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Enrofloxacin belongs to the fluoroquinolone class of antibiotics. It is commonly used in a variety of reptile species due to its wide spectrum of efficacy, partly due to its formation of an active metabolite ciprofloxacin. Enrofloxacin shows wide disposition variability among all species resulting in large differences in the plasma concentrations of both enrofloxacin and ciprofloxacin. The aim of this study was to evaluate the pharmacokinetics of enrofloxacin and ciprofloxacin after a single intracoelomic injection of 10 mg/kg of enrofloxacin in 9 tortoises (Testudo hermanni). Blood samples were collected at 0, 0.5, 2, 4, 10, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240 and 264 h and analyzed using a validated high performance liquid chromatography (HPLC) florescence method. Plasma concentrations of enrofloxacin were quantifiable in all subjects for up to 240 h, while ciprofloxacin was detected in all subjects up to 120 h. The Cmax (s) of enrofloxacin and ciprofloxacin were 8614 ± 1116 ηg/mL obtained at 2.19 h and 605 ± 43 ηg/mL obtained at 4.23 h, respectively. The values of Cmax/MIC ratio and AUC0-24/MIC ratio of enrofloxacin with a MIC value of 0.5 μg/mL were 17.23 and 132.78, respectively. In conclusion, an administration of 10 mg/kg of enrofloxacin via the intracoelomic route in Hermann's tortoises produced optimal pharmacodynamic parameters. [ABSTRACT FROM AUTHOR]

Treatments for inflammation and pain are important consideration in human and veterinary medicine. The classical drugs for treatments of inflammation and pain act by inhibition of cyclooxygenase and lypoxygenase pathways. However, there is still a need to develop new veterinary drugs and trials to apply human drugs to the veterinary field in order to increase the veterinary drug armamentarium. However, it is pivotal to experimentally test human drugs and therapies in veterinary species before veterinary clinical applications. The soluble epoxide hydrolase inhibitors (sEHIs), are novel active ingredients shown to have a number of beneficial effects. This has been especially demonstrated in many animal models in relation to inflammation and pain. The present review reports the state of the art of soluble epoxide hydrolase inhibitors and suggests their potential use in veterinary medicine. [ABSTRACT FROM AUTHOR]

Background : Berberine is a natural alkaloid with hypoglycemic properties. However, its therapeutic use is limited by a very low oral bioavailability. Here we developed a new oral formulation of berberine based on Sucrosomial ® technology and tested its effect on insulin resistance. Methods : Sucrosomial ® berberine was first tested in vitro in the hepatoma cell line Huh7 to assess its effect on proteins involved in glucose homeostasis and insulin resistance. The pharmacokinetics and efficacy on insulin resistance were then studied in C57BL/6 mice fed with standard (SD) and high-fat diet (HFD) for 16 weeks and treated daily during the last 8 weeks with oral gavage of Sucrosomial ® berberine or berberine. Results : Sucrosomial ® berberine did not affect Huh7 cell viability at concentrations up to 40 µM. Incubation of Huh7 with 20 µM of Sucrosomial ® and control berberine induced glucokinase (GK) and the phosphorylation of 5'-adenosine monophosphate (AMP)-activated protein kinase (AMPK), both known targets for the control of insulin resistance. In vivo, we observed an 8-fold higher plasma concentration after 3 weeks of oral administration of 50 mg/kg/day of Sucrosomial ® formulation compared to berberine. HFD, compared to SD, induced insulin resistance in mice as determined by oral glucose tolerance test (OGTT). The treatment with a 6.25 mg/kg/daily dose of Sucrosomial ® berberine significantly reduced the area under the curve (AUC) of OGTT (73,103 ± 8645 vs. 58,830 ± 5597 mg/dL × min), while control berberine produced the same effects at 50 mg/Kg/day (51518 ± 1984 mg/dL × min). Under these conditions, the two formulations resulted in similar berberine plasma concentration in mice. Nevertheless, a different tissue distribution of metabolites was observed with a significant accumulation of reduced, demethylated and glucuronide berberine in the brain after the oral administration of the Sucrosomial ® form. Glucuronide berberine plasma concentration was higher with Sucrosomial ® berberine compared to normal berberine. Finally, we observed similar increases of AMPK phosphorylation in the liver in response to the treatment with Sucrosomial ® berberine and berberine. Conclusions : The Sucrosomial ® formulation is an innovative and effective technology to improve berberine gastrointestinal (GI) absorption with proven in vitro and in vivo activity on insulin resistance.

In this work, we characterized conjugated linolenic acids (e.g., punicic acid) as the major components of the hydrophilic fraction (80% aqueous methanol extract) from pomegranate (Punica granatum L.) seed oil (PSO) and evaluated their anti-inflammatory potential on some human colon (HT29 and HCT116), liver (HepG2 and Huh7), breast (MCF-7 and MDA-MB-231) and prostate (DU145) cancer lines. Our results demonstrated that punicic acid and its congeners induce a significant decrease of cell viability for two breast cell lines with a related increase of the cell cycle G0/G1 phase respect to untreated cells. Moreover, the evaluation of a great panel of cytokines expressed by MCF-7 and MDA-MB-231 cells showed that the levels of VEGF and nine pro-inflammatory cytokines (IL-2, IL-6, IL-12, IL-17, IP-10, MIP-1α, MIP-1β, MCP-1 and TNF-α) decreased in a dose dependent way with increasing amounts of the hydrophilic extracts of PSO, supporting the evidence of an anti-inflammatory effect. Taken together, the data herein suggest a potential synergistic cytotoxic, anti-inflammatory and anti-oxidant role of the polar compounds from PSO.