Antiparasitic microparticles: a promising strategy for the treatment of trichinellosis

PRIOTTI, J.; LEONARDI D.; LAMAS, M. C.

Congreso; III Reunión Internacional de Ciencias Farmacéuticas RICIFA.; 2014

Bulk microstructured materials have been the subject of intense investigations over the last decades due to the unusual properties and their promising applications. Microsuspensions are microsized dispersion systems stabilized by surfactants and/or polymers. A suspension platform (microcrystals, microparticles) is an efficient drug delivery system for water-insoluble drugs because of the increase of the saturation solubility and the surface area available for dissolution. Albendazole and mebendazole are benzimidazole carbamates widely used for the treatment of trichinellosis. They are poorly water soluble and highly lipophilic drugs, belongs to the Class II in the Biopharmaceutics Classification System exhibiting unfavorable bioavailability after oral administration, leading to a variable oral absorption. The main objective of this study was to design and prepare albendazole and mebendazole microparticles. This can be achieved by controlled precipitation or crystallization and evaporation. The benzimidazoles were dissolved in acetic acid:ethanol solution, and then precipitated in a polymeric solution (cellulose derivatives and non ionic surfactants). Finally, the microsuspensions were sprayed using a Büchi Mini Spray Dryer B-290. Different techniques were used to thoroughly investigate the structural characteristics and morphology of the particles such as differential scanning calorimetry, infrared spectroscopy, scanning electronic microscopy, X-ray diffraction, solubility and dissolution rate profiles. The systems profiles showed faster dissolution rates than the raw drugs. Additionally, the microparticles showed good antiparasitic activity against infective larvae of Trichinella spiralis.