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Adding vitamin C to drugs may help treat brain disorders

14 January, 2002

Drugs used to treat brain disorders appear to enter the brain more easily when a vitamin C molecule is attached, according to researchers in Italy. The discovery could lead to safer and more effective drugs that target the brain, they say.

The study is to appear in the Journal of Medicinal Chemistry.

"We’ve opened a door for a promising new way to improve delivery of drugs into the brain using a natural nutrient, ascorbic acid [vitamin C]" says Stefano Manfredini, lead investigator in the study and a professor of pharmaceutical chemistry at the University of Ferrara.

Some drugs that have difficulty entering the brain could cross more easily when attached to a vitamin C molecule, while some that cannot enter the brain could enter for the first time, he says. Potential applications include drugs for central nervous system diseases, viral infections (including AIDS), brain lesions, and neurological conditions including Alzheimer’s, Parkinson’s and epilepsy, Manfredini says.

He calls the results "exciting", but cautions that the data are very preliminary. So far, animal tests of at least one of the vitamin C modified drugs appear promising, but no human tests have been conducted. The new design approach will not enhance the effectiveness of all drugs, while those that do work could take several years to reach the consumer market, the researcher predicts.

One of the major problems in the treatment of brain diseases is the difficulty of distributing drugs to the central nervous system. This is due to a natural barrier, the blood brain barrier, which selectively regulates the movement of chemicals across the brain.

Researchers have known for some time that adding new components to drugs may improve their ability to cross this barrier. For example, glucose and amino acid units have allowed improved penetration into the blood brain barrier for some drugs, according to researchers.

Additional animal studies of vitamin C modified drugs are anticipated, Manfredini and his associates say.