A nanocrystals-based formulation improves the pharmacokinetic performance and therapeutic response of albendazole in dogs

JAVIER PAREDES,; NICOLÁS LITTERIO,; ALICIA DIB; DANIEL ALBERTO ALLEMANDI, ; SERGIO SÁNCHEZ BRUNI, . ; CARLOS LANUSSE; SANTIAGO DANIEL PALMA

Buenos Aires

Congreso; Reunión conjunta de Sociedades de Biociencias; 2017

SAFE

Introduction. Albendazole (ABZ) is broad spectrum antiparasitic agent with a poor aqueous solubility which often leads to erratic bioavailability and therapeutic failures. For poorly soluble drugs, a diminution in particle size could lead to enhanced bioavailability and clinical efficacy. Nanocrystals (NC) are defined as nanoparticles composed of practically 100% drug, being generally stabilized by surfactants or polymeric steric agents and with a mean particle size is below 1 µm. Here we aimed to assess the pharmacokinetic performance and therapeutic response (anthelmintic efficacy) of an ABZ nano-sized formulation in dogs. Methodology. In the pharmacokinetic study, ABZ self-dispersible nanocrystals (SDNCS) and a control formulation were administered orally to healthy dogs using a cross over design (n=6). The concentrations of the sulphoxide metabolite in plasma were determined by High Performance Liquid Cromatography. For the anthelmintic efficacy trial, SDNCS and a commercially available formulation of ABZ were given to naturally parasitized dogs at 3 dose levels: 6.25, 12.5 and 25 mg/kg. The number of Ancylostoma caninum eggs in the feces up to 30 days was determined using the McMaster technique. Key findings. The area under the curve, Tmax and Cmax for the SDNCS were improved significantly compared to the control (p