Abstract. Celecoxib (Cx) shows high efficacy in the treatment of osteoarthritis and rheumatoid arthritis as a result of its high specificity for COX-2, without gastrolesivity or interference with platelet function at therapeutic concentrations. Besides of anti-inflammatory effects, Cx also has a potential role for oral cancer chemoprevention. For these conditions, oral administration in long-term treatment is a concern due to its systemic side effects. However, local application at the site of injury (e.g., buccal inflammation conditions or chemoprevention of oral cancer) is a promising way to reduce its toxicity. In this study, the in vitro characterization of mucoadhesive chitosan (CHT) gels associated to Azone® was assessed to explore the potential buccal mucosal administration of Cx in this tissue. Rheological properties of gels were analyzed by a rheometer with cone-plate geometry. In vitro Cx release and permeability studies used artificial membranes and pig cheek mucosa, respectively. Mucoadhesion were measured with a universal test machine. CHT gels (3.0%) containing 2.0% or 3.0% Az showed more appropriate characteristics compared to the others: pH values, rheology, higher amount of Cx retained in the mucosa, and minimal permeation through mucosa, besides the highest mucoadhesion values, ideal for buccal application. Moreover, the flux (J) and amounts of drug released decreased with increased CHT and Az concentrations. CHT gels (3.0%) associated with 2.0% or 3.0% Az may be considered potential delivery systems for buccal administration of Cx.

This paper aims to gather and discuss important information about nonylphenol, such as physical chemistry properties, toxicity and analytical methods in various matrices. As a degradation product of ethoxylated alkylphenols, nonylphenol presents a higher degree of reactivity than its precursor. Due to its harmful effects on the environment, use and production of nonylphenol has been banned in European Union countries, alongside their precursors. The guide on quality of drinking water (USEPA) recommends a maximum concentration of 28 µg L -1 for fresh water. In Brazil, there is no clear legislation containing values of maximum concentration of nonylphenol. Due to this lack of regulation, a continuous monitoring is necessary of this pollutant in environmental samples. This paper aims to encourage further studies on nonylphenol, seen as a critical environmental pollutant. For proper monitoring is necessary to have reliable analytical methods and easy to perform in routine analysis.

Extracts and essential oils from plants are important natural sources of pesticides. These compounds are considered an alternative to control ectoparasites of veterinary importance. Schinus molle, an endemic species of Brazil, produces a high level of essential oil and several other compounds. The aim of this work was to determinate the chemical composition of extracts and essential oils of S. molle and further to evaluate the activity against eggs and adults of Ctenocephalides felis felis, a predominant flea that infests dogs and cats in Brazil. In an in vitro assay, the non-polar (n-hexane) extract showed 100% efficacy (800 µg cm(-2); LD50 = 524·80 µg cm(-2)) at 24 and 48 h. Its major compound was lupenone (50·25%). Essential oils from fruits and leaves were evaluated, and had 100% efficacy against adult fleas at 800 µg cm(-2) (LD50 = 353·95 µg cm(-2)) and at 50 µg cm(-2) (LD50 = 12·02 µg cm(-2)), respectively. On the other hand, the essential oil from fruits and leaves was not active against flea eggs. This is the first study that reports the insecticidal effects of essential oils and extracts obtained from Schinus molle against Ctenocephalides felis felis.

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The aim of the present study was to evaluate the insecticidal effect of the cassia, thyme and oregano volatile oils against the immature and adult flea's stages. For this purpose, the tested samples were chemically characterized by GC-FID and GC-MS. The mortality of larvae and adult fleas, eggs, and pupae of Ctenocephalides felis felis was performed through in vitro tests at different concentration levels. Inhibition of development and residual efficacy were also determined. The chemical characterization of the cassia, thyme, and oregano volatile oils presented cinnamaldehyde (91%), thymol (44.7%), and carvacrol (76.2%), respectively, as major constituents. In general, the samples showed insecticidal activity for both immature and adult flea's stages. The best LC 50 values for adults were obtained by oregano volatile oils (33.5 and 21.8 μg•cm −2 , respectively, 24 and 48 h). Cassia volatile oils showed the best results against larvae (17.2 and 10.3 μg•cm −2 , respectively, 24 and 48 h), eggs (3 μg.cm −2), and pupae (34.6 μg•cm −2), as well as the lowest value for inhibition of development (2.3 μg•cm −2). The oregano and thyme volatile oils showed residual efficacy greater than 80% for 6 days while cassia showed this result for 4 days. The results demonstrated the potential of volatile oils for flea control in all stages of the life cycle, with emphasis on cassia. The residual effects of the volatile oils are promising for the development of new and environmentally friendly phyto-pesticides for veterinary uses.

With the increasing number of pets in home the human-animal relationship is increasingly close and care about control disease growing. Ivermectin (IVM) is frequently used because its proven safety. IVM is recommended for the treatment of demodectic scabies and prevention of heartworm in dogs, but informally is extremely used to control of Ctenocephalides felis felis and Rhipicephalus sanguineus. The aim of this study is evaluate the use of IVM in dogs, by the oral route at 0.6μg/kg dose, against experimental infection of these parasites using the construction of the plasma concentration curve and efficacy study. A IVM quantification method in canine plasma using HPLC-FL was developed and validated based on RE n°899/03 ANVISA. The samples collected during the efficacy test was analyzed by this validated method and prove C of 350ng/mL at 4h (t) and AUC of 8411ng/h/mL. Spite of formulation have shown good absorption, the highest efficiency values found for Rhipcephalus sanguineus and Ctenocephalides felis felis were very low, 35% and 67% respectively, demonstrating this not be the most appropriate treatment for the control of these parasites.

Increased human-pet interactions have led to concerns related to the prevention and treatment of ectoparasite infestations. Fipronil (FIP) is a widely used ectoparasiticide in veterinary medicine available for topical administration; however, its use may cause damage to the owners and the environment. The aim of the study was to develop immediate-release tablets of FIP, as well as to determine its pharmacokinetic properties after oral administration in beagle dogs. The prepared FIP tablets were evaluated for precompression (angle of repose, speed flow, and Carr's index) and post-compression (weight variation, friability, thickness, hardness, disintegration time, and dissolution rate) parameters. Orally administered FIP at a dose of 2 mg/kg was rapidly absorbed with C máx of 3.13 ± 1.39 μg/mL at 1.83 ± 0.40 h post treatment (P.T.) and metabolized with 1.27 ± 1.04 μg/mL at 2.33 ± 0.82 h P.T. for fipronil sulfone (SULF) (the primary metabolite). The elimination of FIP and SULF occurred slowly and had maintained quantifiable plasma levels in the blood for up to 28 days P.T. The goal of the study is aligned with the concept of One Health, which aims to collaboratively achieve the best health for people, animals, and the environment. Therefore, the use of FIP tablets for the control of ectoparasites in dogs may be a safer alternative for owners and the environment.

Fipronil is a phenylpyrazole class insecticide. It is widely used as an insecticide in agriculture and in the control of ectoparasites in veterinary medicine. The application of fipronil in an injectable form (subcutaneously) becomes an innovation, since there is no commercially available preparation containing fipronil herein. The present study aimed at fipronil usage, applied subcutaneously in cattle, to control Rhipicephalus microplus. The assessing criteria used in the research have been the construction of the plasma concentration curve and efficacy studies. A method using High Performance Liquid Chromatograph with ultraviolet detection was developed for determination of fipronil in bovine plasma samples, providing a fast and simple process with good reproducibility and low limit of quantification. The validation of the analytical method showed linearity, selectivity, precision, accuracy, sensitivity and stability, thus proving it as suitable for routine analysis. This method showed to be an important investigative tool in the analysis of fipronil plasma concentration in cattle. Fipronil administered via subcutaneous in bovine reached the systemic circulation (Cmax=378.06±137.44 ng/mL), was quickly absorbed (t(max)=10±0.87 h), and its elimination occurred slowly (t(1/2)=12 days), while maintaining quantifiable blood plasma levels (23.79±12.16 ng/mL) for up to 21 days after the treatment with a 1 mg/kg dosage. The in vivo efficacy tests proved that fipronil applied subcutaneously in a single dose of 1 mg/kg in cattle exhibited a mean efficacy of 82.41% against R. microplus. The potential of subcutaneous injection as an alternative treatment route in cattle encourage the development of an injectable formulation of fipronil.