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

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,...

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Autores principales:	Masotta, N.E., Martinefski, M.R., Lucangioli, S., Rojas, A.M., Tripodi, V.P.
Formato:	JOUR
Materias:	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
Acceso en línea:	http://hdl.handle.net/20.500.12110/paper_03785173_v556_n_p9_Masotta
Aporte de:	Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) de Universidad de Buenos Aires

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spelling	todo:paper_03785173_v556_n_p9_Masotta2023-10-03T15:33:09Z High-dose coenzyme Q10-loaded oleogels for oral therapeutic supplementation Masotta, N.E. Martinefski, M.R. Lucangioli, S. Rojas, A.M. Tripodi, V.P. 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 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. JOUR info:eu-repo/semantics/openAccess http://creativecommons.org/licenses/by/2.5/ar http://hdl.handle.net/20.500.12110/paper_03785173_v556_n_p9_Masotta
institution	Universidad de Buenos Aires
institution_str	I-28
repository_str	R-134
collection	Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA)
topic	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
spellingShingle	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 Masotta, N.E. Martinefski, M.R. Lucangioli, S. Rojas, A.M. Tripodi, V.P. High-dose coenzyme Q10-loaded oleogels for oral therapeutic supplementation
topic_facet	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
description	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.
format	JOUR
author	Masotta, N.E. Martinefski, M.R. Lucangioli, S. Rojas, A.M. Tripodi, V.P.
author_facet	Masotta, N.E. Martinefski, M.R. Lucangioli, S. Rojas, A.M. Tripodi, V.P.
author_sort	Masotta, N.E.
title	High-dose coenzyme Q10-loaded oleogels for oral therapeutic supplementation
title_short	High-dose coenzyme Q10-loaded oleogels for oral therapeutic supplementation
title_full	High-dose coenzyme Q10-loaded oleogels for oral therapeutic supplementation
title_fullStr	High-dose coenzyme Q10-loaded oleogels for oral therapeutic supplementation
title_full_unstemmed	High-dose coenzyme Q10-loaded oleogels for oral therapeutic supplementation
title_sort	high-dose coenzyme q10-loaded oleogels for oral therapeutic supplementation
url	http://hdl.handle.net/20.500.12110/paper_03785173_v556_n_p9_Masotta
work_keys_str_mv	AT masottane highdosecoenzymeq10loadedoleogelsfororaltherapeuticsupplementation AT martinefskimr highdosecoenzymeq10loadedoleogelsfororaltherapeuticsupplementation AT lucangiolis highdosecoenzymeq10loadedoleogelsfororaltherapeuticsupplementation AT rojasam highdosecoenzymeq10loadedoleogelsfororaltherapeuticsupplementation AT tripodivp highdosecoenzymeq10loadedoleogelsfororaltherapeuticsupplementation
_version_	1807320853283602432

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

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