Inclusion complexes and self-assembled cyclodextrin aggregates for increasing the solubility of benzimidazoles

Albendazole and fenbendazole are imidazole derivatives that exhibit broad spectrum activity against parasites, but the low solubility of these drugs considerably reduces their effectiveness. Complexation of albendazole and fenbendazole with cyclodextrins (β-cyclodextrin and hydroxypropyl-β-cyclodextrin) in both water and an aqueous solution of polyvinylpyrrolidone (PVP-k30) was studied to determine if it could increase the solubility and dissolution rate of the drugs. In an aqueous solution, β-cyclodextrin increased the solubility of albendazole from 0.4188 to ∼93.47 µg mL-1 (223×), and of fenbendazole from 0.1054 to 45.56 µg mL-1 (432×); hydroxypropyl-β-cyclodextrin, on the other hand, increased solubility to ∼443.06 µg mL-1 (1058×) for albendazole and ∼159.36 μg mL-1 (1512×) for fenbendazole. The combination of hydroxypropyl-β-cyclodextrin and polyvinylpyrrolidone enabled a solubility increase of 1412× (∼591.22 µg mL-1 ) for albendazole and 1373× (∼144.66 µg mL-1 ) for fenbendazole. The dissolution rate of the drugs was significantly increased in binary and ternary systems, with hydroxypropyl-β-cyclodextrin proving to be more effective. The presence of the water-soluble PVP-k30 increased the dissolution rate and amorphization of the complexes. Analysis of the changes in displacement and the profile of the cyclodextrin bands in the 1 H NMR spectra revealed a molecular interaction and pointed to an effective complexation in the drug/cyclodextrin systems. Monomeric forms and nanoclusters of cyclodextrins were observed in the drug/cyclodextrin systems, suggesting that the increase in solubility of the drugs in the presence of cyclodextrins should not be attributed only to the formation of inclusion complexes, but also to the formation of cyclodextrin aggregates

A small proportion of Zebu genetic background in crossbred calves may not be enough to improve resistance against natural bovine Babesia spp. infections

2019/22675-6) and the Institute of Animal Science (APTA-SAA). AMG Ibelli is recipient of a productivity fellowship from CNPq. Publisher Copyright: © 2024 Elsevier B.V.The main objective of cattle breeders in tropical and subtropical regions is to acquire animals with taurine-productive traits adapted to the broad weather range of these regions. However, one of the main challenges on using taurine genetics in these areas is the high susceptibility of these animals to tick-borne diseases. Consequently, the present study evaluated from 10 November 2021–19 April 2022, the over 13 assessments, the Babesia bovis and Babesia bigemina DNA loads and the IgG anti-B. bovis and anti-B. bigemina levels in Angus (n = 17, 100% Taurine) and Ultrablack (n = 14, ∼82% taurine and 18% Zebu) calves. Data were analyzed using a multivariate mixed model with repeated measures of the same animal including the fixed effects of evaluation, genetic group, sex, Babesia spp., and their interactions. The repeatability values were estimated from the (co)variances matrix and expressed for each species. The correlations between the DNA loads (CNlog) and IgG titers (S/P) values for the two species were also estimated using the same model. Regarding the specific IgG antibody titers for both Babesia spp., no significant differences were observed between the two genetic groups. However, for B. bovis and B. bigemina DNA loads, Ultrablack calves presented significantly higher values than Angus calves. Under the conditions evaluated in this study, our findings suggest that the low percentage of Zebu genetic in the Ultrablack breed was insufficient to improve resistance against babesiosis. Further studies must demonstrate if the low percentages of Zebu genetics in Taurine breeds can modify the susceptibility to babesiosis infections.publishersversionpublishe

Atividade anti-helmíntica in vitro e in vivo de compostos fitoquímicos para o controle de nematóides gastrointestinais de ovinos

Os óleos essenciais de Mentha piperita, Cymbopogon martinii e Cymbopogon schoenanthus foram avaliados in vitro sobre tricostrongilídeos de ovinos por meio dos testes de eclodibilidade, do desenvolvimento, da inibição da alimentação e da eliminação da cutícula larvar. Utilizou-se cromatografia gasosa acoplada ao espetrômetro de massas para identificação dos constituintes dos óleos. Os óleos apresentaram elevada atividade anti-helmíntica avaliada pela comparação de CL50, sendo o C. schoenanthus o mais ativo. Os mesmos óleos foram testados em ratos Wistar infectados artificialmente com o parasita intestinal Strongyloides venezuelensis nas dosagens de 1,5 mL/kg e 2,3 mL/kg cada um. Os óleos não apresentaram efeito anti-helmíntico significativo medido pela contagem de ovos nas fezes e contagem parasitária quando comparado ao albendazol. C. schoenanthus foi o óleo essencial que apresentou melhor atividade anti-parasitária in vitro sobre trichostrongilídeos de ovinos, portanto, sua atividade foi testada in vivo em cordeiros artificialmente infectados com Haemonchus contortus nas dosagens de 0,2 e 0,4 mL/kg. A redução parasitária (por meio de de contagem de ovos nas fezes e contagem parasitária) e a toxicidade (por meio de de perfis bioquímicos renal e hepático) foram avaliadas. O óleo essencial de C. schoenanthus não foi tóxico nas dosagens utilizadas e embora não tenha propiciado redução significativa no grau de infecção parasitária, proporcionou maior valor de hematócrito e proteína sérica total. Além desse efeito, causou discreta redução no desenvolvimento de larvas nas fezes. Uma metodologia aperfeiçoada de teste in vitro utilizando o nematoide de vida livre Caenorhabditis elegans, mantidos em cultura líquida estéril, também foi descrito, assim como os testes de sensibilidade destes nematoides aos principais solventes utilizados na preparação dos extratos de plantasMentha piperita, Cymbopogon martinii and Cymbopogon schoenanthus essential oils were evaluated in vitro against sheep trichostrongylids through eclodibility assay, larval development assay, larval feeding inhibition assay and larval exsheathment assay. Oils were analysed by chromatography coupled to mass spectrometry. The oils presented high anthelmintic activity by comparison of LC50, being C .schoenanthus is the most active. The oils were tested withWistar rats artificially infected with Strongyloides venezuelensis at 1.5 mL/kg and 2.3 mL/kg. The essential oils didn’t present a significant anthelmintic effect measured by fecal egg count and worm burden when compared to albendazole. The oil of C. schoenanthus had the best anthelmintic activity against sheep trichostrongylids and were evaluated in vivo in lambs artificially infected with Haemonchus contortus at doses of 0.2 and 0.4 mL/kg. Its activity were evaluated by fecal egg count and worm burden and the toxicity evaluated by kidney and liver profile. C. schoenanthus did not show toxic effects at the doses tested and although without significant reduction in parasite infection, it led to a higher packed cell volume and total serum protein and small reduction in larval development in feces. An improved methodology of in vitro test employing the free living nematode Caenorhabditis elegans raised in sterile liquid medium was described as well the toxicity to the major solvents used in preparation of plant extractsCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES

Elaboração de queijo maturado por mofo obtido de coagulação mista (Lática-Coalho), com leite de cabra congelado e coalhada congelada

A caprinocultura leiteira apresenta um caráter sazonal. O congelamento do leite “in natura” e o congelamento da coalhada dessorada são algumas das formas de se contornar a falta de leite de cabra em alguns períodos do ano. O objetivo deste trabalho foi verificar a possibilidade de se fabricar um queijo obtido de coalhada mista, de massa mole, maturada pelo fungo Penicillium candidum, similar ao queijo Bougon . Foi utilizado leite congelado pelo processo lento (através de freezer comum) e pelo processo rápido (através de nitrogênio líquido). Também foi utilizado massa da coalhada dessorada e congelada respectivamente pelos processo lento e rápido. Verificou-se que os queijos resultantes do congelamento do leite e resultantes do congelamento da coalhada pelos processos lento e rápido não diferiram dos queijos controle nos aspectos de rendimento, características físico-químicas, composição química, índice de extensão de maturação, índice de profundidade de maturação e aspectos microbianos. A qualidade microbiana do leite utilizado e dos queijos produzidos foi muito boa. No decorrer da cura do queijo similar ao Bougon houve evolução do pH, que foi se tornando mais alcalino com o desenvolvimento da maturação. O tratamento congelamento lento da coalhada demonstrou comportamento inferior aos demais principalmente nos itens textura na análise sensorial e pela menor pontuação no teste de aceitação do produto. Os queijos provenientes do congelamento do leite pelo processo rápido e do congelamento rápido da coalhada não diferiram dos queijos controle (sem congelamento) na análise sensorial.The goat herd presents a sazonal characteristic. The freezing of the raw milk and the freezing of the curd are some of the ways to round the milk lacking in some periods of the year. The aim of this work was to verify the possibility to make a cheese made from mixed curd (lactic-curdle), soft, ripened by a Penicillium candidum mould, similar to the Bougon cheese. Frozen milk by slow process (through the domestic freezer) and by fast process (through the liquid nitrogen) was used. The frozen curd without whey through the slow and fast process was used either. It was verified that the resulting cheeses from the frozen milk and from the frozen curd by slow and fast process didn´t differ from the control cheeses for the yield, chemicophysical characteristics, chemical composition, extention ripened rate, depth ripened rate and in microbiological aspects. The microbiological quality of the milk and cheeses was very good. During the ripening of the cheese similar to the Bougon occurred the evolution of the pH, that turned more alkaline with the development of ripening of the cheese. The freezing curd by slow process demonstrated inferior quality when it was compared with other tratments in the texture on the sensorial analisis and from the small pontuation in the accept test of product. The cheeses provided from the frozen milk by slow process and from the frozen curd by fast process didn´t differ from the control cheeses (without freezing) in the sensorial analisis

Aspectos físico-químicos e microbianos do queijo maturado por mofo obtido da coagulação mista com leite de cabra congelado e coalhada congelada

Milk goats are indicated as an economic alternative for small farmers and cheese making could improve their profits. Goat's milk has a seasonal production characteristic and shows periods of abundance and others of scarcity. The use of frozen milk or frozen curd to make cheese can be used to solve the problem. The aim of this work was to evaluate the preparation of cheese made from mixed curd and ripened by Penicillium candidum mould using slow frozen milk (in a domestic freezer) or fast frozen milk (by liquid nitrogen). The slow frozen curd and fast frozen curd without whey were used. It was observed that the cheese from the slow and fast frozen milk and from the slow and fast frozen curd did not differ from the control cheese for the yield, chemicophysical characteristics, chemical composition, extention ripened rate, depth ripened rate and microbiological aspects, even when it was expressed as a dry matter content of cheeses

Infestação artificial com carrapato rhipicephalus (bophilus) microplus e consumo de alimentos e condição corporal em bovinos resistentes e susceptíveis

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Effectiveness of Areca catechu Linn against Haemonchus contortus in vitro egg hatch assay

Areca catechu Linn belongs to Palm Arecaceaes family, popularly known as Betel palm, originated from tropical countries of Oceania and East Africa. Popularly known for its wide pharmacological activity, Areca catechu has also antibacterial, antihelmintic, antioxidant and detoxifying activity. In its composition is found carbohydrates, fibers, fats, flavonoids, tannins, alkaloids and minerals, and its nut is the main product with medicinal use. In this study, we tested the action of A. catechu L. on in vitro hatchability of eggs of sheep gastrointestinal nematode Haemonchus contortus. The seed was broken and dried at 37°C, crushed in 2 mm size and its contents were extracted with a solution of acetone:water (70:30), filtered, rotoevaporated and freeze dried. For the main solution it was used 300 mg of plant extract, mixed at 2850 µl of distilled water and DMSO (150 µl), that was diluted in decreasing concentrations (50 mg/ml, 25 mg/mL, 12.5 mg/ml, 6.25 mg/ml, 3.12 mg/ml, 1.56 mg/ml and 0.78 mg/ml). A hundred eggs of H. contortus were added to different concentrations of A. catechu extract in 48-well plate, and incubated for 24 hours at 27°C to evaluate their effectiveness. Data were analyzed with SAS Probit (SAS Inst., Inc., Cary, NC) estimating the LC50 and the independent variables (dose). The results showed that at doses of 7.45 mg/mL can inhibit 50% of the hatchability of eggs of H. contortus (Figure 1)

Infestação artificial com carrapato rhipicephalus (bophilus) microplus e consumo de alimentos e condição corporal em bovinos resistentes e susceptíveis

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Artificial infestation with Rhipicephalus (boophilus) microplus tick and food intake and corporal condition in resistant and susceptible cattle

The cattle-tick Rhipicephalus (Boophilus) microplus is one of the worst pests of domestic livestock due to damages caused to the health. Artificial infestation is still needed in many scientific papers, and, depending on the quantity of infesting larvae and the cattle susceptibility, it can be fatal due to the deleterious effects that this parasite causes to the cattle health. The food intake greatly decreases during massive larval infestations. The objective of this work was to study the impact of an artificial infestation on feed intake and animal body condition. Four susceptible cattle (Holstein Black and White) were infested with 10,000 larvae and 20,000 larvae infested six resistant cattle (Nellore). Animals were an average of 7 months-old. Two weeks before the infestation and during the parasitic life cycle (three weeks after the infestation), each animal was placed in individual pens with water and food ad libitum. It was offered 2 kg of commercial concentrate (minimum 16% crude protein, CP) and 5 kg of Cynodon dactylon cv. Tifton (13.19% CP) a day. The refusal was weighed for 3 consecutive days at the time of: one week before infestation, and one, two and three weeks post-infestation in order to calculate food intake average before and during the life cycle of the parasite. Animals were assessed for body condition (1 - skinny to 5 - obese) weekly. The experimental design was a non-probability sample restricted to 10 animals. Food intake data was analyzed using general linear models (SPSS® statistical package -version 12.0) with breed and day as independent variable. Both effects were significant (P<0.01). Food intake (FI) increased in both breeds, higher in Holstein (5.962 ± 0.154 kg food day-1 versus 5.392 ± 0.126 kg food day-1, for Nellore). The regression of body condition score (BC) was calculated as a function of FI. The body condition from animals of both breeds increased as the food intake was enlarged over the three weeks of parasitic cycle (BC = 3.104 + 0.154 FI – 1.083 Breed, R2 = 0.675). Therefore, it was concluded that artificial infestations with 10,000 larvae in susceptible cattle and 20,000 in resistant cattle did not harmed food intake or body condition. So, we can recommend this amount of larvae for resistant and susceptible cattle in experiments which require tick’s artificial infestation

Potencial anti-helmíntico de formulações contendo óleos essenciais em nematóides gastrintestinais de ovinos

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