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KMID : 0606920100180010099
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Biomolecules & Therapeutics
2010 Volume.18 No. 1 p.99 ~ p.105
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Relative Bioavailability of Coenzyme Q10 in Emulsion and Liposome Formulations
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Choi Chee-Ho
Kim Si-Hun
Shanmugam Srinivasan
Rengarajan Baskaran
Park Jeong-Sook
Yong Chul-Soon
Choi Han-Gon
Yoo Bong-Kyu
Han Kun
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Abstract
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The purpose of this study was to evaluate relative bioavailability of the coenzyme Q10 (CoQ10) in emulsion and three liposome formulations after a single oral administration (60 mg/kg) into rats. Emulsion formulation of CoQ10 was prepared by conventional method using Phospholipon 85G as an emulsifier, and three liposome formulations (neutral, anionic, and cationic) of CoQ10 were prepared by traditional lipid film hydration technique using Phospholipon 85G, cholesterol, and charge carrier lipids (1,2-dioleoyl-3-trimethylammonium- propane chloride salt for cationic liposome and 1,2-dimyristoyl-sn-glycero-3-phosphate monosodium salt for anionic liposome). Mean particle size of all CoQ10-loaded liposome was less than a micron, and size distribution of the liposome population was homogeneous. Bioavailability of CoQ10 in emulsion was 1.5 to 2.6-fold greater than liposome formulations in terms of AUC0-24 h. Tmax was 3 h when administered as emulsion while it was greater than 6 h in liposome formulations. Notably, it was approximately 8 h in cationic liposome. Cmax was highest in emulsion and was significantly decreased when administered as liposome. Charged liposome showed even lower Cmax than neutral liposome, especially in cationic liposome. In conclusion, therefore, it is suggested that clinicians and patients consider bioavailability issue a primary concern when choosing a CoQ10 product, especially when very high plasma level is required such as in the treatment of heart failure and Parkinson’s disease.
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KEYWORD
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Coenzyme Q10, Liposome, Bioavailability, Pharmacokinetic parameters, Photostability
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