714f Inulin Surfactants for Colon-Specific Drug Delivery

Julio C. Arboleda, G. Toriz, S. Beltran, V. Zuņiga, and E. Delgado. Departamento de Madera Celulosa y Papel, Universidad de Guadalajara, Km 15,5 Carretera Guadalajara-Nogales, Las Agujas, Zapopan, Mexico

Inulin is a storage polysaccharide found in plants such as onion, garlic, artichoke, chicory, and tequila agave. It is interesting for biomedical applications because it is metabolized only in the human colon by enzimatic means, which allows the design of site-specific drug delivery systems. Such systems are needed for oral administration of drugs that tend to be unstable, either by being absorbed in the gastrointestinal tract or by leading to side effects. Drugs used for colorectal cancer, ulcerative colitis and inflammatory bowel disease belong to this class.

Derivatives from inulin, with emulsifying behavior, can be produced by reacting hydrophobic moieties with the abundant hydroxyl groups in the polysacharide. It is possible to produce emulsions of different hydrophobic drugs with these surfactants and then, to obtain capsules by crosslinking and drying of the formed micelles.

These capsules are distinctively structured in such a way as to confine the drug in the interior and exposing the inulin moiety to the exterior. The exterior would just be enzymatically metabolized in the colon, triggering the aperture of the capsules and the subsequent release of the drug.

In order to emulsify a drug it is necessary to know its required HLB. Therefore, the synthesis of inulin derivatives had to be optimized as a function of the required HLB, which could be done by changing the molar relationship between inulin and the hydrofobic moiety during the synthesis of the surfactant.

In this work the preparation of surfactants with stearic acid/stearyl chloride and agave inulin is shown. HLB for the emulsification of 5-ASA was determined and the synthesis of agave surfactants was carried out. Drug emulsification, crosslinking and drying of micelles as well as the characterization of the obtained microcapsules are presented.