High-dose coenzyme Q10-loaded oleogels for oral therapeutic supplementation.
Int J Pharm
; 556: 9-20, 2019 Feb 10.
Article
em En
| MEDLINE
| ID: mdl-30529659
ABSTRACT
Coenzyme Q10 (CoQ10) is a mitochondrial respiratory cofactor and potent endogenous antioxidant. In CoQ10-deficient patients, early treatment with high-oral doses (5-50â¯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 1â¯g of dissolved CoQ10 per 5â¯g-disk were successfully developed with proved stability and solubility for 12â¯months (25.0⯰C). SMS was better than lecithin as a surfactant because it allowed lower syneresis, higher CoQ10 retention for 12â¯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.
Palavras-chave
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)
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Tensoativos
/
Celulose
/
Ubiquinona
/
Antioxidantes
Idioma:
En
Revista:
Int J Pharm
Ano de publicação:
2019
Tipo de documento:
Article
País de afiliação:
Argentina