Physicochemical and pharmacokinetic characterization of water-soluble Coenzyme Q 10 formulations

• Published in: International journal of pharmaceutics Vol. 363; no. 1; pp. 112 - 117
• Main Authors: Hatanaka, Junya, Kimura, Yoshihiro, Lai-Fu, Zhogn, Onoue, Satomi, Yamada, Shizuo
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 2008
• Subjects: Bioavailability; Coenzyme Q 10; DSC; Emulsion; PXRD; Emulsion; DSC; Bioavailability; Coenzyme Q 10; PXRD
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2008.07.019

Coenzyme Q 10 (CoQ 10) has been used as a drug for chronic heart failure. Furthermore, various biological effects of CoQ 10 have also been applied for food supplements and cosmetics. However, CoQ 10 was found to be poorly soluble in water, so that its bioavailability was low and variable depending on food intake. In the present investigation, a novel liquid (nano-emulsion, NE) and water-soluble powder formulations, including cyclodextrin–Q10 complex (CoQ 10–CD) and dry-emulsion (DE), were prepared. The physicochemical properties of each formulation were characterized by dynamic light scattering (DLS), scanning electron microscopy (SEM), powder X-ray diffractometry (PXRD), and differential scanning calorimetry (DSC). In all powder formulations prepared, CoQ 10 existed mainly as an amorphous form as determined by PXRD and DSC, and each powder formulation exhibited high solubility and dispersibility in water resulting in the formation of a nano-sized emulsion (NE; 60 nm) and micron sized particles (DEs and CoQ 10–CD; 0.77–2.4 μm). The pharmacokinetic study of each dosage form, in comparison to a CoQ 10 crystal suspension, was also carried out in rats after a single oral dose. Although similar kinetic values were seen with T max of 1.5 and 1.7 h, respectively, for NE and crystalline CoQ 10, NE exhibited ca 1.7-fold higher AUC and C max than the crystalline CoQ 10.