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Development of a safe pediatric liquisolid self-nanoemulsifying system of triclabendazole for the treatment of fascioliasis.
Int J Pharm
October 2022
College of Pharmacy and Health Sciences, St. John's University, Queens, NY, United States. Electronic address:
Fascioliasis, a common parasitic infection observed in the pediatric patient population, is a leading cause of concern in countries with poor/unhealthy water resources. To treat this condition first line agent such as triclabendazole (TBZ) has been the choice therapy. However, there is a major hurdle in exploiting TBZ.
View Article and Find Full Text PDFRepurposing of the Fasciolicide Triclabendazole to Treat Infections Caused by spp. and Vancomycin-Resistant Enterococci.
Microorganisms
August 2021
Australian Centre for Antimicrobial Resistance Ecology, Roseworthy Campus, School of Animal and Veterinary Sciences, The University of Adelaide, Roseworthy, SA 5371, Australia.
One approach to combat the increasing incidence of multidrug-resistant (MDR) bacterial pathogens involves repurposing existing compounds with known safety and development pathways as new antibacterial classes with potentially novel mechanisms of action. Here, triclabendazole (TCBZ), a drug originally developed to treat (liver fluke) in sheep and cattle, and later in humans, was evaluated as an antibacterial alone or in combination with sub-inhibitory concentrations of polymyxin B (PMB) against clinical isolates and reference strains of key Gram-positive and Gram-negative bacteria. We show for the first time that in vitro, TCBZ selectively kills methicillin-sensitive and methicillin-resistant and at a minimum inhibitory concentration (MIC) range of 2-4 µg/mL, and vancomycin-resistant enterococci at a MIC range of 4-8 µg/mL.
View Article and Find Full Text PDFImproving the Dissolution of Triclabendazole from Stable Crystalline Solid Dispersions Formulated for Oral Delivery.
AAPS PharmSciTech
December 2019
Instituto de Química de Rosario, Consejo Nacional de Investigaciones Científicas y Tecnológicas, Suipacha 531, 2000, Rosario, Argentina.
Triclabendazole belongs to the class II/IV of the Biopharmaceuticals Classification System, and its low aqueous solubility represents a major drawback during the development of effective dosage forms. Therefore, the goal of this study was to elucidate whether polymeric solid dispersions would represent a suitable approach to overcome such disadvantage. Due to the lack of information on triclabendazole release, four different dissolution media were evaluated to analyze drug dissolution rate.
View Article and Find Full Text PDFPharmacologic interaction between oxfendazole and triclabendazole: In vitro biotransformation and systemic exposure in sheep.
Exp Parasitol
September 2019
Laboratorio de Farmacología, Centro de Investigación Veterinarias de Tandil (CIVETAN. CONICET-CIC-UNCPBA), Facultad de Ciencias Veterinarias, Universidad Nacional del Centro de la Provincia de Buenos Aires (FCV-UNCPBA), Tandil, Argentina. Electronic address:
The aim of the current work was to evaluate a potential pharmacokinetic interaction between the flukicide triclabendazole (TCBZ) and the broad-spectrum benzimidazole (BZD) anthelmintic oxfendazole (OFZ) in sheep. To this end, both an in vitro assay in microsomal fractions and an in vivo trial in lambs parasitized with Haemonchus contortus resistant to OFZ and its reduced derivative fenbendazole (FBZ) were carried out. Sheep microsomal fractions were incubated together with OFZ, FBZ, TCBZ, or a combination of either FBZ and TCBZ or OFZ and TCBZ.
View Article and Find Full Text PDFTotal determination of triclabendazole and its metabolites in bovine tissues using liquid chromatography-tandem mass spectrometry.
J Chromatogr B Analyt Technol Biomed Life Sci
March 2019
Division of Foods, National Institute of Health Sciences, 3-25-6, Tonomachi, Kawasaki-ku, Kawasaki-shi, Kanagawa 210-9501, Japan.
A reliable LC-MS/MS analytical method for the determination of residual triclabendazole and its principal metabolites (triclabendazole sulfoxide, triclabendazole sulfone and keto-triclabendazole) in bovine tissues was developed, in which triclabendazole and its metabolites are oxidized to keto-triclabendazole as a marker residue. The method involves sample digestion with hot sodium hydroxide, thus releasing the bound residues of various triclabendazole metabolites in bovine tissues. The target compounds are extracted from the digest mixture with ethyl acetate, defatted by liquid-liquid partitioning using n-hexane and acetonitrile, then oxidized with hydrogen peroxide in a mixture of ethanol and acetic acid.
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