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

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

Pamplona

Simposio; 19th International Symposium on MICROENCAPSULATION; 2013

International Microencapsulation Society

Cyclodextrins (CDs) are cyclic oligosaccharides derived from starch. 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 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 b-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. 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. Therefore, the aim of this work was focused in the synthesis of a b-CD-citrate derivative to improve the solubility and dissolution rate of ABZ and the design of new oral delivery systems to improve the drug efficacy.