitosan nanoparticles. Clomazone release profile, showed a significant difference in release behavior of pure herbicide in solution when compared with herbicide loaded in both alginate nanoparticles. This study is important to construct a biodegradable release system using herbicide for later release into more specific targets, avoiding contamination of environmental matrices.

Implicações do uso de lodo de esgoto como fertilizante em culturas anuais: acidez do solo.

A utilização de lodo de esgoto na agricultura traz o benefício da reciclagem da energia (representada pela matéria orgânica) e dos nutrientes nele contidos, em especial o nitrogênio, pelo seu valor econômico. E traz como riscos a possibilidade de contaminação ambiental com nitrato, metais pesados e, ou produtos orgânicos tóxicos. Em solos com pH próximos à neutralidade a solubilidade de elementos tóxicos às plantas ou aos animais é baixa, e ocorrem condições biológicas favoráveis à decomposição do resíduo. No entanto, a mineralização dos lodos de esgoto induz à acidificação do solo, devido principalmente à formação de ácidos orgânicos e à ocorrência de reações de nitrificação. Por estas razões a acidez deve ser monitorada, com o objetivo de verificar quando é necessária a calagem. Considerando-se estes aspectos, apresentam-se neste trabalho dados de pH de experimento conduzido em campo, com duas aplicações sucessivas de lodo de esgoto, em dois cultivos de milho. Avaliaram-se duas doses do resíduo, um de origem urbana e outro de origem urbano-industrial. A quantidade de lodo a aplicar foi calculada em função do N potencialmente disponível às plantas e da recomendação agronômica de adubação nitrogenada para milho, critério utilizado por órgãos ambientais para evitar lixiviação de nitrato no perfil do solo; estudando-se também o dobro dessa dose. Os resultados evidenciaram diferentes potenciais de acidificação para os dois lodos de esgoto. Na primeira aplicação, o lodo de esgoto urbano acidificou o solo na dose recomendada (1N) e na dose 2N; o lodo de esgoto urbano-industrial acidificou o solo somente na dose 2N. A reaplicação dos dois lodos acidificou o solo, tanto na dose recomendada quanto no dobro da mesma. Verificou-se, assim, que o potencial acidificante do lodo de Franca pode ser um fator mais restritivo que o teor de N quando se calculam doses ambientalmente seguras a aplicar em solos.

Aspectos morfológicos y autoafines de las superficies de fractura lenta en el vidrio

El presente trabajo es un estudio del comportamiento autoafín de la superficies de factura en un vidrio sódico-cálcico.

Citotoxicidade de curcumina presente em nanoparticulas de quitosana/sultato de condroitina contendo lecitina

Dissertação (mestrado)–Universidade de Brasília, Universidade UnB de Planaltina, Programa de Pós-Graduação em Ciência de Materiais, 2015.