Masotta, N.E.; Martinefski, M.R.; Lucangioli, S.; Rojas, A.M.; Tripodi, V.P. "High-dose coenzyme Q10-loaded oleogels for oral therapeutic supplementation" (2019) International Journal of Pharmaceutics. 556:9-20
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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. © 2018 Elsevier B.V.


Documento: Artículo
Título:High-dose coenzyme Q10-loaded oleogels for oral therapeutic supplementation
Autor:Masotta, N.E.; Martinefski, M.R.; Lucangioli, S.; Rojas, A.M.; Tripodi, V.P.
Filiación:Departamento de Industrias, Facultad de Ciencias Exactas y Naturales, University of Buenos Aires, Int. Güiraldes 2620, Ciudad Universitaria, Buenos Aires, C1428BGA, Argentina
Departamento de Química Analítica y Fisicoquímica, Facultad de Farmacia y Bioquímica, University of Buenos Aires, Junín 954, Buenos Aires, C1113AAD, Argentina
Departamento de Tecnología Farmacéutica, Facultad de Farmacia y Bioquímica, University of Buenos Aires, Junín 954, Buenos Aires, C1113AAD, Argentina
Palabras clave:Coenzyme Q10 (PubChem CID: 9962735); Coenzyme Q10 stability; Coenzyme Q10 treatment; Dynamic rheology; Dysphagia; Ethylcellulose; Ethylcellulose (PubChem CID: 24832091); High-dose coenzyme Q10; Lecithin from soybean (PubChem CID: 57369748); MCT oil (PubChem CID: 93356); Oleogels; SMS or sorbitan monostearate or Span 60 (PubChem CID: 14928); ethyl cellulose; medium chain triacylglycerol; phosphatidylcholine; ubidecarenone; Article; bulk density; controlled study; drug absorption; drug formulation; drug megadose; drug solubility; gel; glass transition temperature; human; hydrogen bond; kidney disease; melting point; oleogel; priority journal; supplementation; viscosity
Página de inicio:9
Página de fin:20
Título revista:International Journal of Pharmaceutics
Título revista abreviado:Int. J. Pharm.
CAS:ethyl cellulose, 9004-57-3; phosphatidylcholine, 55128-59-1, 8002-43-5; ubidecarenone, 303-98-0


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---------- APA ----------
Masotta, N.E., Martinefski, M.R., Lucangioli, S., Rojas, A.M. & Tripodi, V.P. (2019) . High-dose coenzyme Q10-loaded oleogels for oral therapeutic supplementation. International Journal of Pharmaceutics, 556, 9-20.
---------- CHICAGO ----------
Masotta, N.E., Martinefski, M.R., Lucangioli, S., Rojas, A.M., Tripodi, V.P. "High-dose coenzyme Q10-loaded oleogels for oral therapeutic supplementation" . International Journal of Pharmaceutics 556 (2019) : 9-20.
---------- MLA ----------
Masotta, N.E., Martinefski, M.R., Lucangioli, S., Rojas, A.M., Tripodi, V.P. "High-dose coenzyme Q10-loaded oleogels for oral therapeutic supplementation" . International Journal of Pharmaceutics, vol. 556, 2019, pp. 9-20.
---------- VANCOUVER ----------
Masotta, N.E., Martinefski, M.R., Lucangioli, S., Rojas, A.M., Tripodi, V.P. High-dose coenzyme Q10-loaded oleogels for oral therapeutic supplementation. Int. J. Pharm. 2019;556:9-20.