Modificação de membranas de quitosana por plasma para uso biológico

Chitosan membranes have been modified by plasma, utilizing the following gases: nitrogen (N2), methane (CH4), argon (Ar), oxygen (O2) and hydrogen. The modified membranes by plasma were compared to the unmodified ones. The membranes were characterized by absorption assay, contact angle, atomic force microscopy (AFM). Also, permeability assay of sodium sulfamerazine from such membranes were carried out. Through the absorption assay and contact angle it was possible to obtain information of the wettability of the membranes and what changes the plasma treatment can promote in relation to it. The plasma treatment using oxygen promoted increase of the wetability and swelling while the samples treated with methane decrease of the wetability and swelling. Through the Optical Emission Spectroscopy (OES) it was possible to identify which species were present in the plasma during the treatment. And through the AFM analysis it was possible to observe the changes nanotopography occurred on the surface of the samples. Permeability assay were archived for all treated membranes and compared to no treated ones. Due to that assay it was possible verify which the plasma treatment increased the permeability spectrum of the membranes which has varied from 1,4548 *10-5cm2.min-1 to 2,7713*10-5cm2.min-1. Chitosan membranes with permeability varied are importance in systems drug delivery, to liberate a wide variety of drugs

Desenvolvimento de uma formulação cólon específica visando o tratamento da colite ulcerativa

Micro and nanoparticulate systems as drug delivery carriers have achieved successful therapeutic use by enhancing efficacy and reducing toxicity of potent drugs. The improvement of pharmaceutical grade polymers has allowed the development of such therapeutic systems. Microencapsulation is a process in which very thin coatings of inert natural or synthetic polymeric materials are deposited around microsized particles of solids or around droplets. Products thus formed are known as microparticles. Xylan is a natural polymer abundantly found in nature. It is the most common hemicellulose, representing more than 60% of the polysaccharides existing in the cell walls of corn cobs, and is normally degraded by the bacterial enzymes present in the colon of the human body. Therefore, this polymer is an eligible material to produce colon-specific drug carriers. The aim of this study was to evaluate the technological potential of xylan for the development of colon delivery systems for the treatment of inflammatory bowel diseases. First, coacervation was evaluated as a feasible method to produce xylan microcapsules. Afterwards, interfacial cross-linking polymerization was studied as a method to produce microcapsules with hydrophilic core. Additionally, magnetic xylan-coated microcapsules were prepared in order to investigate the ability of producing gastroresistant systems. Besides, the influence of the external phase composition on the production and mean diameter of microcapsules produced by interfacial cross-linking polymerization was investigated. Also, technological properties of xylan were determined in order to predict its possible application in other pharmaceutical dosage forms

Nanopartículas de alginato como sistema de liberação para o herbicida clomazone

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

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

Micropartículas poliméricas à base de xilana e Eudragit® S-100 contendo mesalazina visando à liberação cólon-específica

Colon-specific drug delivery systems have attracted increasing attention from the pharmaceutical industry due to their ability of treating intestinal bowel diseases (IBD), which represent a public health problem in several countries. In spite of being considered a quite effective molecule for the treatment of IBD, mesalazine (5-ASA) is rapidly absorbed in the upper gastrointestinal tract and its systemic absorption leads to risks of adverse effects. The aim of this work was to develop a microparticulate system based on xylan and Eudragit® S- 100 (ES100) for colon-specific delivery of 5-ASA and evaluate the interaction between the polymers present in the systems. Additionaly, the physicochemical and rheological properties of xylan were also evaluated. Initially, xylan was extracted from corn cobs and characterized regarding the yield and rheological properties. Afterwards, 10 formulations were prepared in different xylan and ES100 weight ratios by spray-drying the polymer solutions in 0.6N NaOH and phosphate buffer pH 7.4. In addition, 3 formulations consisting of xylan microcapsules were produced by interfacial cross-linking polymerization and coated by ES100 by means of spray-drying in different polymer weight ratios of xylan and ES100. The microparticles were characterized regarding yield, morphology, homogeneity, visual aspect, crystallinity and thermal behavior. The polymer interaction was investigated by infrared spectroscopy. The extracted xylan was presented as a very fine and yellowish powder, with mean particle size smaller than 40μm. Regarding the rheological properties of xylan, they demonstrated that this polymer has a poor flow, low density and high cohesiveness. The microparticles obtained were shown to be spherical and aggregates could not be observed. They were found to present amorphous structure and have a very high thermal stability. The yield varied according to the polymer ratios. Moreover, it was confirmed that the interaction between xylan and ES100 occurs only by means of physical aggregation

Micropartículas de poli (ácido lático-co-ácido glicólico) obtidas por spray drying para a liberação prolongada de metotrexato

Methotrexate (MTX) is a drug used in the chemotherapy of some kind of cancers, autoimmune diseases and non inflammatory resistant to corticosteroids uveits. However, the rapid plasmatic elimination limits its therapeutic success, which leads to administration of high doses to maintain the therapeutic levels in the target tissues, occurring potential side effects. The aim of this study was to obtain spray dried biodegradable poly-lactic acid co-glycolic acid (PLGA) microparticles containing MTX. Thus, suitable amounts of MTX and PLGA were dissolved in appropriate solvent system to obtain solutions at different ratios drug/polymer (10, 20, 30 and 50% m/m). The physicochemical characterizing included the quantitative analysis of the drug using a validate UV-VIS spectrophotometry method, scanning electron microscopy (SEM), infrared spectrophotometry (IR), thermal analyses and X-ray diffraction analysis. The in vitro release studies were carried out in a thermostatized phosphate buffer pH 7.4 (0.05 M KH2PO4) medium at 37°C ± 0.2 °C. The in vitro release date was subjected to different kinetics release models. The MTX-loaded PLGA microparticles showed a spherical shape with smooth surface and high level of entrapped drug. The encapsulation efficiency was greater then 80%. IR spectroscopy showed that there was no chemical bond between the compounds, suggesting just the possible occurrence of hydrogen bound interactions. The thermal analyses and X-ray diffraction analysis shown that MTX is homogeneously dispersed inside polymeric matrix, with a prevalent amorphous state or in a stable molecular dispersion. The in vitro release studies confirmed the sustained release for distinct MTX-loaded PLGA microparticles. The involved drug release mechanism was non Fickian diffusion, which was confirmed by Kornmeyer-Peppas kinetic model. The experimental results demonstrated that the MTX-loaded PLGA microparticles were successfully obtained by spray drying and its potential as prolonged drug release system.

Preparação e caracterização de sistemas emulsionados contendo benznidazol

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior

Avaliação citológica em base líquida de fármacos moduladores estrogênicos

Hormone therapy is an important tool in the treatment of breast cancer and tamoxifen represents one of the most important drugs used in this type of treatment. Recently other drugs based on the inhibition of aromatase had been developed, this enzyme is responsible for the synthesis of estrogenic esteroids from the androgenic ones. The objective of this study would be the development of a quantitative cytological model of murine estral analysis that allowed the characterization of different hormone drugs effect over vaginal epithelium. The technique of monochromatic staining with Evans blue (C.I. 23860) showed to be efficient in the qualitative and quantitative classification of the cycle. It had been observed differences in the cytological standard of animals submitted to the studied drugs; tamoxifen presented a widening of phases of lesser maturation (diestrais), while anastrozole and exemestane increased the duration of the phases of larger maturation (estrais). The data were analysed through a cubical non linear regression (spline) which allowed a better characterization of the drugs, suggesting a proper cytological profile to the antagonism of the estrogen receptor (tamoxifen), aromatase competition (anastrozole) and inhibition of the enzyme (exemestane)

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

Estudo da população microbiana e da liberação de amônia da cama de frangos tratada com gesso agrícola

O presente trabalho foi realizado com o objetivo de avaliar a população microbiana (contagem padrão) e a liberação de amônia da cama de frangos de maravalha tratada com gesso agrícola, durante o ciclo de criação das aves. Foram utilizados 1440 pintos de um dia para corte, criados em galpão convencional dividido em boxes, sob densidade de nove aves/m². Os dados das variáveis analisadas foram coletados no início, no 25º dia e ao final do experimento (49º dia de vida). O delineamento experimental adotado foi o inteiramente ao acaso, com a distribuição de nove tratamentos em esquema fatorial 4 × 2 + 1 (níveis de gesso × formas de aplicação), com quatro repetições e 40 aves por parcela. Os resultados evidenciaram a capacidade inibidora do gesso na volatilização de amônia da cama de frangos no 25º dia e ao final do experimento, principalmente para a aplicação parcelada, implicando no decréscimo da contagem padrão de microrganismos.

Deterioração controlada em sementes de beterraba

O uso de testes de vigor é fundamental na avaliação do potencial fisiológico de sementes produzidas e comercializadas. O trabalho foi realizado com o objetivo de estudar o uso do teste de deterioração controlada na avaliação do potencial fisiológico de sementes de beterraba. Após lavagem dos frutos contendo as sementes em água corrente, oito lotes da cultivar Top Tall Early Wonder foram previamente avaliados pelos testes de germinação e de emergência de plântulas (EP). Para o ajuste do teor de água (TA) foram estudados os métodos de atmosfera úmida (AU) e substrato úmido (SU). O teste de deterioração controlada (DC) foi conduzido com 22 e 24% de água e exposição durante 12, 24 e 36 horas à temperatura de 45 ºC. Usou-se o delineamento experimental inteiramente casualizado, com oito repetições de 25 sementes, exceto o de EP, conduzido com quatro repetições de 50 sementes. Os dados foram analisados separadamente para cada combinação TA x períodos de deterioração e as médias comparadas usando-se o teste de Tukey (P<0,05). Análises de correlação simples foram estabelecidas entre os resultados dos testes de laboratório e a EP. O ajuste do TA de semente deve ser feito pelo método do SU. O teste de DC pode ser utilizado para avaliar o potencial fisiológico de sementes de beterraba, sendo indicada a combinação TA de 22%, a 45ºC, durante 24 horas.

Deterioração controlada para avaliar o potencial fisiológico de sementes de beterraba

Sementes de hortaliças quase sempre apresentam elevado valor comercial, motivo pelo qual devem ter o potencial fisiológico eficientemente avaliado. O teste de deterioração controlada é um dos recomendados para avaliação do vigor de sementes pequenas, como as de beterraba. O objetivo do trabalho foi determinar o melhor procedimento para a condução de referido teste em sementes de beterraba e sua relação com a emergência de plântulas em campo. Foram utilizados sete lotes de sementes da cultivar Top Tall Early Wonder, adquiridos no comércio. Após lavagem em água corrente, as sementes foram submetidas aos testes de germinação, velocidade de germinação, envelhecimento acelerado, emergência de plântulas em campo, velocidade de emergência e deterioração controlada (temperaturas de 41 e 45ºC, teores de água de 22, 24 e 26% e períodos de exposição de 12, 24 e 36 horas). As combinações 41ºC/24%/12 h, 41ºC/24%/36 h, 41ºC/26%/36 h e 45ºC/24%/24 h apresentaram potencial para uso na avaliação do vigor de sementes de beterraba. No entanto, sob as combinações de 41°C/24%/12 h ou 45°C/24%/24 h reduziu-se o tempo de condução do teste.

Sequências de culturas em sistema de semeadura direta: II - decomposição e liberação de nutrientes na entressafra

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Decomposição e liberação de nitrogênio de resíduos culturais de plantas de cobertura em um solo de cerrado

A produção de massa seca, a taxa de decomposição e a liberação de nitrogênio (N) foram avaliadas em um experimento com sete tipos de cobertura vegetal: milheto pérola (Pennisetum americanum sin. tiphoydes), braquiária (Brachiaria brizantha), sorgo forrageiro (Sorghum bicolor L. Moench), guandu (Cajanus cajan (L.) Millsp), crotalária juncea (Crotalarea juncea) e aveia-preta (Avena strigosa Schreb), em pousio e em área de cultivo convencional (testemunha), em solo de cerrado, em Uberaba, região do Triângulo Mineiro. Dentre as coberturas avaliadas, o milheto e a crotalária foram as que apresentaram a maior produção de massa seca, maior acúmulo e a maior liberação de N. A braquiária foi a cobertura que apresentou a maior taxa de decomposição. Todas as coberturas apresentaram a maior taxa de liberação de N até 42 dias após dessecação.