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ANA CAROLINA DA SILVA COSTA
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NANOPARTÍCULAS DE QUITOSANA CONTENDO ALBENDAZOL PARA APLICAÇÃO NA SANIDADE DE TAMBAQUIS AMAZÔNICOS (Colossoma macropomum
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Data: 20/12/2019
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A intensificação da atividade pesqueira oriunda do incentivo a produção do agronegócio do pescado é uma realidade mundial que traz a necessidade de desenvolvimento de novas alternativas farmacêuticas mais eficazes, sustentáveis e racionais contra a disseminação de agentes infecciosos e parasitários como da classe Monogenea frequentemente encontrada em Tambaquis amazônicos (Colossoma macropomum) Objetivo: Este estudo teve como objetivo obter e caracterizar nanopartículas de quitosana (CS) contendo albendazol (ABZ) para aplicação na sanidade de tambaquis. Metodologia:.Foi realizado estudo teórico através de simulações por dinâmica molecular para avaliar as interações entre CS e ABZ . As nanopartículas quitosana albendazol (NP/CS-ABZ) foram preparadas pela técnica de emulsão reticulação volátil e caracterizadas físico-quimicamente, realizados estudo de estabilidade de 65 dias e os efeitos da atividade eletromiografica e parâmetros hematologicos de tambaquis parasitados com monogenea sp antes e apos tratamento com (NP/CS-ABZ). Resultados e discussão: Simulações por dinâmica molecular evidenciaram interações favoráveis entre CS e ABZ e espontaneidade para a formação das NP/CS-ABZ, foram obtidas teor médio 70% e DL 14,99% tamanho de 167,4 nm; PDI :0,251 e carga + 42,2 e melhor estabilidade em ambiente de geladeira (GEL) após 65 dias. Através das análises eletromiograficas ( EMG), para o grupo parasitado observou-se menor tempo de contração muscular e maior tempo de descanso. e grupo desparasitado, mesmo após 72 horas de tratamento, a atividade muscular não retornou ao normal quando comparado ao controle Conclusões: NP/CS-ABZ mostrou alta capacidade de carreamento e liberação sustentada de ABZ contra monogeneas que interferem no processo de contração muscular e podem prejudicar estímulos de reação do tambaqui a predação e fuga.
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ANTONIO TAYLON AGUIAR GOMES
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Nanostructured lipid carriers based tucuman fat (astrocaryum vulgare) containing ketoconazole
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Data: 19/12/2019
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Nanostructured lipid carriers (CLN) are drug delivery systems composed ofnanometer sized particles, these nanocarriers have been applied in dermocosmetic formulationsbecause they promote sustained release and better absorption of the assets, among otheradvantages. Amazonian vegetable fats are considered lipid matrices of great potential for theproduction of CLN, due to their low toxicity, biocompatibility and their emollient, skin occlusive andantioxidant properties. The Tucumã (Astrocaryum vulgare Mart.) Is a palm tree found in SouthAmerican countries such as Bolivia, Brazil, Guyana, French Guiana and Suriname. Tucumã seedfat is popularly used in moisturizing hair and skin because it is excellent emollient and has a goodspread. Objective: In this work we aim to obtain and characterize nanostructured lipid carriers(CLN) from the tucumã fat (Astrocarym vulgare) and to test it against fungal culture. Methodology:Fat was evaluated for acidity index, refractive index, iodine index, gas chromatographic fatty acidprofile, differential exploratory calorimetry melting point and Fourier transform infrared spectrumprofile. The best lipid mixture was determined by DSC and XRD tests. A factorial design wasperformed to determine the best formulations. The formulations prepared by high pressurehomogenization were evaluated for encapsulation efficiency, carrying capacity, ph, zeta potential,particle size for 70 days. A drug release test, minimum inhibitory concentration and minimumfungicidal concentration were performed. Results and discussions: The acidity, refraction andiodine index of tucumã fat were respectively 2.73; 1.499 and 15.11. The fatty acid profile showedthat fat has a large amount of lauric, myristic and oleic acid. The melting point occurs at 35 ° C andthere was no other thermal event up to 200 ° C. Through the infrared spectrum profile andthermogravimetry, we observed that fat is basically composed of fatty acid triglycerides. The bestlipid mixture was tucumã fat with carnauba wax in the proportion of 50% of each. The CLN4formulation showed an encapsulation efficiency of 80%, released 40% of the drug in 8 hours and80% in 60 hours and showed a 0.25 μg / mL inhibition of fungal growth, 8 times better thaninhibition. Conclusions: Tucumã fat is of excellent quality and its use in the production ofketoconazole-containing lipid carriers showed excellent encapsulation efficacy, controlled drugrelease and improved ketoconazole antifungal activity.capsulation efficacy, controlled drug releaseand improved ketoconazole antifungal activity.
Keywords: Astrocaryum vulgare, Nanostructured lipid carrier, ketoconazole, factorial design, highpressure homogenization.
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DAYSE LÚCIA DO NASCIMENTO BRANDÃO
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Medicinal importance of Portulaca pilosa L. for Amazon region Brandão
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Data: 17/12/2019
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Portulaca pilosa is widely used in Amazonian folk medicine to treat different diseases, such as diarrhea, gastric problems, scarring, febrile diseases, malaria, among others. Chemical studies are scarce and reported the isolation of diterpenes. In addition, there is a lack of biological studies that contradict the results obtained, justifying the realization of the present thesis. Objective: To evaluate, on different aspects, the medicinal importance of P. pilosa. Methodology: For integrative reviews of ethnobotanical and biological studies, different databases were searched. The construction of the malaria vicious cycle article required a literature review, as well as meetings for the critical analysis of the results obtained. Predmet, Pass online, Molinspiration, Smartcyp, Protox, Pred-Herg, CPi-PREDICTOR and SuperPerd were used for in silico studies. Plants were processed, obtaining the ethanolic extract of the area parts (EEPP), which was fractionated in a chromatographic column using silica as a stationary phase and solvent mixtures of increasing polarities as a mobile phase. The extract and its fractions were monitored by thin layer chromatography and high performance liquid chromatography analyzes coupled to diode arrays. Antiplasmodic activity was performed in clone W2 by the LDH method and leishmanicidal activity in L. chagasi and L. amazonensis isolates. Results and discussion: Several claims of popular use lack biological studies, but some indications already have preliminary studies that demonstrate the high pharmacological potential of the species. One use claim is as wound healing, though if Leishmania causes the wound, the preliminary results suggest that P. pilosa may not be promising. However, in the case of malaria, the EEPP was promising (IC50 = 18.35 µg / mL) and fractionation contributed to the activity, with the active fractions ethyl acetate and methanolic (IC50 = 5.77 µg / mL and IC50 = 7.53 µg / mL), it appears that this activity is related to diterpenes. In silico studies suggest that diterpenes are not mutagenic, carcinogenic and have favorable pharmacokinetics. Conclusion: P. pilosa is very important for Amazonian medicine, presenting promising results as antimalarial and it seems that diterpenes are involved in this activity.
Keywords: Portulaca pilosa, malaria, diterpene.
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VALDICLEY VIEIRA VALE
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Eleutherine pilcata was promising as an antiplasmodic agent, the dichloromethane and isoleuterine fraction presented superior genotoxic effect than the negative control. Objective: To conduct chemical and antiplasmodic studies of E. plicata, investigating possible mechanisms of action and pharmacological marker. Methodology: Isoeleuterine analogs were submitted to in silico prediction evaluation for biological, pharmacokinetic and toxicity activities. dockingMolecular was performed for the majority compounds. The ethanol extract was fractionated and from the dichloromethane fraction were isolated substances, which were identified by spectroscopic methods and were submitted to antiplasmodic evaluation by the traditional microstest method and parasitic lactate dehydrogenase. Parasitic changes were also evaluated by transmission electron microscopy and evaluated the inhibition of β-hematin formation. Results: In in silico studies, no proposed alteration of isoeleuterine decreased toxicity, did not significantly alter pharmacokinetic aspects, biological activities were antineoplastic and antimalarial. Eleuterine and isoleuterine bound to cyt bc1 similarly to atovaquone. From the extract were isolated two naphthoquinones: eleuterine and isoeluterine, two naphthalenes, eleuterol and hongconin, an anthraquinone. Fractionation of the extract led to higher antiplasmodic activity (IC50 dichloromethane fraction <10 μg / mL). The antiplasmodic activity of this fraction was attributed to eleuterine (3d7 = 8.05 ± 6.48; 6.35 ± 1.93; W2 = 5.72 ± 3.49; 14.18 ± 4.19 μg / mL) and isoeleuterine isomer (3d7 = 2.57 ± 0.78; 8.63 ± 0.85; W2 = 3.38 ± 1.97; 7.01 ± 1.16 μg / mL), but their selectivity indices were less than 1. Transmission electron microscopy analyzes showed that isoleuterine and eleuterine alter mitochondrial morphology, decrease hemozoin, cause cytoplasmic inclusions and dense chromatin in P. falciparum. These compounds did not inhibit β-hematin formation. Conclusion: Eleuterine and isoeleuterine are responsible for the antiplasmodic activity of E. plicata, causing changes in various parasite structures and ultrastructures and it seems that their antiparasitic effect may be similar to atovaquone.
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Data: 16/12/2019
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Keywords: Eleutherine plicata; naphthoquinones; antiplasmodial.
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LUCIANO APARECIDO STECANELLA
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Nano/microparticle inhalation containing glycyrrhizin for chronic respiratory disease treatment.
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Data: 24/09/2019
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As doenças respiratórias crônicas (DRCs) são doenças das vias respiratórias, sendo as mais comuns: doença pulmonar obstrutiva crônica (DPOC), asma, alergias respiratórias e hipertensão pulmonar. As principais causas, além do cigarro, incluem a poluição do ar, produtos químicos, e frequentes infecções respiratórias na infância. De acordo com as últimas estimativas da OMS (2017), obtidas em 2004, mostram que 235 milhões de pessoas têm asma, 64 milhões de pessoas têm a doença pulmonar obstrutiva crônica (DPOC), levando a 3 milhões de mortes/ano, o que pode levar a se tornar a terceira causa de morte em todo o mundo até 2030. Somente na Europa as DRCs são responsáveis por 315.000 mortes/ano e custa às economias 300 bilhões de euros/ano. A terapêutica atualmente disponível para o tratamento das DRCs, como corticosteroides, broncodilatadores, antiinflamatórios, inibidores da enzima fosfodiesterase 4 e inibidores de receptores de leucotrienos, apresentam muitos efeitos colaterais, existindo a necessidade de novas moléculas que atuem de forma mais específica, havendo assim grande interesse em plantas medicinais e suas substâncias isoladas. Sendo assim, foi escolhido para este trabalho o fármaco glicirrizina, um glicosídeo triterpênico, com comprovada atividade anti-inflamatória, antiviral, antitumoral, hepatoprotetora, anti-ulcerosa, anti-alérgica, anti-oxidantes, etc. Visando um tratamento mais eficiente das DRCs, novas vias de administração e formulações que ajam mais diretamente no local de ação estão sendo pesquisadas, sendo assim, a via pulmonar é a primeira escolha, e os produtos inalatórios, são a primeira escolha neste tipo de terapêutica. Dentre estas formas farmacêuticas, os pós inalatórios estão no centro das pesquisas. Portanto, o objetivo será produzir pós nano/microparticulados contendo glicirrizina, caracterizados por um elevado teor do fármaco, respirabilidade e fluidez, e que seja seguro e eficaz. Nos resultados parciais obtidos, foi possível caracterizar o fármaco, através das técnicas de espectrometria de massas, RMN, FTIR, DRX e análise térmica por DSC e TG, também os excipientes, através das técnicas de FTIR, DRX e análise térmica por DSC e TG, e avaliar a compatibilidade entre fármaco e excipientes pelas FTIR, DRX e análise térmica por DSC, sendo concluído que os mesmos são compatíveis. Também foi realizado o desenvolvimento e validação do método de análise de acordo com a RE 899.2003 da ANVISA, o que permite detectar e quantificar o fármaco. Foram obtidas nanopartículas de lecitina/quitosana, conforme técnica descrita por Barbieri et al. 2013, com tamanho médio de 208 nm, PdI de 0,187 e zeta potencial de +30,5 mV, mas em visualização por MET foi verificado que elas possuem tamanho inferior a 100 nm, o que nos leva a sugerir que a técnica de DSL está apresentando valores de diâmetro hidrodinâmico de populações homogêneas de aglomerados, e não de nanopartículas isoladas.
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RAYANNE ROCHA PEREIRA
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Nanostructured lipid carriers based ucúuba fat (Virola surinamensis) for transungual administration of antifungal drugs
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Data: 08/07/2019
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Introduction: Ucúuba fat (Virola surinamensis) is used in the Amazon region of northern Brazil to produce candles, creams and medicinal soaps. It is rich in myristic and lauric acid, giving subsides for use as raw material for the production of nanostructured lipid carriers (NLC). Objective: The objective of this work was to use Ucúuba fat as an oil phase for the production of NLC and to evaluate the transungual permeation of NLC loaded with ketoconazole, used as a model drug, to treat onychomycosis. Method: Ucúuba fat was characterized as fatty acid, triglyceride, crystallinity and polymorphism. Through an experimental design Box-Behnken type we optimize the conditions of preparation of NLC. Using a Franz cell model, we evaluated the permeation of ketoconazole over a 24-hour period through the nail plate using porcine nail tissue. Results: Ucúuba fat is rich in myristic and lauric acids, trimyristin is the main triglyceride of the ucúuba fat, the melting point was approximately 42°C, crystallizes predominantly in polymorph β'. The NLCwere standardized in two specific sizes to evaluate the influence of this parameter on nail permeation, the formulations were denominated F30 and F85, and presented 33.4nm and 74.6nm, respectively. Permeation studies showed that none of the formulations crosses the nail, but accumulates in the nail plate at concentrations greater than the inhibitory minimum concentration (MIC) for ketoconazole. Finally, to facilitate application of the formulations to the nail, we used chitosan for the gelation of F85, as this formulation showed a better result of the accumulation of ketoconazole in the nail. Conclusion: Although they are a lipid system, NLC were able to allow the penetration of ketoconazole in the nail at concentrations above the MIC, showing to be a promising vehicle for the transungual administration of antifungals.
Keywords: Virola surinamensis; nanostructured lipid carriers (NLC), onychomycosis, uuculean fat, Box- Behnken
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