The influence on the spray drying process in the formulation of albendazole : beta-cyclodextrin systems

GARCIA, A.; LEONARDI, D.; LAMAS, M.C.

Rosario

Congreso; II Reunión Internacional de Ciencias Farmacéuticas; 2012

Cyclodextrins (CDs) are natural or semisynthetic cyclic oligosaccharides with a central cavity having the ability to host a wide variety of hydrophobic compounds. The main pharmaceutical application of the design of CDs systems is to increase the apparent solubility of the included drugs. By far beta-Cyclodextrin (beta-CD) is the most widely used CD, consisting of seven glucopyranose units linked by alfa-(1,4) bonds. The mayor disadvantage is the exceptional low aqueous solubility and crystalline characteristics of beta-CD (18,5 mg/mL at 25 ºC) limiting the improved solubility of poorly soluble compounds as a result of the solid combination. Many chemically modified beta-CD have been synthesized, among which Methyl-beta-Cyclodextrin (M-b-CD) and 2-Hydroxypropyl-beta-Cyclodextrin (HP-b-CD) being excellent solubilizers due to the fact that their amorphous characteristics. Albendazole (ABZ) is a broad spectrum anthelmintic drug that exhibits very low aqueous solubility, and as a consequence has an erratic bioavailability. The ability of cyclodextrins to solubilize drugs probably contributes to lower response variability. The aim of this work was to increase the apparent solubility and dissolution rate of ABZ formulation of inclusion complexes. The methodology selected for the preparation of ABZ:CDs complexes was spray drying methodology. The spray drying methodology was an efficient method to prepare ABZ-CDs inclusion complexes in amorphous state, highlighting the physicochemical advantages related to the improved drug release rate and the solubility.