Antiparasitic microparticles: a promising strategy for the treatment of trichinellosis.

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

Cordoba

Congreso; Ricifa 2014; 2014

Ricifa

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 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 (ABZ) is a benzimidazole carbamate widely used for the treatment of helminthic diseases. ABZ has an unfavorable bioavailability after oral administration, leading to a variable oral absorption. The main objective of this study was to design and prepare ABZ microparticles. This can be achieved by controlled precipitation or crystallization and evaporation. The antipasasitic drug was 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. The scanning electronic microscopy images confirmed the uniform size (5-20μm) and spherical shape. Powder X-ray diffraction patterns for ABZ exhibited several reflection peaks revealing its crystalline nature. The diffractograms of the microparticles displayed amorphous patterns, indicating that the drug underwent a transition from a crystalline to an amorphous state. The best results obtained by the dissolution profiles of ABZ loaded in the microparticles exhibited the 100% drug release after 30 minutes of the running assay while ABZ (pure drug) exhibited a 2.8%. Additionally, the microparticles were in vitro evaluated employed infective larvae of Trichinella spiralis. Two different concentration of ABZ (0.5 and 1 μm/mL) were employed during 72 h. Cellulose derivatives microparticles were the most effective systems reducing the percentage of infective larvae. These results remarkably demonstrate the improvement of the dissolution rate of ABZ, loaded in the microparticles. Keywords: albendazole, microparticles, controlled precipitation.