INVESTIGADORES
MARTINEFSKI Manuela Romina
artículos
Título:
High-dose coenzyme Q10-loaded oleogels for oral therapeutic supplementation
Autor/es:
MASOTTA, NATALIA EHRENHAUS; MARTINEFSKI, MANUELA R.; LUCANGIOLI, SILVIA; ROJAS, ANA M.; TRIPODI, VALERIA P.
Revista:
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Editorial:
ELSEVIER SCIENCE BV
Referencias:
Año: 2019 vol. 556 p. 9 - 20
ISSN:
0378-5173
Resumen:
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 renal disease and the onset of neurological manifestations. Crystalline CoQ10 is lipophilic, water-insoluble, and poorly absorbed 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-chain triglyceride (MCT) oil, using ethylcellulose (EC) for gelling, and a surfactant (sorbitan monostearate ?SMS- or lecithin). ?True gels? were only obtained with the surfactant presence. Thermoreversible oleogels with 1 g of dissolved 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 retention for 12 months, and notably higher oxidative-stability of the MCT-oil, best immobilized by its true gel network. Plastic deformation without fracture was determined under compression, emulating the soft deformation behavior inside the mouth. SMS-oleogels allowed loading a maximal solubilized CoQ10 dose with maximal stability, and may be easier to swallow by CoQ10-deficient patients who suffer from secondary dysphagia.