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

Int J Pharm

Departamento de Tecnología Farmacéutica, Facultad de Farmacia y Bioquímica, University of Buenos Aires, Junín 954, C1113AAD Buenos Aires, Argentina.

Published: February 2019

AI Article Synopsis

  • * CoQ10 is poorly absorbed when taken normally due to its lipophilic (fat-loving) nature and low bulk density, making it challenging to formulate into effective oral medications.
  • * The study proposes the use of oleogels made with medium-chain triglyceride oil and a surfactant (like sorbitan monostearate) to create a more stable and soluble form of CoQ10, which may improve swallowing for patients who have difficulty.

Article Abstract

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.

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http://dx.doi.org/10.1016/j.ijpharm.2018.12.003DOI Listing

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

Int J Pharm

February 2019

Departamento de Tecnología Farmacéutica, Facultad de Farmacia y Bioquímica, University of Buenos Aires, Junín 954, C1113AAD Buenos Aires, Argentina.

Article Synopsis
  • * CoQ10 is poorly absorbed when taken normally due to its lipophilic (fat-loving) nature and low bulk density, making it challenging to formulate into effective oral medications.
  • * The study proposes the use of oleogels made with medium-chain triglyceride oil and a surfactant (like sorbitan monostearate) to create a more stable and soluble form of CoQ10, which may improve swallowing for patients who have difficulty.
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