Bioavailability of coenzyme Q(10) loaded in an oleogel formulation for oral therapy: Comparison with a commercial-grade solid formulation

摘要

Coenzyme Q(10) (CoQ(10)) is essential in mitochondrial bioenergetics and is a potent endogenous antioxidant. Low CoQ(10) levels are associated with neurodegenerative, metabolic, muscular and cardiovascular disorders. Early treatment with high doses (5-50 mg/kg/day) demonstrated to limit the onset and progression of neuropathology. Recently, we developed an oleogel matrix able to support a high dose of oil-dissolved CoQ(10), easy to swallow by CoQ(10)-deficient patients who suffer from secondary dysphagia. In the present study, we evaluated the bioavailability of oleogel-dissolved CoQ(10) and plasma antioxidant status in healthy adults in single-dose and repeated-dose studies. The single-dose study demonstrated that, in terms of CoQ(10) bioavailability, 1 g CoQ(10)/5g oleogel-disk was equivalent to the solid form (1 g CoQ(10)/three 00-size-capsules), whereas the repeated-dose study (14-days-administration) demonstrated a significantly higher increase in plasma CoQ(10) when administered through the oleogel, which could be compatible with the levels necessary to achieve an adequate therapeutic response. Also, a trend to a higher plasma apparent half-life (greater than24 h) was observed for the oleogelloaded-CoQ(10). In conclusion, the oleogel matrix does not compromise the oil-dissolved CoQ(10) bioavailability and can prevent the non-adherence to this vital supplementation in patients with high CoQ(10) requirements. No significant variation in the plasma antioxidant status (vitamins A, E and C, glutathione and TBARs) was observed.