Desenvolvimento de formas farmacêuticas semissólidas a partir de capim-limão (Cymbopogon citratus)

O capim-limão (Cymbopogon citratus, Poaceae) é uma planta herbácea com diversas propriedades medicinais, entre elas atividade antimicrobiana e antifúngica. Apesar do seu amplo uso etnofarmacológico, não há medicamentos fitoterápicos disponíveis, sendo sua utilização restrita a preparações caseiras (infusão). Logo, a presente pesquisa teve por objetivo avaliar estabelecer as condições de obtenção da droga vegetal e do extrato, bem como, incorpora-lo em formulações para uso tópico. A droga vegetal foi obtida em sala com desumidificação após 3 dias de armazenamento. O processo extrativo foi investigado por meio de um planejamento fatorial tendo a relação droga:solvente e concentração de etanol no solvente extrator como variáveis. Foi observado que a proporção 1:15 (droga:solvente, m/v) e etanol a 20% resultou em extratos com maior resíduo seco. Após eliminação do etanol e concentração do extrato, foram preparadas formulações semissólidas (emulsão e gel). A emulsão testada não apresentou estabilidade (separação de fase) durante o preparo, enquanto o gel resultou em uma formulação de aspecto grumoso, mas com boa espalhabilidade na pele. Assim, observa-se a potencialidade do capim-limão no desenvolvimento de formulações antissépticas de uso tópico, contudo, estudos adicionais são necessários para obtenção de uma forma farmacêutica estável, segura e eficaz

Toltrazuril-loaded polymeric nanocapsules as a promising approach for the preventive control of coccidiosis in poultry

Coccidiosis is a disease caused by intracellular protozoan parasites of the genus Eimeria that affect the intestinal tract of poultry. However, strain resistance and drug residue in the carcass have drawn the attention of the productive sector. The nanotechnology can improve the biological effect of drugs, reducing of administered doses and toxic effects. Due to this, toltrazuril-load polymeric nanoparticles based on Eudragit® S100 (NCt) or poly-"-caprolactone (LNCt) were developed to prevent coccidiosis in broilers. Nanoformulations were produced and showed homogeneous particle diameter distribution in the nanometer range (z-average and D (4.3) 90%. Cell viability assays using avian fibroblasts showed that LNCt presented no relevant toxicity up to 72 h. LNCt was then prophylactically administrated to chicken followed by challenge with Eimeria oocysts. The evaluation of the small intestine and cecum showed that the treatment with LNCt (3.5 mg/kg/day) in drinking water reduced the lesion scores and oocysts excretion, similar to the reference medicine containing toltrazuril (Baycox®, 7 mg/kg/day). The current study shows the potential protective use of nanoencapsulating anticoccidial drugs as a promising approach for the control of coccidiosis in poultry

Development of mucoadhesive nanocapsules of poly(ε-caprolactone) and poly(methyl methacrylate-b-2-(methylamino)ethyl methacrylate) blend and their evaluation as nose-to-brain drug delivery system

A liberação intranasal de fármacos tem sido proposta como estratégia para escapar da seletividade da barreira hemato-encefálica. Recentemente, o uso da nanotecnologia tem sido uma abordagem promissora para a liberação cerebral pela via nasal, uma vez que o encapsulamento de fármacos em nanocarreadores tem aumentado sua distribuição cerebral, assim como melhorado seus efeitos farmacológicos quando comparados ao fármaco em solução. Além disso, para garantir um bom desempenho, tais formulações requerem propriedades mucoadesivas. Nesse contexto, esta tese apresenta a síntese de um copolímero anfifílico em bloco [Poli(MMA-b-DMAEMA)] e sua utilização para preparar nanocápsulas poliméricas com Poli(ε-caprolactona) para biodistribuição cerebral de fármacos pela via nasal. Elas apresentaram resposta frente a variações de pH devido a presença do revestimento com Poli(DMAEMA) (uma poliamina). As propriedades mucoadesivas foram estabelecidas em relação à capacidade de interagir com mucina e de aumentar a retenção de um fármaco em mucosa nasal in vitro. A partir desses resultados, foi realizada a avaliação biológica das nanocápsulas contendo um fármaco modelo (olanzapina) e foi verificado que a administração intranasal da formulação em ratos aumentou o teor de fármaco no cérebro de ratos, o que acarretou maior atividade antipsicótica em um modelo animal de esquizofrenia. Ainda, não foi verificado dano a mucosa nasal dos ratos após a administração das nanocápsulas brancas em dose única ou repetidas, sugerindo a segurança do sistema. Além disso, foi investigada a capacidade do nanocarreador desenvolvido de encapsular fármacos, sendo verificado que tanto moléculas hidrofílicas quanto hidrofóbicas podem ser encapsuladas através de um algoritmo desenvolvido para predizer o mecanismo de distribuição nas nanocápsulas. Esses achados mostram que as nanocápsulas delineadas com propriedades mucoadesivas são promissoras para o carreamento de fármacos no sistema nervoso central após administração intranasal.The intranasal delivery of drugs has been proposed as strategy to overcome the brain blood barrier selectivity. Recently, the use of nanotechnology has been a promising approach for nose-to-brain delivery, since the entrapment of drugs into nanocarriers has increased their distribution into brain as well as improved their pharmacological effects when compared to the drug solution. Besides, mucoadhesive properties are required to the formulation to enhance its performance. Based on this, this thesis presents the synthesis of an amphiphilic block copolymer [Poly(MMA-b-DMAEMA)] and its application to prepare polymeric nanocapsules with Poly(ε-caprolactone) for nose-to-brain drug delivery. They were pH-sensitive due to the presence of the Poly(DMAEMA) coating (a polyamine). The mucoadhesive properties were evaluated in terms of ability to interact with mucin and to increase the drug residency on nasal mucosa in vitro. Considering these findings, biological studies were carried out and the intranasal application of the formulation in rats increased the model drug (olanzapine) in brain, what led to improved antipsychotic effects in an animal model of schizophrenia. Also, no damage to rat nasal mucosa was observed after single or repeated doses of blank nanocapsules, suggesting the system safety. In addition, the ability of the developed nanocarrier to entrap drugs was investigated and both hydrophilic and hydrophobic molecules could be encapsulated, so that an algorithm was proposed to predict the drug distribution mechanism in the nanocapsule. These findings show that the designed nanocapsules with mucoadhesive properties are promising for nose-to-brain drug delivery after intranasal administration

Influência dos grupos terapêuticos em Centro de Atenção Psicossocial entre usuários com dependência de cocaína/crack

Analisa a influência dos grupos terapêuticos em Centro de Atenção Psicossocial entre usuários com dependência de cocaína/crack, em Fortaleza - Ceará. Estudo descritivo e retrospectivo, entre 2009 e 2010. Realizou-se uma análise bivariada entre as variáveis dependentes e independentes. Os grupos terapêuticos foram influenciados pela profissão, por abandono de tratamento, drogas ilícitas, número de consultas e prescrições. Observa-se a necessidade de elaborar estratégias para melhorar as ações preventivas comunitárias, visando a aumentar a adesão dos dependentes de cocaína/crack às atividades terapêuticas, conforme a legislação vigente de saúde mental

A polyvalent virosomal influenza vaccine induces broad cellular and humoral immunity in pigs

Abstract Background Influenza A virus (IAV) is endemic in pigs globally and co-circulation of genetically and antigenically diverse virus lineages of subtypes H1N1, H1N2 and H3N2 is a challenge for the development of effective vaccines. Virosomes are virus-like particles that mimic virus infection and have proven to be a successful vaccine platform against several animal and human viruses. Methods This study evaluated the immunogenicity of a virosome-based influenza vaccine containing the surface glycoproteins of H1N1 pandemic, H1N2 and H3N2 in pigs. Results A robust humoral and cellular immune response was induced against the three IAV subtypes in pigs after two vaccine doses. The influenza virosome vaccine elicited hemagglutinin-specific antibodies and virus-neutralizing activity. Furthermore, it induced a significant maturation of macrophages, and proliferation of B lymphocytes, effector and central memory CD4+ and CD8+ T cells, and CD8+ T lymphocytes producing interferon-γ. Also, the vaccine demonstrated potential to confer long-lasting immunity until the market age of pigs and proved to be safe and non-cytotoxic to pigs. Conclusions This virosome platform allows flexibility to adjust the vaccine content to reflect the diversity of circulating IAVs in swine in Brazil. The vaccination of pigs may reduce the impact of the disease on swine production and the risk of swine-to-human transmission

Eugenol as a Promising Molecule for the Treatment of Dermatitis: Antioxidant and Anti-inflammatory Activities and Its Nanoformulation

Contact dermatitis produces an inflammatory reaction primarily via stimulation of keratinocytes and cells of the immune system, which promote the release of cytokines, reactive oxygen species (ROS), and other chemical mediators. Eugenol (EUG, phenylpropanoid of essential oils) has attracted attention due to its anti-inflammatory properties, as well as antioxidant effect. On the other hand, it is volatile and insoluble and is a skin irritant. In this case, nanostructured systems have been successfully employed as a drug carrier for skin diseases since they improve both biological and pharmaceutical properties of active compounds. The cytotoxic, antioxidant, and anti-inflammatory effects of EUG were assessed in human neutrophils and keratinocytes. Additionally, polymeric nanocarries (NCEUG) were prepared to improve the chemical and irritant characteristics of EUG. EUG presented apparent safety and antioxidant and anti-inflammatory effects on human neutrophils, but presented cytotoxic effects on keratinocytes. However, the nanocapsules were able to reduce its cytotoxicity. An in vivo experiment of irritant contact dermatitis (ICD) in mice induced by TPA showed that NCEUG reduced significantly the ear edema in mice when compared to the EUG solution, as well as the leukocyte infiltration and IL-6 level, possibly due to better skin permeation and irritancy blockage. These findings suggest that EUG is a promising bioactive molecule, and its nanoencapsulation seems to be an interesting approach for the treatment of ICD

NEOTROPICAL CARNIVORES: a data set on carnivore distribution in the Neotropics

Mammalian carnivores are considered a key group in maintaining ecological health and can indicate potential ecological integrity in landscapes where they occur. Carnivores also hold high conservation value and their habitat requirements can guide management and conservation plans. The order Carnivora has 84 species from 8 families in the Neotropical region: Canidae; Felidae; Mephitidae; Mustelidae; Otariidae; Phocidae; Procyonidae; and Ursidae. Herein, we include published and unpublished data on native terrestrial Neotropical carnivores (Canidae; Felidae; Mephitidae; Mustelidae; Procyonidae; and Ursidae). NEOTROPICAL CARNIVORES is a publicly available data set that includes 99,605 data entries from 35,511 unique georeferenced coordinates. Detection/non-detection and quantitative data were obtained from 1818 to 2018 by researchers, governmental agencies, non-governmental organizations, and private consultants. Data were collected using several methods including camera trapping, museum collections, roadkill, line transect, and opportunistic records. Literature (peer-reviewed and grey literature) from Portuguese, Spanish and English were incorporated in this compilation. Most of the data set consists of detection data entries (n = 79,343; 79.7%) but also includes non-detection data (n = 20,262; 20.3%). Of those, 43.3% also include count data (n = 43,151). The information available in NEOTROPICAL CARNIVORES will contribute to macroecological, ecological, and conservation questions in multiple spatio-temporal perspectives. As carnivores play key roles in trophic interactions, a better understanding of their distribution and habitat requirements are essential to establish conservation management plans and safeguard the future ecological health of Neotropical ecosystems. Our data paper, combined with other large-scale data sets, has great potential to clarify species distribution and related ecological processes within the Neotropics. There are no copyright restrictions and no restriction for using data from this data paper, as long as the data paper is cited as the source of the information used. We also request that users inform us of how they intend to use the data