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1.
Braz. J. Pharm. Sci. (Online) ; 56: e18414, 2020. tab, graf
Article in English | LILACS | ID: biblio-1249155

ABSTRACT

Tolmetin sodium (TS) is a powerful non-steroidal mitigating drug for the treatment of rheumatoid joint inflammation, osteoarthritis, and adolescent rheumatoid joint pain. In addition to its gastrointestinal (GIT) problems, TS has a short biological half-life (1 hr). In a trial to overcome these side effects and control the rate of (TS) release, chitosan coated alginate microspheres are recommended. A Box-Behnken experimental design was employed to produce controlled release microspheres of TS in the sodium alginate and chitosan copolymers (Alg-Ch) by emulsification internal gelation methodology. The effect of critical formulation variables namely, drug to polymer ratio (D:P ratio), speed of rotation and span 80% on drug encapsulation efficiency (% EE), drug release at the end of 2 hours (Rel2) and drug release at the end of 8 hours (Rel8) were analyzed using response surface modeling. The parameters were assessed using the F test and mathematical models containing only the significant terms were generated for each parameter using multiple linear regression analysis. The produced microspheres were spherical in shape with extensive pores at D:P ratio 1:1 and small pores at a drug to polymer ratio (D:P ratio) 1:3. Differential scanning calorimetry (DSC) affirmed the steady character of TS in microspheres and revealed their crystalline form. All formulation variables examined exerted a significant influence on the drug release, whereas the speed emerged as a lone factor significantly influencing % EE. Increasing the D: P ratio decreases the release of the drug after two and 8 hours. The increase in speed results in an increase in drug release after two and eight hours. The drug release from the microspheres followed zero order kinetics. TS Alg-Ch microspheres exhibited a significant anti-inflammatory effect on incited rat paw edema after eight hours. These results revealed that the internal gelation technique is a promising method to control TS release and eradicate GIT side effects using Alg-Ch copolymers.


Subject(s)
Tolmetin/analysis , Chitosan/analysis , Alginates/analysis , Microspheres , Calorimetry, Differential Scanning/methods , Pharmaceutical Preparations , Arthralgia/pathology , Drug Liberation , Inflammation/pathology , Joints/pathology
2.
Braz. J. Vet. Res. Anim. Sci. (Online) ; 57(3): e162942, 2020. tab
Article in English | LILACS, VETINDEX | ID: biblio-1122180

ABSTRACT

This study aimed to evaluate the effects of increasing levels of chitosan (CHI) on sugarcane fermentation profile and losses, chemical composition, and in situ degradation. Treatments were: 0, 1, 2, 4, and 8 g of CHI/kg of dry matter (DM). Twenty experimental silos (PVC tubing with diameter 28 cm and height 25 cm) were used. Sand (2 kg) was placed at the bottom of each silo to evaluate effluent losses, and silos were weighed 60 d after ensiling to calculate gas losses. Samples were collected from the center of the silo mass to evaluate silage chemical composition, in situdegradation, fermentation profile, and mold and yeast count. Data were analyzed as a completely randomized design, and the treatment effect was decomposed using polynomial regression. Chitosan linearly increased acetic acid and NH3-N concentration, while yeast and mold count, and ethanol concentration decreased. Intermediary levels of CHI (from 4.47 to 6.34 g/kg DM) showed the lower values of effluent, gas, and total losses. There was a quadratic effect of CHI on the content of non-fiber carbohydrates, neutral and acid detergent, and in situ DM degradation. The lowest fiber content was observed with levels between 7.01 and 7.47 g/kg DM, whereas the highest non-fiber carbohydrate content and in situ DM degradation were found with 6.30 and 7.17 g/kg DM of CHI, respectively. Chitosan linearly increased acetic acid and NH3-N concentration, whereas it linearly reduced ethanol concentration and count of yeast and mold. Thus, intermediary levels of CHI, between 4.47 and 7.47 g/kg of DM, decrease fermentation losses and improve the nutritional value of sugarcane silage.(AU)


Foram avaliados os efeitos do aumento dos níveis de quitosana (CHI) sobre o perfil e as perdas fermentativas, a composição química e degradação in situ da silagem de cana-de-açúcar. Os tratamentos foram: 0, 1, 2, 4 e 8 g de CHI / kg de matéria seca (MS). Foram utilizados vinte silos experimentais (tubos de PVC com 28 cm de diâmetro e 25 cm de altura). Areia (2 kg) foi adicionada na porção inferior de cada silo para avaliar as perdas por efluentes e os silos foram pesados 60 dias após a ensilagem para calcular as perdas por gases. Amostras foram coletadas do centro da massa do silo para avaliar a composição química, degradação in situ, perfil fermentativo e a contagem de fungos e leveduras da silagem. Os dados foram analisados como um delineamento inteiramente casualizado e o efeito do tratamento foi decomposto usando regressão polinomial. A CHI aumentou linearmente a concentração de ácido acético e N-NH3, enquanto diminuiu a contagem de leveduras e bolores e a concentração de etanol. Os níveis intermediários de CHI (de 4,47 a 6,34 g/kg MS) mostraram os menores valores de perdas por efluentes, gases e totais. Houve efeito quadrático da CHI sobre o teor de carboidratos não fibrosos, fibra em detergente neutro e ácido e sobre a degradação in situ da MS. Os menores teores de fibras foram observados com níveis de CHI entre 7,01 e 7,47 g/kg MS, enquanto que os maiores teores de carboidratos não fibrosos e degradação in situ da MS foram encontrados com 6,30 e 7,17 g/kg MS de CHI, repectivamente. A CHI aumentou linearmente as concentrações de ácido acético e N-NH3, enquanto reduziu linearmente a concentração de etanol e a contagem de fungos e leveduras. Desta forma, níveis intermediários de CHI, entre 4,47 e 7,47 g / kg de MS, diminuem as perdas fermentativas e melhoram o valor nutricional da silagem de cana-de-açúcar.(AU)


Subject(s)
Silage/analysis , Saccharum/chemistry , Chitosan/analysis , Acetic Acid/analysis , Ethanol
3.
São Paulo; s.n; s.n; 2019. 105 p. tab, graf.
Thesis in Portuguese | LILACS | ID: biblio-996861

ABSTRACT

Quitosana é um biopolímero encontrado principalmente na parede celular de crustáceos e é obtida pela desacetilação da quitina. Como biopolímero a quitosana é utilizada como excipiente para medicamentos e composição de alimentos. No entanto a quitosana devidamente purificada para uso farmacêutico ou alimentício tem custo financeiro elevado. Outro fator que contribui para o uso limitado é a falta de procedimento padronizado para desacetilação, o que resulta em materiais com diferentes graus de qualidade, dificultando suas aplicações e controle de qualidade de matéria prima e produto. Este trabalho tem como principal objetivo estabelecer procedimento reprodutível para a extração da quitina e da quitosana, por meio da aplicação dos conceitos de Quality by Design e planejamento de experimentos. A quitosana foi obtida pela desacetilação da quitina de crustáceos pelas etapas de desmineralização, desproteinização e despigmentação. O procedimento técnico para purificação da quitosana foi definido a partir de planejamento fatorial com ponto central para as etapas otimizadas, por meio da aplicação dos conceitos de Quality by Design e planejamento de experimentos. O projeto definiu um procedimento padronizado para purificação da quitosana que pode ser empregado em escala industrial, e financeiramente vantajoso para produção de medicamentos ou alimentos


Chitosan is a biopolymer found mainly in the cell wall of crustaceans and is obtained by the deacetylation of chitin. As biopolymer chitosan is used as excipient for medicaments and food composition. However, chitosan duly purified for pharmaceutical or food use has a high financial cost. Another factor that contributes to the limited use is the lack of standardized procedure for deacetylation, which results in materials with different grades of quality, hindering their applications and quality control of raw material and product. This work has as main objective to establish a reproducible procedure for the extraction of chitin and chitosan, through the application of the concepts of Quality by Design and planning of experiments. Chitosan was obtained by the deacetylation of chitin from crustaceans through the demineralization, deproteinization and depigmentation stages. The technical procedure for purification of chitosan was defined from a factorial planning with a central point for the optimized steps, through the application of the concepts of Quality by Design and planning of experiments. The project defined a standard procedure for the purification of chitosan that can be used on industrial scale and financially advantageous for the production of medicines or foods


Subject(s)
Pharmaceutical Preparations/classification , Chitosan/isolation & purification , Chitosan/analysis , Process Optimization , Food/classification , Chitin/isolation & purification
4.
Braz. J. Pharm. Sci. (Online) ; 55: e17105, 2019. tab, graf, ilus
Article in English | LILACS | ID: biblio-1019532

ABSTRACT

The efficacy of conventional ocular formulations is limited by poor corneal retention and permeation, resulting in low ocular bioavailability. Mucoadhesive chitosan (CS)/ tripolyphosphatesodium (TPP) and chitosan (CS)/ tripolyphosphatesodium (TPP)-alginate (ALG) nanoparticles were investigated for the prolonged topical ophthalmic delivery of ofloxacin. A modified ionotropic gelation method was used to produce ofloxacin-loaded nanoreservoir systems. The ofloxacin-loaded CS/TPP and CS/TPP-ALG nanoparticles were characterized for particle size, morphology, zeta potential, encapsulation efficiency, subsequent release and corneal penetration study. The designed nanoparticles have a particle size from 113.8 nm to 509 nm and zeta potential from 16.2 mV to 40.3 mV and encapsulation efficiency values ranging from 19.7% to 33.1%. Nanoparticles revealed a release during the first hours, followed by a more gradual drug release. The ofloxacin-loading CS/TPP or CS/TPP-ALG NPs developed are pronounced penetration enhancing effect as compared to OFX solution (5-6.5 times). Thus, these nanoparticles have a strong potential for ocular drug delivery.


Subject(s)
Ofloxacin/analysis , Chitosan/analysis , Nanoparticles/analysis , Administration, Ophthalmic , Ocular Physiological Phenomena , Eye Infections/classification , Chromatography, High Pressure Liquid/methods , Cornea
5.
São Paulo; s.n; s.n; 2018. 177 p. tab, graf, ilus.
Thesis in English | LILACS | ID: biblio-1361779

ABSTRACT

Chitosan is a biocompatible and biodegradable mucoadhesive polymer with unique advantages, such as the distinct trait of opening the junctions to allow paracellular transport of antigen and good tolerability. However, the poor solubility of chitosan in neutral or alkalinized media has restricted its applications in the pharmaceutical field. Chitosan can be easily carboxymethylated to improve its solubility in aqueous media, while its biodegradability and biocompatibility are preserved. Apart from this, carboxymethyl chitosan (CMCS) can be easily processed into nanoparticles which highlight its suitability and extensive usage for preparing different drug delivery formulations. The present study deals with the development and characterization of a delivery system based on CMCS nanoparticles using ovalbumin as model protein. We demonstrated that ovalbumin loaded nanoparticles were successfully synthetized using calcium chloride as a cross-linker by ionic gelation. The nanoparticles exhibited an average size of approximately 169 nm and presented a pseudo-spherical shape. The nanoparticles size increased according to the addition of CaCl2 due to the strong electrostatic attraction. During storage the nanoparticles size increased was attributed to swelling and aggregation. The loading efficiency of ovalbumin was found to be 17%. Confocal microscopy clearly showed the association between ovalbumin and CMCS chains into nanoparticles. Therefore, we suggest these nanoparticles can be considered as an attractive and promising carrier candidate for proteins and antigens. The major challenge that limits the use of such carriers is their instability in an aqueous medium. Thus, the next step of this work was to determine the robustness of several formulations using distinct freeze-drying protocols. This study demonstrated that mannitol in concentration of 10% (w/v) is well suited to preserve ovalbumin loaded CMCS nanocapsules from aggregation during lyophilization and subsequent reconstitution. Importantly, the results showed that an annealing step has a huge impact on porosity of freeze-dried cake by nearly complete crystallization of mannitol, once the crystalline matrix prevents the partial collapse and the formation of larger pores observed without annealing. Therefore, the usual observation that annealing increases the pore size due to growth of ice crystal size does not always apply, at least when crystallization of solute is involved. Since all characterizations and stability studies had been performed, the main purpose of this study was to develop a stable antigen delivery system for oral immunization using CMCS and inactivated rabies virus (RV) as the antigen. RV loaded nanoparticles was found to enhance both systemic (IgG) and local (IgA) immune responses against RV after oral delivery in mice. The effective doses 50% were 50-times higher than the negative controls, indicating that the immune response started only after the third boosting dose. Furthermore, enough neutralizing antibodies was produced to be protected against the harmful effects of the rabies virus. It is therefore concluded, that the CMCS nanoparticles formulated in this study, are suitable for oral vaccine delivery, and can be suggested as a promising delivery system for a diverse range of antigens as well as a gene/protein delivery system, especially for those positively charged. Since several approaches show that effective intervention in airway allergic inflammation can be achieved with allergen-activated interleukin-10-secreting cells, the final part of this work was dedicated to assessing whether IL-10 loaded chitosan nanoparticles (IL10-CSNPs) could be used as a possible inhalable therapeutic tool for preventing exacerbations in asthmatic patients. As positive controls, we also assess whether interleukin 17A and interleukin 9 have the ability to stimulate human airway smooth muscle (HASM) cell contractility using magnetic twisting cytometry (MTC). Significant decreased baseline cell stiffness was observed in HASM cells pre-treated with IL-10, but not with IL10-CSNPs, whereas treatment with IL-17A significantly enhanced baseline cell stiffening. Our findings reveal a previously unknown mechanism underlying immunotherapy for prevention and treatment of asthma


A quitosana é um polímero mucoadesivo biocompatível e biodegradável, com vantagens únicas, tais como a característica distinta de abrir as junções que permitim o transporte paracelular de antígenos e boa tolerabilidade. No entanto, sua baixa solubilidade em meios neutros ou alcalinizados tem restringido suas aplicações no campo farmacêutico. A quitosana pode ser facilmente carboximetilada para melhorar de sua solubilidade em meios aquosos, enquanto sua biodegradabilidade e biocompatibilidade são preservadas. Além disso, a carboximetilquitosana (CMCS) pode ser facilmente processada na forma de nanopartículas, o que destaca sua adequabilidade para uso extensivo no preparo de sistemas de delivery de medicamentos. O presente estudo trata do desenvolvimento e caracterização de um sistema de delivery baseado em nanopartículas de CMCS utilizando ovalbumina como proteína modelo. Nós demonstramos que as nanopartículas carregadas com ovalbumina foram sintetizadas com sucesso utilizando cloreto de cálcio como agente de reticulação por gelificação iônica. As nanopartículas exibiram um tamanho médio de aproximadamente 169 nm e apresentaram uma forma pseudo-esférica. O tamanho das nanopartículas aumentou de acordo com a adição de CaCl2 devido à forte atração eletrostática. Durante o armazenamento, o tamanho aumentado das nanopartículas foi atribuído a incorporação de água e agregação. A eficiência de encapsulamento da ovalbumina foi de aproximadamente 17%. A microscopia confocal mostrou claramente a associação entre ovalbumina e a cadeias de CMCS nas nanopartículas. Sugerimos, portanto, que tal sistema pode ser considerado como candidato atraente e promissor para o carreamento de proteínas e antígenos. O principal desafio que limita o uso desses carreadores consiste na instabilidade em meio aquoso. Assim, o próximo passo deste trabalho foi determinar a robustez de várias formulações utilizandose diferentes protocolos de liofilização. Este estudo demonstrou que o manitol em uma concentração de 10% (p/v) é adequado para preservar da agregação as nanocápsulas de CMCS carregadas com ovalbumina durante a liofilização e subsequente reconstituição. Mais importante, os resultados mostraram que uma etapa de annealing tem um enorme impacto sobre a porosidade da amostra liofilizada devido a quase completa cristalização do manitol, uma vez que a matriz cristalina evita o colapso parcial e a formação de poros maiores observados na ausência do annealing. Portanto, a observação comum de que o annealing aumenta o tamanho doporos devido ao crescimento dos cristais de gelo nem sempre se aplica, pelo menos quando a cristalização de um soluto está envolvida. Uma vez que todas as caracterizações e estudos de estabilidade foram realizados, o principal objetivo deste estudo foi desenvolver um sistema estável de delivery de antígeno para imunização oral utilizando CMCS e vírus rábico inativado (RV) como antígeno. Verificou-se que as nanopartículas carregadas com RV aumentam as respostas imune sistêmica (IgG) e local (IgA) contra o RV após administração oral em camundongos. As doses efetivas 50% foram 50 vezes maiores que os controles negativos, indicando que a resposta imune foi iniciada apenas após a terceira dose da vacina. Além disso, foram produzidos anticorpos neutralizantes suficientes para proteção contra os efeitos nocivos do vírus rábico. Conclui-se, portanto, que as nanopartículas de CMCS formuladas neste estudo, são adequadas para o delivery oral de vacinas, e podem ser sugeridas como um sistema promissor de delivery para uma gama diversa de antígenos, bem como para o delivery de genes/proteínas, especialmente para aqueles carregados positivamente. Uma vez que diversas abordagens mostram que uma intervenção efetiva em casos de inflamação alérgica de vias aéreas pode ser conseguida por meio de células secretoras de interleucina 10 (IL-10) mediante ativação por alergenos, a parte final deste trabalho esteve dedicada a avaliação de nanopartículas de quitosana carregadas com IL-10 (IL10-CSNPs) como possível ferramenta terapêutica inalável para prevenção de exacerbações em pacientes asmáticos. Como controles positivos, avaliou-se adicionalmente se as interleucinas 17A (IL-17A) e 9 (IL-9) possuem a capacidade de estimular a contratilidade de células humanas de músculo liso de vias aéreas humanas (HASM) por meio de citometria de torção magnética (MTC). Uma diminuição significativa da rigidez celular basal foi observada em células HASM pré-tratadas com IL-10, mas não com IL10-CSNPs, enquanto que o tratamento com IL-17A aumentou significativamente a magnitude rigidez celular basal. Nossos resultados revelam um mecanismo previamente desconhecido subjacente à imunoterapia para prevenção e tratamento da asma


Subject(s)
Asthma/pathology , In Vitro Techniques/instrumentation , Pharmaceutical Preparations , Ovalbumin/analysis , Chitosan/analysis , Administration, Oral , Interleukins/pharmacology , Microscopy, Confocal/methods , Nanocapsules , Nanoparticles/classification , Freeze Drying/methods
6.
São Paulo; s.n; s.n; 2018. 114 p. graf, tab, ilus.
Thesis in Portuguese | LILACS | ID: biblio-995936

ABSTRACT

Pacientes com queimaduras e outras lesões cutâneas de grande extensão apresentam alta propensão a infecções multirresistentes. Neste contexto, o objetivo deste trabalho é a obtenção de nanopartículas de quitosana carregadas com composto derivado de 5-nitro-heterocíclico com estrutura análoga à nifuroxazida, N'-((5-nitrofurano-2-il)metileno)-2-benzidrazida (C-H), que apresentou importante atividade frente a diversas cepas de bactérias multirresistentes. Por sua vez, a quitosana é um biopolímero com atividade antimicrobiana, analgésica, regeneradora tecidual e que, mediante contato com exsudato de lesões cutâneas forma filmes hidrogéis protetores no local de aplicação, sendo estas atividades importantes para a prevenção e tratamento de infecções e da exsudação excessiva de lesões de grande extensão. As nanopartículas de quitosana carregadas com o composto (Nps-H) foram obtidas pelo método de gelificação iônica com tripolifosfato de sódio como agente reticulante, variando a concentração de NaCl e polissorbato 80 do sistema, orientada por análise fatorial. As Nps-H obtidas foram caracterizadas por Dynamic Light Scattering (DLS) para determinação do tamanho, índice de polidispersão (IPD) e potencial zeta (ζ). A eficiência de encapsulação (EE%) foi determinada por espectrofotometria UV/VIS a 370 nm por método indireto. Entre os experimentos desenvolvidos, aquele que apresentou os melhores resultados resultou em partículas de tamanho médio de 321 d.nm, IPD 0,18, Pζ +37 mV e EE% de 48%. A morfologia e superfície das Nps-H foram analisadas por Microscopia Eletrônica de Varredura (MEV) e mostraram que as Nps-H são esféricas e de superfície irregular. A partir da obtenção e caracterização das Nps-H determinou-se a concentração inibitória mínima (CIM) das Nps-H, do composto livre (C-H) e das nanopartículas de quitosana vazias (Nps-Cs) por método colorimétrico e microdiluição frente às cepas de Staphylococcus aureus ATCC 29213, hVISA e ORSA. As Nps-H apresentaram atividade bastante superior comparando-se ao C-H e as Nps-Cs frente às cepas de S. aureus estudadas. Com vista à preparação de uma formulação farmacêutica estável, partiu-se para a liofilização das Nps-H e com esse objetivo realizou-se análises térmicas das Nps-H por Differential Scanning Calorimetric (DSC) para determinação das temperaturas de transição vítrea e eutética (Tg' e Teut) e análise por criomicroscopia para determinação da temperatura de colapso (Tcol). Amostras de Nps-H com lio/crioprotetores glicina, lactose e sacarose a diferentes concentrações foram liofilizadas a -40 ºC a 100 mTorr. As amostras de Nps-H com lactose e sacarose ambas a 2,5% e 5% demonstraram preservar as características originais das Nps-H após o processo de liofilização. Observou-se, com os resultados obtidos neste trabalho que as Nps-H representam uma promissora alternativa na prevenção e tratamento de pacientes com lesões cutâneas infeccionadas por bactérias multirresistentes e no controle da exsudação excessiva, principalmente por suas atividades terapêuticas em conjunto, diminuindo a mortalidade e morbidade desses quadros


Patients with burns and others extensive skin lesions show high propension to multiresistant infections. In this context, the aim of this project is to obtain chitosan nanoparticles carried with 5-nitro-heterocyclic derivate with structure analogue to nifuroxazide N'-((5-nitrofuran-2-yl) methylene)-2-benzhydrazide, that showed important activity against multiresistant bacteria strains. In its turn, the chitosan is a biopolymer with antimicrobial, analgesic, tecidual regenerator activities and by contact with excessive burns and extensive skin lesions exsudate process, form protective hydrogel films on place of application, being these activities important to infection and excessive exsudate treatment and prevention of extensive burns and lesions. The chitosan nanoparticles carried with compound (Nps-H) were obtained by ionic gelation method with sodium tripolyphosphate as crosslinker agent, varing the NaCl and polysorbate 80 concentrations in the system, oriented by factorial analyze. The Nps-H obtained were characterized by Dynamic Light Scattering (DLS) to size determination, polydispersion index (PDI) and zeta potential (ζ-P). The encapsulation efficiency (EE%) were determined by spectrophotometry UV/VIS at 370 nm by indirect method. Bepolissorbato the experiments developed, the one who showed the best results, resulted in particles with size of 321 d.nm, PDI of 0,18, ζ-P of +37 mV and EE% of 48%. The Nps-H morphology and surface were analyzed by Scanning Electronic Microscopy (SEM) and showed that Nps-H are spherical and with irregular surface. Starting of Nps-H obtain and characterization were determined the Nps-H, free compound (C-H) and empty chitosan nanoparticles (Nps-Cs) Minimal Inhibitory Concentrations (MIC) by colorimetric method and microdilution against Staphylococcus aureus ATCC 29213, ORSA and hVISA strains. The Nps-H showed the superior activity comparing to C-H and Nps-H against all strains tested. With a view to preparation of stable pharmaceutic formulation, started to Nps-H freeze-drying and with this aim, were realized Nps-H thermal analyzes by Differential Scanning Calorimetric (DSC) to determine glass transition and euthetic temperatures (Tg' and Teut) and the cryomicroscopy analyze to determine collapse temperature (Tcol). The Nps-H samples with lyo/cryoprotectants as glycine, lactose and sucrose at different concentrations were lyophilized at -40 ºC at 100 mTorr. The Nps-H samples with lactose and sucrose both at 2,5% and 5% demonstrated to preserve the original Nps-H characteristics after freeze-drying process. Were observed, with the results obtained in this project that Nps-H represent the promising alternative to prevention and treatment of patients with infected skin lesions by multiresitant bacteria and to control of excessive exudate process, mainly by their therapeutic activities combined, decreasing the mortality and morbidity of these cases


Subject(s)
Chitosan/analysis , Nanoparticles/classification , Anti-Infective Agents/analysis , Skin , Staphylococcus aureus/classification , Burns , Drug Discovery
7.
Arq. Inst. Biol ; 84: e0542015, 2017. graf
Article in Portuguese | LILACS, VETINDEX | ID: biblio-981748

ABSTRACT

A caprinocultura é representada por um efetivo bastante considerável no Nordeste brasileiro, porém, infecções causadas por nematoides e o sério problema da resistência parasitária se tornaram barreiras para a criação desses animais. Como alternativa, o controle com bioprodutos entra como uma solução sustentável e viável para auxiliar na criação da região. Nesse contexto, o presente trabalho avaliou a atuação da quitosana fúngica sobre o desenvolvimento larval de nematoides gastrintestinais em amostras de caprinos naturalmente infectados. Para tanto, foi realizada a seleção de 5 propriedades e confirmada a positividade do rebanho, além de coproculturas com solução de quitosana a 0,5; 1,0 e 1,5%, com cada tratamento realizado em 5 repetições. As larvas de terceiro estágio (L3) foram recuperadas e cem larvas por tratamento foram contabilizadas e identificadas. Os gêneros identificados foram Haemonchus, Strongyloides, Oesophagostomum e Trichostrongylus. Na análise da inibição do desenvolvimento larval, a concentração de 1,0% impediu o desenvolvimento larval do Haemonchus em 35%, porém, os resultados não tiveram diferença estatística significante. Assim, sugere-se buscar novas concentrações de quitosana fúngica como anti-helmíntico, visto que se apresenta como uma alternativa promissora no controle sustentável desses endoparasitos.(AU)


The goat is represented by a very considerable effective in the Northeastern Brazil, but infections caused by nematodes and the serious problem of parasitic resistance have become barriers to breed these animals. Alternatively, the control with bioproducts comes as a sustainable and viable solution to help breeding in this region. In this context, the present study evaluated the performance of fungal chitosan on the larval development of gastrointestinal nematodes in naturally infected goat samples. Therefore, the selection was performed at five properties. The positive herd was confirmed, and coprocultures were performed with chitosan solution 0.5, 1.0 and 1.5%, with each treatment performed in 5 replicates. The third-stage larvae (L3) were recovered and one hundred larvae/treatment were counted and identified. The identified genera were Haemonchus, Strongyloides, Oesophagostomum and Trichostrongylus. In the analysis of inhibition of larval development, the concentration of 1.0% prevented the development of larval Haemonchus by 35%, but the results were not statistically significant. Thus, it is suggested to seek new concentrations of fungal chitosan as anthelmintic, since it appears as a promising alternative to sustainable control of these endoparasites.(AU)


Subject(s)
Animals , Ruminants/parasitology , Chitosan/analysis , Larvicides , Fungi , Anthelmintics/analysis , Nematoda , Cunninghamella , Gastrointestinal Diseases/veterinary
8.
Braz. j. pharm. sci ; 50(4): 869-876, Oct-Dec/2014. tab, graf
Article in English | LILACS | ID: lil-741337

ABSTRACT

The objective of the research was to formulate and evaluate selegiline hydrochloride loaded chitosan nanoparticles for the Parkinson's therapy in order to improve its therapeutic effect and reducing dosing frequency. Taguchi method of design of experiments (L9 orthogonal array) was used to get optimized formulation. The selegiline hydrochloride loaded chitosan nanoparticles (SHPs) were prepared by ionic gelation of chitosan with tripolyphosphate anions (TPP) and tween 80 as surfactant. The SHPs had a mean size of (303.39 ± 2.01) nm, a zeta potential of +32.50mV, and entrapment efficiency of SHPs was 86.200 ± 1.38%. The in vitro drug release of SHPs was evaluated in phosphate buffer saline (pH 5.5) using goat nasal mucosa and found to be 82.529% ± 1.308 up to 28 h. Release kinetics studies showed that the release of drug from nanoparticles was anomalous (non-fickian) diffusion indicating the drug release is controlled by more than one process i.e. superposition of both phenomenon, the diffusion controlled as well as swelling controlled release. SHPs showed good stability results as found during stability studies at different temperatures as mentioned in ICH guidelines. The results revealed that selegiline hydrochloride loaded chitosan nanoparticles are most suitable mode of delivery of drug for promising therapeutic action.


O objetivo da pesquisa foi formular e avaliar nanopartículas de quitosana contendo cloridrato de selegilina para terapia do Parkinson, a fim de melhorar o seu efeito terapêutico e reduzir a frequência de dosagem. Método de Taguchi, de planejamento experimental, (L9 matriz ortogonal) foi usado para obter a formulação otimizada. As nanopartículas de quitosana contendo cloridrato de selegilina (PCHs) foram preparadas por gelificação iônica de quitosana com ânions tripolifosfato (TPP) e Tween 80 como tensoativo. As PCHs apresentaram tamanho médio de (303.39 ± 2,01) nm, potencial zeta de +32.50 mV e eficiência de encapsulação de 86.200±1,38%. A liberação do fármaco in vitro foi avaliada em solução salina de tampão fosfato (pH 5,5), usando a mucosa nasal de cabra e o resultado encontrado foi de 82.529% ± 1.308, acima de 28 h. Estudos de cinética de liberação mostraram que a liberação do fármaco das nanopartículas foi por difusão anômala (não fickiana), indicando que é controlada por mais de um processo, ou seja, a superposição dos fenômenos de difusão controlada e intumescimento. As PCHs mostraram resultados de boa estabilidade, encontrada durante os estudos de estabilidade em temperaturas diferentes, como mencionado em diretrizes do ICH. Os resultados revelaram que o sistema de nanopartículas de quitosana contendo cloridrato de selegilina é o mais adequado sistema de liberação de fármacos de ação terapêutica promissora.


Subject(s)
Nanoparticles/statistics & numerical data , Parkinson Disease/therapy , Chemistry, Pharmaceutical , Chitosan/analysis , Drug Liberation , Selegiline/analysis
9.
Braz. j. pharm. sci ; 50(4): 919-930, Oct-Dec/2014. tab, graf
Article in English | LILACS | ID: lil-741359

ABSTRACT

An oleaginous fraction obtained from an alcohol extract of the fruit of Pterodon pubescens Benth. (FHPp) was microencapsulated in polymeric systems. These systems were developed using a complex coacervation method and consisted of alginate/medium-molecular-weight chitosan (F1-MC), alginate/chitosan with greater than 75% deacetylation (F2-MC), and alginate/low-molecular-weight chitosan (F3-MC). These developed systems have the potential to both mask the taste of the extract, and to protect its constituents against possible chemical degradation. The influence of the formulation parameters and process were determined by chemical profiling and measurement of the microencapsulation efficiency of the oleaginous fraction, and by assessment of microcapsule morphology. The obtained formulations were slightly yellow, odorless, and had a pleasant taste. The average diameters of the microcapsules were 0.4679 µm (F2-MC), 0.5885 µm (F3-MC), and 0.9033 µm (F1-MC). The best formulation was F3-MC, with FHPp microencapsulation efficiency of 61.01 ± 2.00% and an in vitro release profile of 75.88 ± 0.45%; the content of vouacapans 3-4 was 99.49 ± 2.80%. The best model to describe the release kinetics for F1-MC and F3-MC was that proposed by Higuchi; however, F2-MC release displayed first-order kinetics; the release mechanism was of the supercase II type for all formulations.


Uma fração oleaginosa obtida do extrato etanólico de frutos de Pterodon pubescens Benth (FHPp) foi microencapsulada em um sistema polimérico. Estes sistemas foram desenvolvidos utilizando o método de coacervação complexa, constituído de alginato/quitosana massa molecular média (F1-MC), alginato/quitosana com desacetilação superior a 75% (F2-MC) e alginato/quitosana de massa molecular baixa (F3-MC). Estes sistemas desenvolvidos têm o potencial tanto de mascarar o sabor do extrato, quanto de protegê-lo de possível degradação química. A influência dos parâmetros de formulação e processo foram determinadas por caracterização química, determinação da eficiência de microencapsulação da fração oleaginosa e por avaliação morfológica da microcápsula. As formulações mostraram-se ligeiramente amareladas, inodoras e com sabor agradável. Os diâmetros médios das microcápsulas foram de 0,4679 µm (F2-MC), 0,5885 µm (F3-MC) e 0,9033 µm (F1-MC). A melhor formulação foi F3-MC, considerando-se que apresentou eficiência de encapsulação de 61,01 ± 2,00%, e perfil de liberação in vitro de 75,88 ± 0,45%; o conteúdo dos vouacapanos 3-4 foi 99,49 ± 2,80%. O melhor modelo para descrever a cinética de liberação foi o modelo proposto por Higuchi para F1-MC e F3-MC, entretanto, para F2-MC foi o modelo de primeira ordem, e o mecanismo de liberação foi do tipo super caso II para todas as formulações.


Subject(s)
Alginates/analysis , Biological Products/analysis , Fabaceae/classification , Chitosan/analysis , Drug Compounding/statistics & numerical data
10.
Braz. j. microbiol ; 44(1): 189-195, 2013. graf, tab
Article in English | LILACS | ID: lil-676907

ABSTRACT

Chitosanase production of Gongronella sp. JG cells immobilized in calcium alginate gel and polyurethane foam was compared with that of the free cells, there was a 60% increase in the enzyme yield (2429 U/L) compared to the highest yield obtained from free cells (1513 U/L). The optimal immobilization parameters (concentrations of sodium alginate, calcium chloride, bead inoculums, bead diameter, etc) for the enhanced production of chitosanase were determined as: sodium alginate 2% (w/v), 0.1 M calcium chloride, inoculum 10 mL beads to 100 mL production media and 2.7 mm bead diameter. Maximum chitosanase production was achieved with initial pH of 5.5 and temperature of 30 ºC. The alginate beads had well stability, retained 85% ability of enzyme production even after 7 cycles of repeated batch fermentation. These results showed the immobilization technique was a feasible and economical method for chitosansase production by Gongronella sp. JG.


Subject(s)
Animals , Alginates , Crustacea/enzymology , Crustacea/microbiology , Fermentation , Aquatic Fungi/analysis , Polyurethanes/analysis , Chitosan/analysis , Chitosan/isolation & purification , Sodium/analysis , Attention , Cells, Immobilized , Enzyme Activation , Food Samples , Methods , Reference Standards
11.
Braz. j. microbiol ; 43(2): 800-809, Apr.-June 2012. ilus, graf, tab
Article in English | LILACS | ID: lil-644499

ABSTRACT

The inhibitory effects of fifteen chitosans with different degrees of polymerization (DP) and different degrees of acetylation (F A) on the growth rates (GR) of four phytopathogenic fungi (Alternaria alternata, Botrytis cinerea, Penicillium expansum, and Rhizopus stolonifer) were examined using a 96-well microtiter plate and a microplate reader. The minimum inhibitory concentrations (MICs) of the chitosans ranged from 100 µg × mL-1 to 1,000 µg × mL-1 depending on the fungus tested and the DP and F A of the chitosan. The antifungal activity of the chitosans increased with decreasing F A. Chitosans with low F A and high DP showed the highest inhibitory activity against all four fungi. P. expansum and B. cinerea were relatively less susceptible while A. alternata and R. stolonifer were relatively more sensitive to the chitosan polymers. Scanning electron microscopy of fungi grown on culture media amended with chitosan revealed morphological changes.


Subject(s)
Animals , Rats , Antifungal Agents/analysis , Culture Media , Mitosporic Fungi/growth & development , Mitosporic Fungi/pathogenicity , In Vitro Techniques , Polymers/analysis , Chitosan/analysis , Acetylation , Food Samples , Methods , Microbial Sensitivity Tests , Microscopy, Electron, Scanning , Virulence
12.
Braz. j. microbiol ; 42(1): 96-104, Jan.-Mar. 2011. ilus, tab
Article in English | LILACS | ID: lil-571380

ABSTRACT

Representative strains of Serratia marcescens from an edible cactus plant and silkworms were characterized and a comparison based on their cellular fatty acid composition, 16S rRNA and groE gene sequence analysis as well as silkworm virulence and chitosan susceptibility was carried out. Results from this study indicate that there are no significant differences between the phenotypic and molecular characterization, virulence and chitosan susceptibility of the S. marcescens strains from the cactus plant and silkworms. Silkworms inoculated with S. marcescens from either plant or silkworm resulted in nearly 100 percent mortality. Chitosan solution exhibited strong antibacterial activity against S. marcescens. This activity increased with the increase of chitosan concentration and incubation time regardless of the strain source. Also, the results indicate that the plant associated S. marcescens maybe plays a possible role in the contamination of humans and animals, in particular silkworms, while chitosan showed a potential to control the contamination caused by S. marcescens.


Subject(s)
Anti-Bacterial Agents/analysis , Anti-Bacterial Agents/isolation & purification , Base Sequence , Bombyx/genetics , Enzyme Reactivators , Genetic Predisposition to Disease , Chitosan/analysis , Chitosan/isolation & purification , Serratia marcescens/genetics , Serratia marcescens/isolation & purification , Enzyme Activation , Methods , Methods , Virulence
13.
Braz. j. microbiol ; 40(1): 20-25, Jan.-Mar. 2009. graf, tab
Article in English | LILACS | ID: lil-513110

ABSTRACT

In this work, we propose the reuse of apple pomace as a substrate for fungal chitosan production by liquid cultivation of Gongronella butleri CCT4274. Different concentrations of reducing sugars and sodium nitrate were added to the aqueous extract of apple pomace and the best result was obtained with 40 g/L of reducing sugars and 2.5 g/L of sodium nitrate. The results indicate the possibility of producing 1.19 g/L of chitosan per liter of culture medium after 72.5 hours of cultivation, representing around 21% of the biomass content.


Este trabalho propõe o reuso do bagaço de maçã como substrato para a produção de quitosana fúngica em cultivo liquido do fungo Gongronella butleri CCT4274. Diferentes concentrações de açúcares redutores e nitrato de sódio foram adicionadas ao extrato aquoso do bagaço de maçã. O melhor resultado foi obtido para concentrações de 40 g/L e 2,5 g/L de açúcares redutores e nitrato de sódio, respectivamente. Os resultados indicam a possibilidade de produzir 1,19 g/L de quitosana após 72,5 horas de cultivo, representando 21% da composição da biomassa.


Subject(s)
Carbohydrates/analysis , Malus , Culture Media/analysis , Chitosan/analysis , Substrates for Biological Treatment/analysis , Food Samples , Methods , Methods
14.
Nutrire Rev. Soc. Bras. Aliment. Nutr ; 32(3): 1-13, 2007. tab, ilus
Article in Portuguese | LILACS | ID: biblio-882078

ABSTRACT

The recommendation for a larger intake of food fiber has been an important strategy for the control and prevention of obesity and its co-morbidities. Chitosan, an animal fiber, has been related to the reduction of fat uptake by the intestine, serum cholesterol and glucose, as well as appetite inhibition and weight loss. This study evaluated the effects of consuming powdered chitosan on some nutritional and biochemical parameters in adult female rats. Adult female Wistar rats (n=14) were divided in control group (GC): fed a diet based on casein and microcrystaline cellulose (AIN 93 G) for 10 days; and chitosan group(GQ): fed a diet based on casein and powdered chitosan (5%) substituting microcrystalline cellulose for 10 days. No differences were observed I the food intake, evolution of the body weight, liver weight, fat depots in the abdomen and in the carcass. Also, there were no differences in the glucose and total protein serum concentrations or in the lipid profile.The GQ presented smaller stomach and intestine (with contents) weights.However, these findings are insufficient to suggest any effect on saciety since no difference was observed in the food intake between the groups


El aumento de la ingestión de fibra alimentar ha sido una importante estrategia para el control de la obesidad y sus comorbidades. La quitosana,una fibra de origen animal, está siendo responsabilizada por reducir la absorción de grasas a nivel intestinal, disminución del colesterol y la glucosa séricos y también por la inhibición del apetito y reducción del peso corporal. Este estudio evaluó el efecto de la incorporación de quitosana en polvo, en dietade ratas adultas, sobre algunos parâmetros nutricionales y bioquímicos. Ratas Wistar (n=14) fueron divididas en grupo control (GC), raciónAIN-93G, a base de caseína y celulosa microcristalina (5%) y grupo quitosana e (GQ),ración AIN-93G y quitosana en polvo (5%) em substitución de la celulosa micro cristalina, por10 días. No se observaron diferencias en el consumo alimentar ni en la evolución de los pesos corporal o del hígado, de los depósitos de grasa abdominal y de la carcasa, ni tampoco en las concentraciones séricas de glucosa,proteínas totales y perfil lipídico. Sin embargo, el grupo GQ presentó menores pesos de estómago e intestino delgado (con su contenido). No obstante, estos resultados son insuficientes para deducir algún efecto en la saciedade considerando que no se observó diferencia en el consumo de ración de los grupos


O maior consumo de fibra alimentar tem sido uma das importantes estratégias para o controle e prevenção da obesidade e suas co-morbidades. A quitosana, fibra de origem animal, vem sendo relacionada à redução da absorção de gorduras em nível intestinal, do colesterol e glicose séricos e, também, com inibição do apetite e redução de peso corporal. Este estudo avaliou os efeitos do uso de quitosana em pó, na ração de ratas adultas, sobre alguns parâmetros nutricionais e bioquímicos. Ratas Wistar adultas (n=14) foram divididas em grupo controle (GC): ração AIN-93G, à base de caseína e celulose microcristalina (5%) e grupo quitosana (GQ): dieta AIN-93G e quitosana em pó (5%), em substituição à celulose microcristalina, por 10 dias. Não se observaram diferenças no consumo alimentar, na evolução do peso corporal, do fígado, dos depósitos de gordura abdominal e da carcaça, e, nem tampouco nas concentrações séricas de glicose, proteínas totais e no perfil lipídico. O GQ apresentou menor peso do estômago e do intestino delgado (com conteúdo) sendo, entretanto esses resultados, insuficientes para inferir sobre algum efeito na saciedade, tendo em vista que não foi observada diferença no consumo de ração entre os grupos


Subject(s)
Animals , Rats , Chitosan/analysis , Chitosan/metabolism , Chitosan/therapeutic use , Dietary Fiber/administration & dosage , Reference Standards/analysis , Reference Standards/statistics & numerical data , Satiety Response
15.
Acta cient. venez ; 56(1): 16-23, 2005. tab, graf
Article in Portuguese | LILACS | ID: lil-537186

ABSTRACT

Fueron evaluados los efectos de la adición de diferentes niveles de quitosana en salchichas tipo frankfurter con bajo contenido de gordura sobre la composición química, rendimiento y perfil de textura instrumental (TPA) y sensorial en relación a la salchicha control (C), sin adición de quitosana y con el mismo porcentaje de gordura. Después del procesamiento las salchichas fueron empacadas al vacío y almacenadas a 4ºC para análisis posterior. Los resultados obtenidos mostraron que la adición de quitosana, con los porcentajes utilizados, no presentaron diferencias significativas (p<0.05) sobre la composición química y rendimiento, cuando comparadas con la salchicha control. El perfil de textura instrumental de la salchicha control con relación a las demás con adición de quitosana, no presentó diferencias significativas (p<0.05) para las características de adesividad, elasticidad y coesividad, mientras que hubo diferencias con relación a la dureza, gomosidad y masticabilidad. El perfil sensorial no mostró diferencias (p<0.05) entre el control y las salchichas con diferentes niveles de quitosana, en todas las propiedades sensoriales evaluadas. La matriz de correlación entre las variables instrumental y sensorial demostró que no hubo correlación entre la dureza sensorial y la dureza instrumental. El coeficiente de correlación sensorial mostró alta correlación entre la elasticidad con la gomosidad, y buena correlación entre la dureza con fracturabilidad, adhesividad y liberación de humedad.


Effects of addition of several concentrations of chitosan to low-fat Frankfurter-type sausage on the chemical composition, yield, Textural (instrumental) and sensory perfil analysis were evaluated. The sausages were processed, vacuum packed and stored at 4ºC. There were no significant differences in chemical composition and yield for the sausages with and without chitosan. According to the textural instrumental analysis there were no significant differences in adhessiveness, elasticity, and cohesiveness. However, there were significant differences for hardness, gumminess and chewiness. The sensory analysis profile was similar for the control and the chitosan containing samples according to all the characteristic evaluated. The correlation matrix between instrumental and sensory analysis showed that there was no correlation between the instrumental and the sensory hardness. The sensory correlation coefficient showed a strong correlation between elasticity with gumminess, and a good correlation between hardness and with fracturability, adhesiveness e moisture loss.


Subject(s)
Meat/analysis , Food Analysis , Glucosamine/analysis , Chitosan/analysis , Chitosan/chemistry , Food Technology
16.
Article in Malayalam | WPRIM | ID: wpr-629931

ABSTRACT

Various proportions of chitosan/collagen films (70/30% to 95/05%) w/w were prepared and evaluated for its suitability as skin regenerating scaffold. Interactions between chitosan and collagen were studied using Fourier Transform Infrared spectroscopy (FTIR) and Differential Scanning Colorimetry (DSC). Scanning Electron Microscope (SEM) was used to investigate the morphology of the blend. Mechanical properties were evaluated using a Universal Testing Machine (UTM). The chitosan/collagen films were found to swell proportionally with time until it reaches equilibrium. FTIR spectroscopy indicated no chemical interaction between the components of the blends. DSC data indicated only one peak proving that these two materials are compatible at all proportions investigated. SEM micrographs also indicated good homogeneity between these two materials.


Subject(s)
Biocompatible Materials/analysis , Burns/physiopathology , Burns/therapy , Chitosan/analysis , Collagen Type I/analysis , Materials Testing , Microscopy, Electron, Scanning , Occlusive Dressings , Regeneration/physiology , Skin/physiopathology , Spectroscopy, Fourier Transform Infrared , Tensile Strength
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