Tequila Ingredient Potential Drug-Carrier to Target Colon Diseases

Newswise — Compounds derived from the blue agave, a fruit used to make tequila, shows promise in early laboratory studies as a natural, more effective way to deliver drugs to the colon than conventional drug-carriers, according to chemists at the University of Guadalajara in Mexico. The development could lead to improved treatments for ulcerative colitis, irritable bowel syndrome, cancer, Crohn's disease and other colon diseases, they say.

Drug delivery to the colon is an ongoing challenge to physicians. Many drugs are destroyed by stomach acids before they've had a chance to reach the intestine, where they usually are absorbed. Researchers have tried to circumvent this problem by inserting the drugs into carrier molecules that resist breakdown in the stomach but have had difficulty finding a suitable carrier compound.

The tequila compounds, a class of polysaccharides known as fructans, were developed by the scientists in Mexico into tiny microspheres that are capable of carrying existing drugs that are used to treat colon diseases. Because the compounds resist destruction in the stomach, they could allow more of the drugs to reach the colon intact and improve their effectiveness, the researchers say. Their study was presented today at the 233rd national meeting of the American Chemical Society. "This study shows that the agave fruit is good for more than just tequila. It also has medicinal value," says study leader Guillermo Toriz, Ph.D., an assistant professor at the university. "Agave fructan is the ideal natural carrier of drugs for the colon."

Researchers have known for some time that fructans, which are polymers of fructose, are resistant to acid degradation and theorized that they might be a useful drug delivery vehicle. But only a few plant sources, such as agave, contain fructans in large amounts. The agave fruit is 80 percent fructans by weight when ripe, the researchers say.

Toriz and his associates extracted fructans from the blue agave, the base ingredient of tequila. They chemically modified the fructan compound to allow drugs to be encapsulated, making the drugs resistant to degradation in the digestive system.

The researchers then prepared microspheres of the compounds and filled them with ibuprofen as a model of drug delivery to the colon. In laboratory tests, the ibuprofen-filled microspheres were exposed to hydrochloric acid for an hour and appeared physically intact upon subsequent microscopic examination, the scientists say.

Topiz and his research group currently are working on improving the durability of the fructans and plan animal studies in the future. If further studies show promise, human studies of the agave microspheres are anticipated. Funding for the study was provided by the Mexican National Science and Technology Council.

The American Chemical Society — the world's largest scientific society — is a nonprofit organization chartered by the U.S. Congress and a global leader in providing access to chemistry-related research through its multiple databases, peer-reviewed journals and scientific conferences. Its main offices are in Washington, D.C., and Columbus, Ohio.

The paper on this research, CELL 152, will be presented at 5:00 p.m., Tuesday, March 27, at the McCormick Place Lakeside, Room E267, Level 2, during the symposium, "Functionalization of Renewable Materials: Lignin and Other Natural Compounds."

Guillermo Toriz, Ph.D., is an assistant professor in the Wood Cellulose and Paper Research Department at the University of Guadalajara in Guadalajara, Mexico.

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The paper on this research, CELL 152, will be presented at 5:00 PM, Tuesday, 27 March 2007, during the symposium, "Functionalization of Renewable Materials."

CELL 152Esterified fructans from tequila agave plant to produce microspheres for drug delivery to the colon

Program Selection: Division of Cellulose & Renewable MaterialsTopic Selection: Functionalization of Renewable Materials: Lignin and Other Natural Compounds

Abstract At 5-7 years of age the plant Tequila Agave (Tequilana Weber, Var. Azul) is ripe and has a fructan content of about 80 wt %. The tasty Mexican alcoholic beverage tequila is made by fermentation of the fructans extracted from this plant. On the other hand, since fructans are not degraded in the human digestive tract they could be used for drug delivery to the colon. In this contribution we will discuss the acetylation and succynation of native agave fructans and the preparation of microspheres by the coacervation method. The use of ibuprofen as a model drug to investigate the releasing properties of the microspheres will be shown. The extent of acetylation and/or succynation (determined by NMR, FTIR, and acid-base and potentiometric titrations) and its effect on the morphology/solubility of the microspheres will be discussed as well as the release of ibuprofen in model systems.