Emulsification Using Highly Hydrophilic Surfactants Improves the Absorption of Orally Administered Coenzyme Q10

Abstract

Coenzyme Q10 (CoQ10) is an essential component in the electron-transport systems of mitochondria and bacteria and is often used as a supplementary treatment for some diseases. We previously reported that the bioavailability of CoQ10 powder was less than 10%. In this study, we investigated various preparations to improve the intestinal absorption of CoQ10 with focus on the effect of emulsification. We prepared a suspension and some emulsions with four types of surfactants and investigated the plasma concentration profile after oral administration to rats. The absorption of CoQ10 was improved by an emulsion formulation although there was little absorption of CoQ10 when a suspension was administered. However, little CoQ10 was absorbed in the bile duct-ligated group even when the emulsion formulation was administered (about 50% of the control group). Bile and emulsion formulation are essential for absorption of CoQ10. When the preparations containing Tween20 (polysorbate (20) sorbitan monolaurate) and Tween80 (polyoxyethylene (20) sorbitan monooleate) were administered, plasma concentrations of CoQ10 were higher than those obtained with preparations containing Tween65 (polyoxyethylene (20) sorbitan tristearate) and Span20 (sorbitan monolaurate). Tween20 and Tween80 have higher hydrophile-lipophile balance (HLB) values than those Tween65 and Span20. Our study suggests that highly lipophilic compounds like CoQ10 would diffuse the unstirred water layer and would easily access the intestinal apical membrane by an emulsion containing a surfactant with a high HLB value. Attention must be given to CoQ10 supplementation for patients whose bile is not excreted to the intestine such as patients with cholestasis.Key words coenzyme Q10; absorption; bile; emulsion; intestine; lutein Preventive medicine and anti-aging medicine have received much attention recently due to increases in the proportion of elderly people in the population and patients with lifestyle diseases such as hypertension, dislipidemia and diabetes. Oxidative stress is involved in the onset of lifestyle diseases, 1,2) and various antioxidant supplements and antioxidant-fortified functional foods have recently become available. Many epidemiological studies have shown relationships between consumption of polyphenol or carotenoid-rich foods and prevention of these lifestyle diseases. 3,4) Coenzyme Q (CoQ) has a benzoquinone ring linked to a polyisoprenyl chain of 9 or 10 units in mammalian species. CoQ10, also known as ubiquinone, is a ubiquitous component vital to a number of activities related to energy metabolism. CoQ10 also functions in its reduced form as an antioxidant, protecting biological membranes and serum low density lipoprotein (LDL) from lipid peroxidation. 5,6) The use of CoQ10 as a therapeutic cardiovascular agent was based on its fundamental role in mitochondrial function and cellular bioenergetics. 7,8) Many studies have also indicated a beneficial antioxidant effect of CoQ10 as supplementation, and CoQ10 has received much attention due to its an...

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