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Synthesis and evaluation of selected benzimidazole derivatives as potential antimicrobial agents. An investigation into the synthesis of substituted benzimidazoles and their evaluation in vitro for antimicrobial activity.Alasmary, Fatmah A.S. January 2013 (has links)
Microbe resistence is a serious issue, especially as they have become resistant to
most well known drugs. Therefore this is considered as a global problem and is now
dealt with at a poitical level. Since no new classes of antimicrobial agents have
been discovered in the past three deacdes, the development of new drugs is
extremely urgent. Therefore the aim of this project was to synthesise derivatives of
benzimidazole, and then assesses their antimicrobial activities in vitro by using disc
(well) diffusion and MICs tests.
A total of 69 benzimidazole derivatives, with substituents at positions 1, 2, and 5,
were synthesised, characterised and tested against selected bacteria and fungi. In
addition, six bezimidazole silver complexes were prepared and evaluated for their
antimicrobial behavior.
The SAR showed that the antimicrobial activity of the compounds depended on the
substituents attached to the bicyclic heterocycle. Some promising results were
obtained. In particular, 5 compounds displayed antibacterial activity against two
MRSA strains with MIC values corresponding to ciprofloxacin, which can be
considered significant. The compounds have some common features; four possess
5-chloro or 5-bromo substituents; two are derivatives of (S)-2-
ethanaminebenzimidazole and the others are derivative of one 2-(chloromethyl)-1Hbenzo[d]imidazole, (1H-benzo[d]imidazol-2-yl)methanethiol and 2-(methoxymethyl)-1-methyl-1H-benzo[d]imidazole.
The results from the antifungal screening were very interesting as there were 26
compounds, including two silver complexes, which were potent fungicides against
the selected fungal species. They showed equivalent or greater potentency in their
MIC values than amphotericin B. In particular, the 5-fluoro, 5-chloro and 5-bromo
benzimidazole showed broad spectrum activity. / Saudi Culture Bureau and King Saud University
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Investigating Novel Streptomyces Bacteriophage Endolysins as Potential Antimicrobial AgentsManeekul, Jindanuch 12 1900 (has links)
As antibiotic resistance has become a major global threat, the World Health Organization has urgently called scientists for alternative strategies for control of bacterial infections. Endolysin, a protein encoded by a phage gene, can degrade bacterial peptidoglycan (PG). Currently, there are three endolysin products in the clinical phase. We, thus, are interested in exploring novel endolysins from Streptomyces phages as only a few of them have been experimentally characterized. Using bioinformatics tools, we identified nine functional domain groups from 250 Streptomyces phages putative endolysins. NootNoot gp34 (transglycosylase; Nt34lys), Nabi gp26 (amidase; Nb26lys), Tribute gp42 (PGRP; Tb42lys), and LazerLemon gp35 (CHAP; LL35lys) were selected for experimental studies. We hypothesized that (1) the proteins of interest will have the ability to degrade PG, and (2) the proteins will be potential antimicrobial agents against ESKAPE safe relatives. The results showed that LL35lys, Nb26lys and Tb42lys exhibit PG-degrading activity on zymography and hydrolysis assay. The enzymes (400 µg/mL) can reduce PG turbidity to 32-40%. The killing assay suggested that Tb42lys possess a boarder range (Escherichia coli, Pseudomonas putida, Acinetobacter baylyi and Klebsiella aerogenes). While Nb26lys can attack Gram-negative bacteria, LL35lys can only reduce the growth of the Gram-positive strains with an MIC90 of 2 µg/mL. A higher concentration (≥300 µg/mL) of Nb26lys is needed to treat P. putida and K. aerogenes. Therefore, endolysins from Streptomyces phage have potential as possible antimicrobial agents against ESKAPE bacteria.
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Synthesis of citrate-ciprofloxacin conjugates.Md-Saleh, S.R., Chilvers, E.C., Kerr, Kevin G., Milner, S.J., Snelling, Anna M., Weber, J.P., Thomas, G.H., Duhme-Klair, A-K., Routledge, A. January 2009 (has links)
No / Two regioisomeric citrate-functionalized ciprofloxacin conjugates have been synthesized and their antimicrobial
activities against a panel of clinically-relevant bacteria have been determined. Cellular uptake
mechanisms were investigated using wild-type and ompF deletion strains of Escherichia coli K-12.
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Control of Foodborne Pathogenic Bacteria Using Natural Plant AntimicrobialsReyna-Granados, Javier Rolando January 2012 (has links)
Foodborne pathogens are a threat to public health worldwide. Because many consumers prefer natural compounds to synthetic additives, research on safe plant-derived compounds with antimicrobial activity against foodborne pathogens is vital. The aim of this investigation was to evaluate the antimicrobial activities of plant essential oils (oregano, cinnamon, lemongrass), their active components (carvacrol, trans-cinnamaldehyde, citral) and plant-extracts such as green tea, apple skin extract, black and decaffeinated black tea, grapes seed and pomace extracts against foodborne bacteria. Salmonella enterica serotype Typhimurium DT104, and serotype Newport, were selected conducting an antibiotic screening on 23 Salmonella isolates using seven antibiotics to determine antibiotic resistance. Listeria monocytogenes (strain 101M; beef and pork sausage isolate; resistant to antimicrobials in past investigations) was included to represent gram-positive bacteria. Escherichia coli O157:H7 virulent isolates (932- apple juice isolate; ATCC 35150- human isolate; F4637- sprouts isolate; used as a cocktail) were selected after conducting a Multiplex PCR over nine E. coli O157:H7 isolates to detect shiga-toxin 1 and 2 genes. All antimicrobials were evaluated in vitro in phosphate buffered saline. In general, all pathogens were more susceptible to essential oils and their active components, than powder extracts. The most active antimicrobials from each category were directly applied on foods. The activity of oregano oil (0.5%) and green tea (3%) was evaluated against S. Typhimurium on chicken and S. Newport on tomatoes and sprouts, and the results showed that oregano oil was more effective. In addition, baby spinach leaf samples inoculated with green fluorescent protein labeled S. Newport were examined under confocal scanning laser microscope before and after antimicrobial treatments. Antimicrobial experiments against L. monocytogenes on sprouts, ham and bologna, carvacrol at 0.5% and grape seed extract at 3% were used and carvacrol showed better activity. Antimicrobial activity against E. coli O157:H7 was tested on romaine lettuce, spinach and ground beef using oregano oil at 0.5% and green tea at 3%. Both compounds were effective showing no recovery of E. coli O157:H7 from lettuce and spinach; however, was not reduced in ground beef. Antimicrobial plant compounds have the potential for reducing foodborne pathogenic bacteria on/in various foods.
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Exploiting Molecular Diversity to Access Biologically Relevant ChemotypesMartinez Ariza, Guillermo, Martinez Ariza, Guillermo January 2016 (has links)
Small-molecule libraries with enhanced structural diversity are of value in drug discovery campaigns where novel biologically active hits are desired. As such, multicomponent reactions (MCRs) have proven fruitful to enhance the molecular diversity of chemical collections and expedite forward progression of the drug discovery chain. Bicalutamide (Casodex), an anticancer drug, and Telaprevir (Incivek), an antiviral, are two examples of marketed drugs that can be synthesized using an MCR. The research topic of this dissertation involves the design, discovery, and development of novel MCRs and new combinations of MCRs with post-condensation modifications to generate over twenty-five new drug-like scaffolds in an operationally friendly, atom-economical, time- and cost-effective fashion. The developed chemical methodologies possess inherent 'iterative efficiency','high exploratory power', and 'bond forming efficiency' that allow them to quickly explore chemical space and navigate the 'hypothesis-synthesis-screening' loop that is key for a medicinal chemistry project. The prepared molecules were submitted to the Community for Open Antimicrobial Drug Discovery (CO-ADD) for antimicrobial screening against pathogens that are known to cause drug-resistance infections.
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"Avaliação da atividade antimicrobiana e citotóxica in vitro do vinagre a ácido acético: perspectiva na terapêutica de feridas" / In vitro evaluation of antimicrobial and cytotoxicity activities of vinegar and acetic acid: perspectives for wound therapeutics Ribeirão Preto.Utyama, Iwa Keiko Aida 29 September 2003 (has links)
O uso correto de produtos químicos com ação antimicrobiana na terapêutica de feridas tem sido uma das preocupações dos profissionais da saúde. A temática em questão representa uma séria problemática agravada, principalmente, pela diversidade de opções, o que traz a insegurança sobre qual é a mais indicada, bem como, pelo uso indiscriminado o que pode resultar na seleção de cepas resistentes. Diante do exposto, foi estabelecido como objetivos: avaliar in vitro a atividade antimicrobiana do ácido acético e do vinagre por meio da Técnica de Difusão de Poço sobre as cepas de Pseudomonas aeruginosa, E. coli e Staphylococcus aureus; determinar a Concentração Inibitória Mínima (CIM); e revelar a citotoxicidade dos referidos produtos sobre Artemia salina Leach. Para análise estatística foi usado o teste de variância ANOVA ONEWAY seguida do teste de comparações múltiplas; com nível de significância  = 5%. Assim sendo, pelo método de difusão de poço o vinagre branco, tinto (30,0 e 25,0%) e o ácido acético a 1,0 são mais eficazes que o ácido acético a 0,7%, vinagre branco e tinto a 10,0% (p<0.05) sobre as cepas de Pseudomonas aeruginosa e Escherichia coli. Vale considerar que os produtos analisados não apresentaram ação antimicrobiana sobre Staphylococcus aureus. A Concentração Inibitória Mínima (CIM) do ácido acético nas cepas avaliadas foi a 0,25%, e do vinagre branco a 2,0% para Pseudomonas aeruginosa e Escherichia coli sendo que para Staphylococcus aureus a 3,0%. As cepas de P. aeruginosa e E. coli foram todas inibidas pelo vinagre tinto a 1,5%, e sobre as de Staphylococcus aureus a 3,0%. Ainda, com relação a CIM dos produtos químicos testados, não se verificou diferença entre cepas de Staphylococcus aureus hospitalar e comunidade. O ácido acético foi citotóxica em todas as concentrações estudadas. Já, o vinagre branco e tinto em 0,25% e 0,125% não apresentaram citotoxicidade. Ainda que, não tenha sido a preocupação nesse momento de buscar correlação entre os dados desse estudo com o uso in vivo é importante atentar que tais produtos têm sido amplamente utilizados como agente antimicrobiano no tratamento de feridas, e muitas vezes em concentrações elevadas que podem causar danos aos tecidos dificultando, assim, o processo de cicatrização. A nosso ver é premente despertar nos profissionais da saúde a consciência crítica-reflexiva em relação à utilização das evidências científicas de maneira que possam analisar e aplicar com critério os resultados das pesquisas em prol da qualidade da assistência à saúde. / One of the concerns of health professionals has been the correct use of chemical products with antimicrobial action on wound therapeutics. This issue represents a serious problem, which is made even worse due to the facts that there is a diversity of options of products, which builds insecurity in regards to which product is more appropriate, and there is an uncontrolled use that may result in the selection of resistant species. In this sense, we set the following goals for this study: perform an in vitro assessment of the antimicrobial activity of acetic acid and vinegar using the Technique of Diffusion of Well on strains of Pseudomonas aeruginosa, E. coli, and Staphylococcus aureus; determine the Minimal Inhibitory Concentration (MIC); and reveal the cytoxicity of the referred products over Artemia salina Leach. ANOVA ONEWAY test was used for statistic analysis, followed by the multiple comparison test; with a significance level  = 5%. By the well diffusion technique, the white vinegar, red vinegar (30 and 25%), and the acetic acid at 1.0 % are more effective than the acetic acid at 0.7%, white and red vinegar at 10% (p<0,05) over the strains of Pseudomonas aeruginosa and Escherichia coli. The analyzed products did not present antimicrobial actions over Staphylococcus aureus. The Minimal Inhibitory Concentration for the acetic acid on the species was 0.25%. For white vinegar on Pseudomonas aeruginosa and Escherichia coli was 2.0%, and 3.0% on Staphylococcus aureus. All P. aeruginosa and E. coli were inhibited by red vinegar at 1.5%, and at 3.0% for Staphylococcus aureus. In regard to the MIC of the tested chemical products, no difference was found between the hospital and community Staphylococcus aureus. Acetic acid was cytotoxic in all studied concentrations, while white and red vinegar in 0.25% and 0.125% did not show any cytoxicity. Although this study was not concerned with finding a relation among the studys data with the in vivo use, it is important to observe that such products have been largely used as antimicrobial agents for wound treatment, at concentrations often so high that human tissue might suffer damage; thus hindering the healing process. It is, therefore, essential to stimulate health professionals a critical-reflexive consciousness regarding the use of scientific evidence in a way to analyze and apply the research outcomes in favor of a quality health care.
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LEDs-UV como fontes luminosas alternativas para processos oxidativos avançados: inativação de nitrofurantoína pelo processo foto-Fenton / UV LEDs as alternative light sources for Advanced Oxidation Process: Inactivation of Nitrofurantoin by the photo-Fenton processLabriola, Vanessa Feltrin 10 April 2017 (has links)
O objetivo desta pesquisa foi estudar a degradação,pelo processo foto-Fenton, de um poluente-modelo (um antibiótico da classe dos nitrufuranos:a nitrofurantoína), utilizando-seLEDs-UV no lugar das lâmpadas tradicionalmente utilizadas, ou seja, das lâmpadas fluorescentes negras.Foram comparadas duas câmaras de irradiação, cada uma com um tipo de fonte, em termos de: porcentagem de remoção, ecotoxicidade (Lactuca sativa), atividade antimicrobiana (Escherichia coli), custos de capital (equipamentos), de operação (consumo energético) e das fontes luminosas, além do espaço ocupado. Os experimentos de degradação foramrealizados e otimizados via planejamento experimental, utilizando-se a Metodologia de Superfície de Resposta, obtendo-se as concentrações ótimas denitrofurantoína, de íons férricoe de peróxido de nitrogênio para cada caso.As câmaras estudadas apresentaram desempenhos semelhantes na remoção de nitrofurantoína (mais de 95% em 15 min), além de não ter havido a geração de produtos ecotóxicos (Lactuca sativa) e de ter sido alcançada a inativação biológica (Escherichia coli) do fármaco.A câmara de irradiação com LEDs é compacta, custa duas vezes menos que a outra e é quatro vezes mais eficiente em termos de consumo elétrico. A única desvantagem encontrada foi o custo dos LEDs-UV. Levando-se em conta o número de LEDs e de lâmpadas fluorescentes negras nas câmaras, o custo é trinta vezes maior. No entanto, o custo adicional dos LEDs-UV em relação às lâmpadas fluorescentes negras é facilmente compensado pela economia realizada nos custos de capital (aquisição do equipamento) e de operação (consumo energético).Em suma, pelo menos no caso da degradação da nitrofurantoína pelo processo foto-Fenton, os LEDs-UV mostraram-se substitutos vantajosos das lâmpadas fluorescentes negras, tradicionalmente utilizadas. / The goal of this research was to study the degradation, by the photo-Fenton process, of a model-pollutant (an antibiotic fromthe nitrofurans group: nitrofurantoin), using UV-LEDs instead of the lamps traditionally used, i.e. black fluorescent lamps. Two irradiation chambers were compared, each one of them with a type of light source, regarding: removal percentage, ecotoxicity (Lactuca sativa), antimicrobial activity (Escherichia coli), capital costs (equipment), operating costs (energy consumption), and light sources costs, as well as the space the chambers occupy.The degradation experiments were performed and optimized by experimental design, using the Response Surface Methodology, and obtaining the optimum concentrations of nitrofurantoin, ferric ions, and hydrogen peroxide, for each of the chambers. The studied chambers showed similar performances regarding nitrofurantoin removal (more than 95% in 15 min), besides the generation of no ecotoxic products (Lactuca sativa) and the biological inactivation (Escherichia coli) of the drug. The irradiation chamber with UV-LEDs is compact,cheaper (it is half of the price of the other one), and it is four times more efficient in terms of electric consumption. The sole disadvantage found was the cost of the UV-LEDs. Taking into consideration the number of LEDs and black fluorescent lamps used in the chambers, thiscost is 30 times greater. However, the additional cost of the UV-LEDsin comparison to black fluorescent lamps is easily compensated by the savings in capital costs (equipment acquisition) and operating costs (electric consumption). In summary, at least regarding the nitrofurantoin degradation by the photo-Fenton process, the UV-LEDs proved to beworthwhile alternatives for black fluorescent lamps, which are traditionally used.
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Desenvolvimento e caracterização de sistemas de liberação de própolis intrabolsa periodontal / Development and characterisation of into the periodontal pocket propolis delivery systems.Bruschi, Marcos Luciano 09 November 2006 (has links)
As doenças periodontais constituem um grupo de condições inflamatórias e infecciosas que afetam as estruturas de suporte dental, resultando na formação de bolsas entre a gengiva e o dente que causam retração gengival e a formação de um ambiente ideal para o crescimento de microorganismos, podendo progredir e causar a perda do dente. O tratamento fundamenta-se na remoção dos microorganismos responsáveis pela infecção e a utilização de antimicrobianos e/ou antiinflamatórios. Existem vários estudos comprovando a atividade da própolis no tratamento de doenças periodontais, na forma de solução extrativa. Além disso, nos dias de hoje, busca-se o controle das bactérias subgengivais através da liberação dos fármacos no interior da bolsa periodontal a partir de sistemas biodegradáveis ou não, permanecendo por tempo pré-determinado, exercendo ação terapêutica. Nesse sentido, no presente trabalho, dois sistemas para liberação de própolis no interior da bolsa periodontal foram desenvolvidos e caracterizados. Os sistemas contendo micropartículas de própolis foram baseados em semisólido bioadesivo termo-sensível, formado por poloxamer 407 e Carbopol 934P®, e em precursor de fase líquida cristalina, formado por álcool cetílico etoxilado 20-OE e propoxilado 5-OP e miristato de isopropila, sendo que ambos demonstraram propriedades adequadas à liberação de própolis intrabolsa periodontal. A determinação do perfil de liberação in vitro desses sistemas demonstrou que a própolis pode ser liberada de forma controlada por um período de, no mínimo, sete dias no interior da bolsa periodontal. / Periodontal diseases are a group of inflammatory and infectious conditions that affects the supporting structures of the teeth. It results in the formation of pockets between the soft tissue of the gingiva and the tooth, producing gingival retraction and an ideal environment to the microorganisms growth and can eventually cause the tooth loss. The treatment of periodontal diseases is based on the removing of microorganisms and the utilization of antimicrobial and anti-inflammatory agents. There are many studies showing the propolis activity on the periodontal diseases treatment, using propolis extractive solution. Moreover, nowadays, the treatments aim the control of subgingival bacteria through the drug delivery into the periodontal pocket from biodegradable or not-biodegradable systems, staying of a predetermined time, exerting therapeutic action. Thus, in this exclusive study, two into the periodontal pocket propolis delivery systems were developed and characterised. Systems containing propolis microparticles were based in thermo-sensitive bioadhesive semi-solid, composed by poloxamer 407 with Carbopol 934P®, and based in precursor system of liquid crystalline phase, composed by 20-OE ethoxilated and 5-OP propoxylated cetyl alcohol with isopropyl myristate. Both of the systems had showed suitable properties to delivery propolis into the periodontal pocket. The determination of in vitro delivery behaviour of these systems showed that the propolis can be delivered of a controlled way for a time of, at least, seven days within the periodontal pocket.
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Atividade antimicrobiana de produtos naturais para obtenção de novos biofármacos: estudo dos extratos brutos e suas associações / Antimicrobial activity of natural products for obtainment of new biodrugs: study of crude extracts and their associationsSilva, Cristiane Karina Malvezzi da 21 May 2010 (has links)
Estudos da atividade biológica de produtos naturais visando suas aplicações no controle de microrganismos são estratégicos e de fundamental importância econômica e social. Considerando o grande potencial da biodiversidade brasileira, o objetivo deste trabalho foi avaliar a atividade antimicrobiana do xilitol e dos extratos brutos obtidos das folhas das plantas Eugenia uniflora, Psidum guajava, Punica granatum e Syzygium cumini, bem como da associação entre os extratos e entre o xilitol e os extratos. Os extratos foram obtidos de folhas frescas maceradas em uma solução de etanol 95%, filtrada após 72 horas e concentrada em evaporador rotatório sob pressão reduzida. Foi realizada a técnica de macrodiluição em caldo e o crescimento das bactérias Staphylococcus aureus (ATCC 25923) e Escherichia coli (ATCC 25922) foi verificado pela leitura da absorbância dos tubos. O crescimento bacteriano normal foi considerado como 100%. A porcentagem de inibição sobre o crescimento bacteriano foi calculada subtraindo-se de 100% a porcentagem de crescimento na presença do extrato, xilitol ou associações. Todos os extratos inibiram o crescimento bacteriano, no entanto a atividade sobre a bactéria E. coli foi inferior aquela obtida para a bactéria S. aureus. Nos ensaios na presença de xilitol apenas a bactéria S. aureus teve seu crescimento inibido. As associações entre os extratos das folhas das espécies E. uniflora e P. guajava e das espécies E. uniflora e P. granatum promoveram inibições superiores e em concentrações menores sobre o crescimento da bactéria S. aureus quando comparadas com as inibições promovidas pelos extratos isolados, indicando um efeito antimicrobiano sinérgico entre estes extratos. As associações entre o xilitol e os extratos das folhas das espécies E. uniflora ou S. cumini e entre o xilitol e os extratos das folhas das espécies P. guajava ou P. granatum apresentaram um efeito antimicrobiano sinérgico sobre as bactérias S. aureus e E. coli, respectivamente. Os resultados do presente estudo contribuem na busca de novas alternativas terapêuticas antimicrobianas, uma vez que pode servir de subsídio para novos estudos químicos e farmacológicos a partir de fontes naturais brasileiras. / Biological activities studies of natural products aiming their applications in microorganisms control are strategic, economic, and socially important. Considering the Brazilian biodiversity‟s large potential, the purpose of this work was to evaluate antimicrobial activity of xylitol and of crude extracts obtained from leaves of the following plants: Eugenia uniflora, Psidum guajava, Punica granatum and Syzygium cumini, as well as from the association of the extracts and of xylitol with the extracts. The extracts were obtained from fresh leaves macerated in a 95% ethanol solution, filtered after 72 hours and concentrated in spinning evaporator under reduced pressure. The broth macrodilution technique was used and growth of Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 25922) bacteria was observed upon reading of pipes absorption. Regular bacterial growth was considered as 100%. The percentage of inhibition over bacterial growth was calculated by subtracting from 100%, the growth percentage in the presence of the essence, xylitol or associations. All extracts inhibited bacterial growth, but the activity on E. coli bacteria was inferior to the one obtained for S. aureus bacteria. In tests in the presence of xyliol only the S. aureus bacteria had its growth inhibited. Associations between the extracts from leaves of the species E. uniflora and P. guajava and the species E. uniflora and P. granatum promoted superior inhibitions and in inferior concentrations over the growth of S. aureus bacteria in comparison to inhibitions promoted by isolated extracts, indicating a synergetic antimicrobial effect between these extracts. The associations between xylitol and the extracts of E. uniflora or S. cumini species and between xylitol and the extracts from leaves of the species P. guajava or P. granatum presented a synergetic antimicrobial effect over the S. aureus and E. coli bacteria, respectively. The results of the present study contribute in the search of antimicrobial therapeutic alternatives, once it can be used as base for new chemical and pharmacological studies from Brazilian natural sources.
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Hidrogéis poliméricos com nanopartículas de prata para aplicações médicas / Polymeric hydrogels with silver nanoparticles for medical applicationsAlcantara, Mara Tania Silva 03 April 2013 (has links)
O desenvolvimento de novos procedimentos e tecnologias tem proporcionado um grande avanço no tratamento de feridas e queimaduras, melhorando a qualidade de vida das vítimas e reduzindo as taxas de mortalidade de pessoas com queimaduras graves. Entretanto as complicações infecciosas continuam sendo um desafio e uma das principais causas de óbito de queimados. Por outro lado, em todo o mundo tem-se observado um crescente interesse no uso de hidrogéis para aplicação como curativos para queimaduras, ferimentos e úlceras de pele, tendo em vista que são capazes de absorver exsudatos, ajudam na cicatrização e proporcionam conforto ao paciente, uma vez que favorecem o alívio da dor. Além disso, os hidrogéis também podem ser aplicados como matrizes para sistemas de liberação controlada de princípios ativos e agentes antimicrobianos. O objetivo deste trabalho foi estudar as propriedades mecânicas e físico-químicas de hidrogéis compostos por blendas formadas por Poli(N-vinil-2-pirrolidona)/ Polietilenoglicol/ ágar (PVP/PEG/ágar), Poli(N-vinil-2-pirrolidona)/ glicerol/ ágar (PVP/glicerol/ágar); Poli(álcool vinílico)/ kappa-carragena/ ágar (PVA/KC/ágar), reticuladas por radiação ionizante. Para a preparação das blendas, utilizou-se planejamento de misturas como ferramenta, oferecendo assim subsídios a futuros desenvolvimentos de novos hidrogéis, que possam ser usados como curativos e como matrizes poliméricas para liberação de ativos hidrofílicos e lipofílicos. Foram otimizadas três formulações e sintetizadas seis, três das quais hidrogéis nanocompósitos de prata. As nanopartículas de prata (NPAg) foram sintetizadas, in situ, por radiação gama, sem uso de catalisadores ou outro reagente para obtenção de curativo mais puro e com ação antimicrobiana. A caracterização físico-química dos hidrogéis foi obtida por análises de fração gel, intumescimento, ensaios de tração e perfuração, microscopia eletrônica de varredura (MEV), espectroscopia na região do ultravioleta-visível (UV-vis). Também foi avaliada a atividade antimicrobiana dos hidrogéis e realizado estudo de citotoxicidade in vitro. O planejamento de misturas apresentou modelos confiáveis para os resultados de fração gel e intumescimento, porém, para as propriedades mecânicas, os resultados devem ser vistos com cautela. O uso da radiação se mostrou eficaz para a síntese de NPAg in situ nas blendas estudadas. Os resultados sugerem que os hidrogéis sintetizados não liberaram NPAg, porém os hidrogéis de PVP apresentaram atividade bactericida para S. aureus e P. Aeruginosa, enquanto que o hidrogel de PVA apresentou atividade bactericida para P. aeruginosa e atividade bacteriostática para S. aureus, sendo essa atividade pelo contato direto. / The development of new procedures and technologies have provided a major advance in the treatment of wounds and burns improving the quality of life of victims and reducing mortality rates of people with severe burns. However, infectious complications remain a challenge and a major cause death to burn. Furthermore, in the whole world, an increasing interest in the use of hydrogels as dressings for burns, wounds and skin ulcers has been observed, considering that they are capable of absorbing exudates, aid in healing and provide confort to the patient, since they favor the pain relief. In addition, hydrogels can also be applied as matrices for controlled release systems of active and antimicrobial agents. The aim of this study was to investigate the mechanical and physicochemical properties of hydrogels composed of blends formed by poly(N-vinyl-2-pyrrolidone)/ Polyethylene glycol/ agar (PVP/PEG/agar), poly(N-vinyl-2-pyrrolidone)/ glycerol/agar (PVP/ glycerol/agar) and poly(vinyl alcohol)/ kappa-carrageenan/ agar (PVA/KC/agar), crosslinked by ionizing radiation. In blends preparation, design of mixtures was utilized as a tool, thus offering information for future developments of new hydrogels, which can be used as dressings and as polymer matrices for the release of lipophilic and hydrophilic actives. Three formulations were optimized, and six synthesized, being three of these silver nanocomposite hydrogels. The silver nanoparticles (AgNPs) were synthesized, in situ, by gamma irradiation without using a catalyst or other reagent in order to obtain wound dressing with higher purity and antimicrobial activity. The physicochemical characterization of the hydrogels was obtained using assays of gel fraction, swelling, tensile and perforation, scanning electron microscopy (SEM), spectroscopy in the ultraviolet-visible (UV-vis) region. Antimicrobial activity of the hydrogels was evaluated, and cytotoxicity study in vitro also was performed. The mixture design offered reliable models for gel fraction and swelling, but for the mechanical properties the results must be seen with caution. The use of radiation has proven to be effective for synthesis of AgNPs in situ in the blends studied. The results suggest that hydrogels synthesized did not release AgNPs, but the PVP hydrogels showed bactericidal activity for S. aureus and P. aeruginosa, whereas the PVA hydrogel had bactericidal activity for P. Aeruginosa and bacteriostatic activity for S. aureus, being this activity by direct contact.
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