ABSTRACT Purpose: The present study aimed at testing a new formulation of mesalazine linked to chondroitin sulfate and its components alone in the treatment of actinic proctitis in rats. Methods: Forty-seven female Wistar rats were submitted to pelvic radiation and divided into eight groups: control A, mesalazine A, chondroitin A, and conjugate A, gavage of the according substance two weeks after irradiation and sacrifice three weeks after oral treatment; control C, mesalazine C, chondroitin C, and conjugate C, sacrifice six weeks after oral treatment. The rectum was submitted to histological characterization for each of the findings: inflammatory infiltrate, epithelial degeneration, mucosal necrosis, and fibrosis. Results: The inflammatory infiltrate was more intense in chondroitin A, mesalazine A, and conjugate C. The collagen deposition was less intense in chondroitin A, and mesalazine A, and more intense in control C. Conclusions: Mesalazine and chondroitin alone were efficacious in inducing a delayed inflammatory response, hence reducing the late fibrosis. The conjugate was able to induce an ever more delayed inflammatory response.

Abstract Purpose To evaluate different concentrations of ciprofloxacin to prevent infection after open fracture contaminated with S. aureus in rats using absorbable local delivery system. Methods Fifty-two Wistar rats were assigned to six groups. After 4 weeks, all animals underwent 99mTc-ceftizoxima scintigraphy evaluation, callus formation measurement and histological analysis. ANOVA, t-Student and Kruskal Wallis were used for quantitative variables statistical analysis, whereas qui square and exact Fisher were used for qualitative variables. Results Treatment using 25% and 50% of ciprofloxacin incorporated at the fracture fixation device were effective in preventing bone infection compared to control group (p<0.05). Chitosan were not effective in preventing bone infection when used alone compared to control group (p>0.05). Histological findings demonstrated bone-healing delay with 50% of ciprofloxacin. No difference in callus formation were observed (p>0.05). Conclusion Local delivery treatment for contaminated open fracture using chitosan with ciprofloxacin is effective above 25%.

Resumo Campomanesia lineatifolia Ruiz & Pavón (gabiroba) é uma espécie nativa comestível encontrada na Floresta Tropical Amazônica. Estudos prévios têm demonstrado a natureza flavonoídica do extrato etanólico das folhas de C. lineatifolia, além de atividade gastroprotetora e inibição do TNF. No entanto, o processo de extração utilizado foi longo e consumiu uma grande quantidade de solvente. Portanto, o objetivo deste estudo foi obter um extrato bioativo rico em fenólicos, através de um método extrativo simples, rápido e de baixo custo de execução. As folhas de C. lineatifolia foram secas e trituradas e as extrações conduzidas em diferentes solventes / misturas (etanol, metanol, acetato de etila e água) sob banho ultrassônico, agitação eletromagnética e sistema contínuo de refluxo. A eficiência da extração foi avaliada pela concentração do componente flavonoídico majoritário nos extratos, em um método desenvolvido por cromatografia líquida de ultra eficiência. Ensaios de injeção e coinjeção com padrões autênticos, análises em cromatografia líquida de ultra eficiência acoplada à espectrometria ultravioleta foram conduzidos para identificar a presença de catequina e quercitrina. Demonstrou-se que a extração etanólica sob sistema contínuo de refluxo e a mistura de etanol:água (8:2) sob banho ultrassônico representaram métodos otimizados na obtenção dos componentes flavonoídicos identificados. Assim, os resultados obtidos podem contribuir para a padronização químico-biológica do extrato para a avaliação da atividade antiúlcera gástrica.

Abstract Campomanesia lineatifolia (gabiroba) is a native edible species found in the Amazon Rainforest. Previous studies have demonstrated the flavonoid nature of ethanolic extract from the C. lineatifolia leaves, in addition to gastroprotective activity and TNF inhibition. However, the extraction process used was long and consumed a large amount of solvent. Therefore, the objective of this study was to obtain a bioactive extract rich in phenolics, in an extractive method of simpler, faster, and lower-cost execution. The C. lineatifolia leaves were dried and crushed, and the extractions were carried out in different solvents/mixtures (ethanol, methanol, ethyl acetate, and water) under ultrasonic bath (UB), electromagnetic stirring, and continuous reflux extraction (R). The extraction efficiency was evaluated by the flavonoid major compound concentration in the extracts, in a method developed by ultra-high performance liquid chromatography (UHPLC). Injection and pattern matching tests, and UHPLC analyses coupled to ultraviolet spectrometry were conducted to identify catechin and quercitrin. It has been demonstrated that the ethanolic extraction by R and the mixture of ethanol: water (8:2) by UB represented optimized methods in obtaining the flavonoid compounds identified. Thus, the results may contribute to chemical-biological extract standardization for gastric antiulcer activity evaluation.

Neste estudo, verificou-se a utilização de um filme de quitosana para o controle do crescimento e produção de aflatoxinas por A. parasiticus em amendoim. Os filmes foram aplicados sobre os grãos por meio de duas metodologias (aspersão e imersão). Os grãos recobertos foram inoculados com 2,5 ml de uma suspensão contendo 1,0×106 esporos/ml e incubados a 25 oC por 7 dias. A concentração de aflatoxinas foi determinada por cromatografia em camada delgada, utilizando a técnica de densitometria. A verificação da inibição do crescimento fúngico foi realizada por meio da inoculação do patógeno em placas de Petri contendo GYEP suplementado com quitosana a 2% e incubadas por 7 dias a 25 ºC. Após incubação, o diâmetro da colônia do patógeno foi estimado e comparado com o controle. Todos os testes foram realizados com cinco repetições. Para a verificação de alterações morfológicas, uma suspensão de esporos ou hifas incubados na presença de quitosana foi submetida à microscopia eletrônica de varredura. Foi observado que tanto o método de imersão quanto o de aspersão reduziram a produção de aflatoxina significativamente, 84,3% e 86,7% respectivamente. A presença de quitosana no meio de cultura reduziu o diâmetro das colônias e promoveu modificações morfológicas nos esporos de A. parasiticus. Com esse procedimento foi verificado que a utilização de quitosana a 2% na forma de filme, principalmente por aspersão, pode reduzir a concentração de esporos e aflatoxinas de A. parasiticus em amendoim, o que confere a essa substância uma grande perspectiva de utilização no controle de fungos aflatoxigênicos.

In this study, we evaluate the utilization on chitosan film to control the growth and aflatoxin production by A. parasiticus in peanut. The films were inoculated over the grains by aspersion or immersion methods. The chitosan coated grains were inoculated with 2.5 ml solution with 1.0×106spores/ml and incubated at 25 °C for 7 days. The aflatoxin concentration was estimated by thin layer chromatography and densitometry. The fungus growth inhibition was observed by pathogen inoculation in Petri dishes with GYEP media plus 2% chitosan and incubated by 7 days at 25 °C. After incubation the colony diameter was measured and compared with the control. All assays were repeated five times. To verify morphological alterations, a spore/hypha suspension was incubated in media with chitosan and observed in scanning electron microscopy.Both methods (immersion and aspersion) were able to reduce the aflatoxin production significantly, 84.3% and 86.7%, respectively. The chitosan reduced the colonies diameters and promoted morphological alterations in A. parasiticus spores. With this, was observed that a 2% chitosan film, specially inoculated by aspersion, can to reduce A. parasiticus spores and aflatoxins concentrations in peanuts. This characteristic gives to this substance an excellent perspective to be used in aflatoxigenic fungi control.

Leishmaniasis is one of the six major tropical diseases targeted by the World Health Organization. It is a life-threatening disease of medical, social and economic importance in endemic areas. No vaccine is yet available for human use, and chemotherapy presents several problems. Pentavalent antimonials have been the drugs of choice to treat the disease for more than six decades; however, they exhibit high toxicity and are not indicated for children, for pregnant or breastfeeding women or for chronically ill patients. Amphotericin B (AmpB) is a second-line drug, and although it has been increasingly used to treat visceral leishmaniasis (VL), its clinical use has been hampered due to its high toxicity. This review focuses on the development and in vivo usage of new delivery systems for AmpB that aim to decrease its toxicity without altering its therapeutic efficacy. These new formulations, when adjusted with regard to their production costs, may be considered new drug delivery systems that promise to improve the treatment of leishmaniasis, by reducing the side effects and the number of doses while permitting a satisfactory cost-benefit ratio.

The aim of this study was to synthesize and characterize the biodegradable intraocular implants based on poly (D,L-lactide-co-glycolide) (PLGA 75:25) with Cyclosporine-A (CyA) and to evaluate their in vitro drug delivery profile. Thermal analysis was conducted by using Thermogravimetry (TG) and Differential Scanning Calorimetry (DSC). Phase analysis and crystallinity of the polymer-CyA samples were assessed through X ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR). Finally, microstructure and morphology of the systems were investigated by Scanning Electron Microscopy (SEM). The results showed that CyA was successfully incorporated into PLGA network with drug loading of approximately 31.6%. Also, based on FTIR and thermal analyses (TGA/DSC) no significant physical-chemical interaction was detected at the micro-nanoscale level between polymer/drug. SEM micrographs have indicated a uniform drug distribution in PLGA matrix. XRD patterns have showed that the incorporated semi-crystalline structure of CyA has not significantly altered the polymeric mainly amorphous network. In addition, the results have confirmed the chemical and biological drug stability, the drug distribution into the polymeric matrix and the possibility of cyclosporine prolonged delivery system profile.