Formulation and physicochemical characterization of Albendazole-cyclodextrin citrate complexes obtained by spray drying

GARCÍA, A.; LEONARDI, D.; SALOMON, C.; SALAZAR, M.; LAMAS, M. C.

Pamplona

Simposio; 19th International Symposium on Microencapsulation; 2013

International Microencapsulation Society

Cyclodextrins (CDs) are cyclic oligosaccharides derived from starch containing six (α CD), seven (βCD), eight (γCD) or more (α-1,4)-linked α-D-glucopyranose units. The three major cyclodextrins are crystalline and due to the chair conformation of the glucopyranose units, the CDs take the shape of a truncated cone. The secondary hydroxyl groups (C2 and C3) are located on the wider edge of the ring, and the primary hydroxyl groups (C6) on the other edge. The apolar cavity provides a hydrophobic matrix, able to form inclusion complexes with a wide variety of hydrophobic guest molecules. The main interest in CDs could be found in the pharmaceutical field to increase the apparent solubility of poorly water soluble compounds, the dissolution rate, the chemical and physical stability, and, as consequence, their bioavailability. Due to the fact -CD, has attained pharmaceutical relevance, and this natural CD has an anomalously low solubility in water, a chemical modification may produce an increase in solubility. The random substitution, produce very heterogeneous and non cristallizable products.1 CDs derivatives presenting acidic groups in their structure may interact strongly with basic drugs generating extremely stable inclusion complexes. Albendazole (ABZ), a basic compound, very poorly soluble in water (1µg/mL) was assigned to Class II by the BCS. This property limited the absorption and produced unpredictable therapeutic responses in some parasitic infections. The ABZ:beta-CD-citrate complex allow to increase significantly the ABZ solubility and the dissolution rate values in comparison to the pure drug and the complex ABZ:beta-CD.