RESUMEN
Molecules from natural sources, such as essential oils, have shown activity against parasites in vitro, but have not yet been explored extensively in vivo. Anethole and carvone (10% each), encapsulated with 80% of a solid matrix, referred to as EO (encapsulated oils), were tested in vivo in 2 experiments. In Experiment 1: Lambs were artificially infected with multidrug resistant Haemonchus contortus, or left uninfected, and treated (or not) with 50â¯mg/kg bw (body weight) of EO in a controlled environment. Thirty-two male lambs were kept in individual cages for a period of 45 days, after which animals were evaluated for parasitological, hematological, toxicological, and nutritional parameters. After 45 days of treatment, EO at 50â¯mg/kg bw provided a significant (Pâ¯≤â¯0.05) reduction in fecal egg count (FEC). Although FEC was reduced, animals from both treatments had similar counts of total adult worms. The low FEC was caused probably by a significant reduction (Pâ¯≤â¯0.05) in both male worm size and female fecundity. Dry matter intake of uninfected controls was significantly (Pâ¯≤â¯0.05) reduced, although no toxicity was observed in treated animals. Thus, in Experiment 2, conducted for five months we used an EO dose of 20â¯mg/kg bw. Thirty-four weaned lambs, free of parasites, were divided in two groups and kept in collective pens. One group received EO at 20â¯mg/kg bw mixed with concentrate for 5 months and the other was kept as a control group (CTL). Parasitological and hematological parameters as well as body weight were evaluated. In the first 2.5 months, CTL and EO groups were confined, and both presented similar clinical parameters. Then, animals were allotted to graze on contaminated pastures to acquire natural infection for the next 2.5 months. The infection was patent after 25 days and both groups had similar decreases in weight gain, increases in FEC, and decreases in blood parameters. Coprocultures from CTL and EO groups established that parasite population was 90% Haemonchus sp. We concluded that the technology of encapsulation is safe and practical to deliver to lambs at the farm level and anethole and carvone at 50â¯mg/kg bw caused a significant decrease in FEC and, consequently, in pasture contamination by free living stages of H. contortus. However, EO at 20â¯mg/kg bw was not effective to prevent or treat sheep naturally-infected with gastrointestinal nematodes.
Asunto(s)
Anisoles/uso terapéutico , Hemoncosis/veterinaria , Monoterpenos/uso terapéutico , Enfermedades de las Ovejas/tratamiento farmacológico , Enfermedades de las Ovejas/parasitología , Abomaso/parasitología , Derivados de Alilbenceno , Animales , Anisoles/administración & dosificación , Anisoles/química , Aspartato Aminotransferasas/sangre , Cápsulas , Creatinina/sangre , Monoterpenos Ciclohexánicos , Resistencia a Múltiples Medicamentos , Sinergismo Farmacológico , Ingestión de Alimentos , Recuento de Eritrocitos/veterinaria , Heces/parasitología , Femenino , Fertilidad , Hemoncosis/tratamiento farmacológico , Hemoncosis/parasitología , Haemonchus/efectos de los fármacos , Haemonchus/crecimiento & desarrollo , Haemonchus/fisiología , Masculino , Monoterpenos/administración & dosificación , Monoterpenos/química , Recuento de Huevos de Parásitos/veterinaria , Distribución Aleatoria , Ovinos , Urea/sangre , Aumento de Peso , gamma-Glutamiltransferasa/sangreRESUMEN
Albendazole (ABZ), a benzimidazole widely used to control gastrointestinal parasites, is poorly soluble in water, resulting in variable and incomplete bioavailability. This has favored the appearance ABZ-resistant nematodes and, consequently, an increase in its clinical ineffectiveness. Among the pharmaceutical techniques developed to increase drug efficacy, cyclodextrins (CDs) and other polymers have been extensively used with water-insoluble pharmaceutical drugs to increase their solubility and availability. Our objective was to prepare ABZ formulations, including ß-cyclodextrin (ßCD) or hydroxypropyl-ß-cyclodextrin (HPßCD), associated or not to the water-soluble polymer polyvinylpyrrolidone (PVP). These formulations had their solubility and anthelmintic effect both evaluated in vitro. Also, their anthelmintic efficacy was evaluated in lambs naturally infected with gastrointestinal nematodes (GIN) through the fecal egg count (FEC) reduction test. In vitro, the complex ABZ/HPßCD had higher solubility than ABZ/ßCD. The addition of PVP to the complexes increased solubility and dissolution rates more effectively for ABZ/HPßCD than for ABZ/ßCD. In vivo, 48 lambs naturally infected with GIN were divided into six experimental groups: control, ABZ, ABZ/ßCD, ABZ/ßCD-PVP, ABZ/HPßCD, and ABZ/HPßCD-PVP. Each treated animal received 10 mg/kg of body weight (based on the ABZ dose) for three consecutive days. After 10 days of the last administered dose, treatment efficacy was calculated. The efficacy values were as follows: ABZ (70.33%), ABZ/ßCD (85.33%), ABZ/ßCD-PVP (82.86%), ABZ/HPßCD (78.37%), and ABZ/HPßCD-PVP (43.79%). In vitro, ABZ/HPßCD and ABZ/HPßCD-PVP had high solubility and dissolution rates. In vivo, although the efficacies of ABZ/ßCD, ABZ/ßCD-PVP, and ABZ/HPßCD increased slightly when compared to pure ABZ, this increase was not significant (P > 0.05).
Asunto(s)
Albendazol/farmacocinética , Antiparasitarios/farmacocinética , Ciclodextrinas/farmacocinética , Nanopartículas/química , Povidona/farmacocinética , 2-Hidroxipropil-beta-Ciclodextrina/química , 2-Hidroxipropil-beta-Ciclodextrina/farmacocinética , Albendazol/química , Animales , Antihelmínticos/química , Antihelmínticos/farmacocinética , Antiparasitarios/química , Disponibilidad Biológica , Ciclodextrinas/química , Composición de Medicamentos , Parasitosis Intestinales/tratamiento farmacológico , Parasitosis Intestinales/veterinaria , Masculino , Nematodos , Infecciones por Nematodos/tratamiento farmacológico , Infecciones por Nematodos/veterinaria , Povidona/química , Ovinos , Enfermedades de las Ovejas/tratamiento farmacológico , Enfermedades de las Ovejas/parasitología , Solubilidad , beta-Ciclodextrinas/química , beta-Ciclodextrinas/farmacocinéticaRESUMEN
Haemonchus contortus is the most important nematode in small ruminant systems, and has developed tolerance to all commercial anthelmintics in several countries. In vitro (egg hatch assay) and in vivo tests were performed with a multidrug strain of Haemonchus contortus using Terminalia catappa leaf, fruit pulp, and seed extracts (in vitro), or pulp and seed powder in lambs experimentally infected with H. contortus. Crude extracts from leaves, fruit pulp and seeds obtained with 70% acetone were lyophilized until used. In vitro, the extracts had LC50=2.48µg/mL (seeds), LC50=4.62µg/mL (pulp), and LC50=20µg/mL (leaves). In vitro, seed and pulp extracts had LC50 similar to Thiabendazole (LC50=1.31µg/mL). Condensed tannins were more concentrated in pulp extract (183.92g of leucocyanidin/kg dry matter) than in either leaf (4.6g) or seed (35.13g) extracts. Phytochemical tests established that all extracts contained alkaloids, flavonoids, saponins, phenols, and terpenoids. Based on these results, in vivo tests were performed to evaluate the anthelmintic activity of T. catappa whole fruit (pulp+seed) powder. Male Santa Ines lambs were artificially infected with multidrug-resistant H. contortus and divided, according to similar fecal egg count (FEC) and weight, into two groups: Control (infected/untreated) and treated (infected/treated with whole fruit powder). Whole fruit powder was mixed with concentrate and provided at 2g/kg of body weight (BW) for five days. After treatment, parasitological analysis (FEC and egg hatch assay), renal profile (urea and creatinine), liver profile (aspartate aminotransferase) and BW were determined. In vitro (based on LC50), seed/pulp extracts had ovicidal effect similar to Thiabendazole but whole fruit powder had no anthelmintic effect on adult nematodes in the abomasum. We discuss the plausible causes of the lack of in vivo activity.
Asunto(s)
Hemoncosis/tratamiento farmacológico , Hemoncosis/veterinaria , Extractos Vegetales/uso terapéutico , Enfermedades de las Ovejas/parasitología , Terminalia/química , Animales , Antihelmínticos/uso terapéutico , Frutas , Haemonchus/efectos de los fármacos , Masculino , Recuento de Huevos de Parásitos/veterinaria , Fitoterapia , Extractos Vegetales/química , Hojas de la Planta/química , Semillas/química , Ovinos , Enfermedades de las Ovejas/tratamiento farmacológicoRESUMEN
OBJECTIVE: The purpose of this study was to investigate correlations between masseter muscle activity and cephalometric measures in Angle's class III dental malocclusion under the clinical rest position. METHODS: Eight volunteers, both sex, age 7-12, were submitted to an electromyographic analysis of the masseter muscle, subdivided in the upper, medium and lower regions, and to a cephalometric analysis of 15 angle and linear measurements. After normalization, the data was subjected to a statistical, non-parametric Spearman correlation test, by means of the SPSS 12.0 program. RESULTS: Statistically significant correlations were observed between the clinical rest condition before and after the execution of exercises (a serie of mandibular movements), and the cephalometric measurements angle SN GoGn, angle SNA, angle SNB, angle SND, upper incisive. NA angle, upper incisive-NA distance, lower incisive. NB angle, lower incisive-NB distance and angle IMPA, and the different regions of the masseter muscle. CONCLUSIONS: The significant statistical correlation found between the cephalometric analysis and the function of the masseter muscle indicate a strong influence of the musculature under a clinical rest condition over the cranial-facial development in the Angle's class III dental malocclusion. There is a selective activity of the different regions of the masseter muscle under the clinical rest condition in the Angle's class III dental malocclusion. There is a demand for research to complement these findings in other classes of dental malocclusion.