Polímeros sintéticos biodegradáveis: matérias-primas e métodos de produção de micropartículas para uso em drug delivery e liberação controlada

Micropartículas produzidas a partir de polímeros sintéticos têm sido amplamente utilizadas na área farmacêutica para encapsulação de princípios ativos. Essas micropartículas apresentam as vantagens de proteção do princípio ativo, mucoadesão e gastrorresistência, melhor biodisponibilidade e maior adesão do paciente ao tratamento. Além disso, utiliza menores quantidade de princípio ativo para obtenção do efeito terapêutico proporcionando diminuição dos efeitos adversos locais, sistêmicos e menor toxidade. Os polímeros sintéticos empregados na produção das micropartículas são classificados biodegradáveis ou não biodegradáveis, sendo os biodegradáveis mais utilizados por não necessitam ser removidos cirurgicamente após o término de sua ação. A produção das micropartículas poliméricas sintéticas para encapsulação tanto de ativos hidrofílicos quanto hidrofóbicos pode ser emulsificação por extração e/ou evaporação do solvente; coacervação; métodos mecânicos e estão revisados neste artigo evidenciando as vantagens, desvantagens e viabilidade de cada metodologia. A escolha da metodologia e do polímero sintético a serem empregados na produção desse sistema dependem da aplicação terapêutica requerida, bem como a simplicidade, reprodutibilidade e factibilidade do aumento de escala da produção.

Efeitos da administração de monensina por meio de cápsulas de liberação controlada no desempenho de vacas Holandesas no início da lactação

Com o objetivo de estudar o efeito da monensina sobre a produção e composição de leite, a contagem de células somáticas, a condição corporal e os parâmetros sangüíneos e reprodutivos de vacas da raça Holandesa de alta produção no início de lactação, foram utilizadas 44 vacas com produção diária de 33,44 ± 4,93 litros de leite, em delineamento inteiramente casualizado, com dois tratamentos: um controle (C) e outro com cápsulas de liberação controlada de monensina com eficácia de 100 dias (300 mg/vaca/dia). A administração individual de monensina foi realizada 30 dias antes da data provável do parto. A monensina não alterou a produção, a composição do leite e a contagem de células somáticas do leite nem a condição corporal e a concentração de glicose e BHBA (beta-hidroxibutirato) no soro das vacas, no entanto, diminuiu a concentração de AGNE (ácidos graxos não-esterificados) no soro das vacas com 60 dias de lactação. O período de serviço e o número de serviços por concepção não diferiram entre os tratamentos, porém, a administração de monensina diminuiu o número de animais que apresentaram retenção de placenta e laminite. A administração de monensina para vacas Holandesas de alta produção no início de lactação não modifica a produção e a composição do leite, contudo, diminui a concentração de AGNE 60 dias após o parto e a incidência de laminite e retenção de placenta nas vacas no pós-parto.

Hidróxidos duplos lamelares: nanopartículas inorgânicas para armazenamento e liberação de espécies de interesse biológico e terapêutico

Studies about the inorganic nanoparticles applying for non-viral release of biological and therapeutic species have been intensified nowadays. This work reviews the preparation strategies and application of layered double hydroxides (LDH) as carriers for storing, carrying and control delivery of intercalated species as drugs and DNA for gene therapy. LDH show low toxicity, biocompatibility, high anion exchange capacity, surface sites for functionalization, and a suitable equilibrium between chemical stability and biodegradability. LDH can increase the intercalated species stability and promote its sub-cellular uptake for biomedical purposes. Concerning the healthy field, LDH have been evaluated for clinical diagnosis as a biosensor component.

Importância da hidrodinâmica na cinética de flotação de partículas grossas

The processes that govern the rate of particle recovery in a flotation cell include the following sub-processes: collision, attachment, and stability of the aggregate formed by particles and bubbles. Collision is controlled by bulk hydrodynamics inside the flotation cell, while attachment is largely dominated by variables that belong to the domain of surface chemistry (contact angle, induction time). As for the stability of the particle/bubble aggregate, its efficiency depends on both hydrodynamics plus surface chemistry variables of the system. The flotation recovery of coarse particles of apatite and glass spheres was measured by micro-flotation and batch flotation tests in which hydrodynamic parameters were evaluated, such as impeller rotational speed, diameter, and geometry, as well as particle size and density. Results revealed that a proper impeller rotational speed yielded turbulence levels, which enabled to keep particles fully suspended, this way optimizing the collision efficiency between particles and bubbles, without jeopardizing the stability of the particle-bubble aggregates.

Fluoride release profile of a nanofilled resin-modified glass ionomer cement

The present study aimed to compare the fluoride (F-) release pattern of a nanofilled resin-modified glass ionomer cement (GIC) (Ketac N100 - KN) with available GICs used in dental practice (resin-modified GIC - Vitremer - V; conventional GIC - Ketac Molar - KM) and a nanofilled resin composite (Filtek Supreme - RC). Discs of each material (n=6) were placed into 4 mL of deionized water in sealed polyethylene vials and shaken, for 15 days. F- release (μg F-/cm²) was measured each day using a fluoride-ion specific electrode. Cumulative F- release means were statistically analyzed by linear regression analysis. In order to analyze the differences among materials and the influence of time in the daily F- release, 2-way ANOVA test was performed (α=0.05). The linear fits between the cumulative F- release profiles of RC and KM and time were weak. KN and V presented a strong relationship between cumulative F- release and time. There were significant differences between the daily F- release overtime up to the third day only for GICs materials. The daily F- release means for RC were similar overtime. The results indicate that the F- release profile of the nanofilled resin-modified GIC is comparable to the resin-modified GIC.

Dopamina, óxido nítrico e suas interações em modelos para o estudo da esquizofrenia

Modelos experimentais baseados no aumento da neurotransmissão dopaminérgica mimetizam aspectos comportamentais e neuroquímicos característicos da esquizofrenia. Psicoestimulantes, como a anfetamina, são utilizados com esta finalidade, pois aumentam os níveis de dopamina extracelular nas vias mesocorticolímbica e mesoestriatal. As limitações da manipulação direta do sistema dopaminérgico nos modelos animais incentivam abordagens complementares. O óxido nítrico (NO), um neurotransmissor atípico que inibe a recaptação de dopamina e estimula sua liberação, parece modular comportamentos controlados pelo sistema dopaminérgico. O teste de inibição pré-pulso revela uma deficiência no filtro sensório-motor, verificada em esquizofrênicos ou após tratamentos com psicotomiméticos, podendo ser prevenida pela inibição do NO. Esta revisão apresenta evidências da interação do NO com o sistema dopaminérgico em modelos para o estudo da esquizofrenia como uma nova ferramenta de investigação desta patologia.

Study of the equatorial Atlantic Ocean mixing layer using a one-dimensional turbulence model

The General Ocean Turbulence Model (GOTM) is applied to the diagnostic turbulence field of the mixing layer (ML) over the equatorial region of the Atlantic Ocean. Two situations were investigated: rainy and dry seasons, defined, respectively, by the presence of the intertropical convergence zone and by its northward displacement. Simulations were carried out using data from a PIRATA buoy located on the equator at 23º W to compute surface turbulent fluxes and from the NASA/GEWEX Surface Radiation Budget Project to close the surface radiation balance. A data assimilation scheme was used as a surrogate for the physical effects not present in the one-dimensional model. In the rainy season, results show that the ML is shallower due to the weaker surface stress and stronger stable stratification; the maximum ML depth reached during this season is around 15 m, with an averaged diurnal variation of 7 m depth. In the dry season, the stronger surface stress and the enhanced surface heat balance components enable higher mechanical production of turbulent kinetic energy and, at night, the buoyancy acts also enhancing turbulence in the first meters of depth, characterizing a deeper ML, reaching around 60 m and presenting an average diurnal variation of 30 m.

Hydrometeor and latent heat profiles of tropical cyclones Conson, Ivan and Catarina using PR/TRMM data

ABSTRACT Microphysical and thermodynamical features of two tropical systems, namely Hurricane Ivan and Typhoon Conson, and one sub-tropical, Catarina, have been analyzed based on space-born radar PR measurements available on the TRMM satellite. The procedure to classify the reflectivity profiles followed the Heymsfield et al (2000) and Steiner et al (1995) methodologies. The water and ice content have been calculated using a relationship obtained with data of the surface SPOL radar and PR in Rondonia State in Brazil. The diabatic heating rate due to latent heat release has been estimated using the methodology developed by Tao et al (1990). A more detailed analysis has been performed for Hurricane Catarina, the first of its kind in South Atlantic. High water content mean value has been found in Conson and Ivan at low levels and close to their centers. Results indicate that hurricane Catarina was shallower than the other two systems, with less water and the water was concentrated closer to its center. The mean ice content in Catarina was about 0.05 g kg-1 while in Conson it was 0.06 g kg-1 and in Ivan 0.08 g kg-1. Conson and Ivan had water content up to 0.3 g kg-1 above the 0ºC layer, while Catarina had less than 0.15 g kg-1. The latent heat released by Catarina showed to be very similar to the other two systems, except in the regions closer to the center.

Gametogenesis in Madracis decactis Lyman, 1859 (Cnidaria, Scleractinia) from Ilha Grande Bay (Rio de Janeiro), southeastern Brazil

Collections were made every two months in Ilha Grande Bay, Rio de Janeiro, for 21 months (August/2004-May/2006) to study the gametogenesis of Madracis decactis Lyman, 1859. A total of 1800 polyps were examined using standard histological techniques. Madracis decactis is a hermaphroditic species whose male and female gametes develop within different mesenteries. Oogenesis begins in October, while spermatogenesis begins at the end of February, both reaching maturity at the end of April. The peak of reproductive activity occurred between February and April, when all the polyps were fertile, containing mainly stage III oocytes. Examination of fertile polyps indicated the simultaneous presence of stages I, II and III for oogenesis and I, II, III and IV for spermatogenesis. No embryos or planulae were observed in the histological sections. The gametes or planulae spawning may occur between April and May.

Hormônio do crescimento e exercício físico: considerações atuais

Embora o hormônio do crescimento (GH) seja um dos hormônios mais estudados, vários de seus aspectos fisiológicos ainda não estão integralmente esclarecidos, incluindo sua relação com o exercício físico. Estudos mais recentes têm aumentado o conhecimento a respeito dos mecanismos de ação do GH, podendo ser divididos em: 1) ações diretas, mediadas pela rede de sinalizações intracelulares, desencadeadas pela ligação do GH ao seu receptor na membrana plasmática; e 2) ações indiretas, mediadas principalmente pela regulação da síntese dos fatores de crescimento semelhantes à insulina (IGF). Tem sido demonstrado que o exercício físico é um potente estimulador da liberação do GH. A magnitude deste aumento sofre influência de diversos fatores, em especial, da intensidade e do volume do exercício, além do estado de treinamento. Atletas, normalmente, apresentam menor liberação de GH induzida pelo exercício que indivíduos sedentários ou pouco treinados. Evidências experimentais demonstram que o GH: 1) favorece a mobilização de ácidos graxos livres do tecido adiposo para geração de energia; 2) aumenta a capacidade de oxidação de gordura e 3) aumenta o gasto energético.

Enzyme kinetics, structural analysis and molecular modeling studies on a series of Schistosoma mansoni PNP inhibitors

The enzyme purine nucleoside phosphorylase from Schistosoma mansoni (SmPNP) is an attractive molecular target for the development of novel drugs against schistosomiasis, a neglected tropical disease that affects about 200 million people worldwide. In the present work, enzyme kinetic studies were carried out in order to determine the potency and mechanism of inhibition of a series of SmPNP inhibitors. In addition to the biochemical investigations, crystallographic and molecular modeling studies revealed important molecular features for binding affinity towards the target enzyme, leading to the development of structure-activity relationships (SAR).

Time resolved emission spectroscopy of poly(2,5-dicyano-p-phenylene-vinylene) films

Films of poly (2,5-dicyano-p-phenylene vinylene), DCNPPV, were obtained by electrochemical synthesis over gold thin layer (20 nm) transparent electrode deposited on a glass plate. The DCNPPV films of 4 µm thickness were produced by electropolymerization process of α,α,α',α'-tetrabromo-2-5-dicyano-p-xilene at different applied potentials (-0.15, -0.25, -0.40, -0.60, -0.80, and -1.0 V) using 0.1 mol L-1 of tetraethylammonium bromide in acetonitrile as the supporting electrolyte. The emission decays have three exponential components: a fast component in the picosecond range (200-400 ps), and two other of about one and five nanoseconds at 293 K. The fluorescence quenching process seems to occur by exciton trapping in a low-energy site and quenching by residual bromine monomer attached at the end of the polymer chain. However, the electrochemical synthesis generates entrapped bromide or ion pairs during the growth step of the film which also contributes to the deactivation. The change of the electrolyte from bromide to perchlorate reduces significantly this additional quenching effect by allowing ion exchange of formed bromide with the nonquenching perchloride anion.

Enzymatic kinetic resolution of (RS)-1-(Phenyl)ethanols by Burkholderia cepacia lipase immobilized on magnetic nanoparticles

Lipase from Burkholderia cepacia immobilized on superparamagnetic nanoparticles using adsorption and chemisorption methodologies was efficiently applied as recyclable biocatalyst in the enzymatic kinetic resolution of (RS)-1-(phenyl)ethanols via transesterification reactions. (R)-Esters and the remaining (S)-alcohols were obtained with excellent enantiomeric excess (> 99%), which corresponds to a perfect process of enzymatic kinetic resolution (conversion 50%, E > 200). The transesterification reactions catalysed with B. cepacia lipase immobilized by the glutaraldehyde method showed the best results in terms of reusability, preserving the enzyme activity (conversion 50%, E > 200) for at least 8 successive cycles.

Conducting polymer- hydrogel blends for electrochemically controlled drug release devices

Blends formed by electrochemical polymerization of polypyrrole (PPy) into polyacrylamide (PAAm) hydrogels were used as devices for controlled drug release. The influence of several parameters in the synthesis, such as type of hydrogel matrix and polymerization conditions was studied by using a fractional factorial design. The final goal was to obtain an adequate device for use in controlled release tests, based on electrochemical potential control. For controlled release tests, Safranin was used as model drug and release curves (amount of drug vs. time) have shown that these blends are promising materials for this use. The optimized blends obtained were characterized by cyclic voltammetry and Raman spectroscopy.

Thermal behavior and decomposition kinetics of rifampicin polymorphs under isothermal and non-isothermal conditions

The thermal behavior of two polymorphic forms of rifampicin was studied by DSC and TG/DTG. The thermoanalytical results clearly showed the differences between the two crystalline forms. Polymorph I was the most thermally stable form, the DSC curve showed no fusion for this species and the thermal decomposition process occurred around 245 ºC. The DSC curve of polymorph II showed two consecutive events, an endothermic event (Tpeak = 193.9 ºC) and one exothermic event (Tpeak = 209.4 ºC), due to a melting process followed by recrystallization, which was attributed to the conversion of form II to form I. Isothermal and non-isothermal thermogravimetric methods were used to determine the kinetic parameters of the thermal decomposition process. For non-isothermal experiments, the activation energy (Ea) was derived from the plot of Log β vs 1/T, yielding values for polymorph form I and II of 154 and 123 kJ mol-1, respectively. In the isothermal experiments, the Ea was obtained from the plot of lnt vs 1/T at a constant conversion level. The mean values found for form I and form II were 137 and 144 kJ mol-1, respectively.