Researchers at Hebrew University (Jerusalem, Israel) and Harvard University (Boston, MA, USA) developed the nanocomplex based on naringenin, a flavonoid aglycone responsible for the bitter taste in grapefruit, which is poorly absorbed by the body when in its natural form. To overcome this problem, the solubility of naringenin was enhanced by complexation with Hydroxypropoyl-β-cyclodextrin (HPβCD), which increased the solubility of naringenin by over 400-fold, and its transport across a model of the gut epithelium by 11-fold. As an added benefit, when the molecule is turned into cyclodextrin, it becomes sweet; thus, naringenin is no longer bitter.

The researchers then tested the product on rats, and found that the nanocomplex increased naringenin plasma concentrations values by 7.4-fold. Moreover, when the complex was administered just prior to a meal, it decreased very low-density lipoprotein (VLDL) levels by 42% and increased the rate of glucose clearance by 64%, compared to naringenin alone. Histology and blood chemistry analysis indicated this route of administration was not associated with damage to the intestine, kidney, or liver. According to the researchers, these results suggest that the complexation of naringenin with HPβCD is a viable option for the oral delivery of naringenin as a therapeutic entity with applications in the treatment of dyslipidemia, diabetes, and hepatitis c virus (HCV) infection. The study was published in the April 6, 2011, issue of PLoS One.

"The complex is special in that it is taken just before a meal as a preventative measure," said lead author Yaakov Nahmias, PhD, of the Hebrew University School of Engineering and Computer Science. "In comparison, existing medications are given only after chronic development of abnormal lipid levels in the blood."

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