Nutrition Research, 26(10), 503-508, 2006.

Enhancement of oral bioavailability of coenzyme Q10 by complexation with γ-cyclodextrin in healthy adults

Nutrition Research, 26(10), 503-508, 2006.

Enhancement of oral bioavailability of coenzyme Q10 by complexation with γ-cyclodextrin in healthy adults

Keiji Terao, Daisuke Nakata, Hiroshi Fukumi, Gerhard Schmid, Hidetoshi Arima, Fumitoshi Hirayama and Kaneto Uekama

The objective of this study was to determine the effect of molecular encapsulation of coenzyme Q₁₀ (CoQ₁₀) by complexation with γ-cyclodextrin (γ-CD) (CoQ₁₀-γ-CD) compared with a mixture of CoQ₁₀ with microcrystalline cellulose (CoQ₁₀-MCC) on absorption and bioavailability of CoQ₁₀ in supplement form in healthy adults. Twenty-two volunteers received a single dose of a 150-mg capsule containing 30 mg CoQ₁₀ under fasting conditions in an open-label, crossover design with a 2-week washout period. Blood was collected before dosing and after dosing periodically over 48 hours. Plasma levels of CoQ₁₀ were determined by high-performance liquid chromatography using an electrochemical detector and an online reduction system. After 6 and 8 hours of dosing there was a significant increase in mean CoQ₁₀ plasma levels of subjects after a single oral administration of the CoQ₁₀-γ-CD capsule compared with those with the CoQ₁₀-MCC capsule. In addition, the mean plasma levels at 24 and 48 hours tended to be higher after CoQ₁₀-γ-CD administration in comparison with CoQ₁₀-MCC administration. The area under the plasma CoQ₁₀ concentration curve and the maximum plasma concentration (C_max) values as well as their corresponding log-transformed values, log area under the plasma CoQ₁₀ concentration curve, and log C_max for the CoQ₁₀-γ-CD formulation were significantly higher than those for the CoQ₁₀-MCC formulation. These results indicate that the oral absorption and bioavailability of CoQ₁₀ in healthy adult volunteers could be significantly enhanced by complexation with γ-CD, suggesting the potential use of γ-CD as formulation aid for orally administered CoQ_{10Keiji Terao, Daisuke Nakata, Hiroshi Fukumi, Gerhard Schmid, Hidetoshi Arima, Fumitoshi Hirayama and Kaneto Uekama}

The objective of this study was to determine the effect of molecular encapsulation of coenzyme Q₁₀ (CoQ₁₀) by complexation with γ-cyclodextrin (γ-CD) (CoQ₁₀-γ-CD) compared with a mixture of CoQ₁₀ with microcrystalline cellulose (CoQ₁₀-MCC) on absorption and bioavailability of CoQ₁₀ in supplement form in healthy adults. Twenty-two volunteers received a single dose of a 150-mg capsule containing 30 mg CoQ₁₀ under fasting conditions in an open-label, crossover design with a 2-week washout period. Blood was collected before dosing and after dosing periodically over 48 hours. Plasma levels of CoQ₁₀ were determined by high-performance liquid chromatography using an electrochemical detector and an online reduction system. After 6 and 8 hours of dosing there was a significant increase in mean CoQ₁₀ plasma levels of subjects after a single oral administration of the CoQ₁₀-γ-CD capsule compared with those with the CoQ₁₀-MCC capsule. In addition, the mean plasma levels at 24 and 48 hours tended to be higher after CoQ₁₀-γ-CD administration in comparison with CoQ₁₀-MCC administration. The area under the plasma CoQ₁₀ concentration curve and the maximum plasma concentration (C_max) values as well as their corresponding log-transformed values, log area under the plasma CoQ₁₀ concentration curve, and log C_max for the CoQ₁₀-γ-CD formulation were significantly higher than those for the CoQ₁₀-MCC formulation. These results indicate that the oral absorption and bioavailability of CoQ₁₀ in healthy adult volunteers could be significantly enhanced by complexation with γ-CD, suggesting the potential use of γ-CD as formulation aid for orally administered CoQ₁₀