Enhancing Drug Bioavailability: Curcumin and Its Derivatives as Modulators of UGT2B17 and Intestinal Enzymes

Unmet Need: Inhibitor drugs of UGT2B17 that can be used for boosting bioavailability of its substrates.

Since curcumin is a safe bioactive compound with potential health benefits, however, it has poor bioavailability, inventors have explored the use of curcumin as a bioavailability enhancer of other nutrients or drugs. They have developed an approach by developing a natural product that can be used as an inhibitor of UGT2B17. Curcumin is a safe herbal compound and is approved for human use.

The Technology: Tested the concomitant used of drugs and curcumin to increase drug bioavailability

The technology involves the use of curcumin or its derivatives to inhibit UGT2B17, an enzyme active in the intestine. Inventors conducted a series of in vitro experiments using curcumin as a potential UGT2B17 inhibitor. Inventors tested the intestine metabolism of UGT2B17 substrates, testosterone and diclofenac. Their model suggested that inhibition can increase diclofenac bioavailability between 2-8 fold and decrease its variable pharmacokinetic profile to within 2-fold.

Applications: