High-dose coenzyme Q10-loaded oleogels for oral therapeutic supplementation

EHRENHAUS N.; MARTINEFSKI M.,; LUCANGIOLI S.; ROJAS A.; TRIPODI V.

INTERNATIONAL JOURNAL OF PHARMACEUTICS

ELSEVIER SCIENCE BV

Lugar: Amsterdam; Año: 2019 vol. 556 p. 9 - 20

0378-5173

Coenzyme Q10 (CoQ10) is a mitochondrial respiratory cofactor and potent endogenous antioxidant. In CoQ10-deficient patients, early treatment with high-oral doses (5?50 mg/kg/day) can limit the progression of renaldisease and the onset of neurological manifestations. Crystalline CoQ10 is lipophilic, water-insoluble, and poorlyabsorbed in the gut. Here, CoQ10 showed low bulk density, another important disadvantage in solid oral formulations.Thus, we propose the use of oleogels to maintain dissolved a high-dose of CoQ10 in medium-chaintriglyceride (MCT) oil, using ethylcellulose (EC) for gelling, and a surfactant (sorbitan monostearate ?SMS- orlecithin). ?True gels? were only obtained with the surfactant presence. Thermoreversible oleogels with 1 g ofdissolved CoQ10 per 5 g-disk were successfully developed with proved stability and solubility for 12 months(25.0 °C). SMS was better than lecithin as a surfactant because it allowed lower syneresis, higher CoQ10 retentionfor 12 months, and notably higher oxidative-stability of the MCT-oil, best immobilized by its true gelnetwork. Plastic deformation without fracture was determined under compression, emulating the soft deformationbehavior inside the mouth. SMS-oleogels allowed loading a maximal solubilized CoQ10 dose withmaximal stability, and may be easier to swallow by CoQ10-deficient patients who suffer from secondary dysphagia