A high-dose coenzyme Q10-emulgel for chronic oral therapy of deficient patients with secondary dysphagia

Abstract

Coenzyme Q₁₀ (CoQ₁₀) is the major endogenously fat-soluble antioxidant synthesized in the mitochondrion inner membrane as the electron carrier in the respiratory chain. In CoQ₁₀-deficient patients, early high-oral doses (5–50 mg/kg/day) can constrain renal dysfunction and neurological signs. CoQ₁₀, a typical class IV drug, with low bulk density, was dissolved at high-dose (1 g) in the oil phase (20:80 O/W) of a novel emulgel of small serving size (25 g) for its chronic administration in deficient patients with secondary dysphagia, as an alternative to maintain therapy adherence. The novelty is that CoQ₁₀ remained dissolved in 5 g of oil phase (MCT and coconut oils) per 25 g of alginate-emulgel. This was physically stable for 9 months at 25 °C as a “weak gel” type network, with high zeta potential (‒80 mV) being then the oil droplet size (5.0 μm) successfully maintained. The emulgel showed pseudoplastic behavior and four times lower viscosities than those of a contrast fluid used for swallow studies in dysphagic patients. Chemical stability of CoQ₁₀ was 100 % for 12 months. Emulgel administration (25 g/day) for 2 weeks increased CoQ₁₀ plasma concentration in 3.9 times. The number of doses for high CoQ₁₀ therapy can then be reduced, without swallowing discomfort.