High dose coenzyme Q10 loaded oleogel for therapeutic supplementation.

HÖCHT, C.; TRIPODI V.P.; MARTINEFSKI M.R.; ROJAS A.M.; EHRENHAUS MASOTTA, N.; LUCANGIOLI S.

New York

Conferencia; The 9th Conference of the International Coenzyme Q10 Association.; 2018

International Coenzyme Q10 Association.

In recent years the therapeutic recommended dose of Coenzyme Q10 (CoQ10) significantly increased, reaching values up to 50 mg/kg/day. Patients with CoQ10 deficiency usually have swallowing difficulties, whereby the use of solid dosage forms is not the best option because they find them hard to swallow resulting in a lower adherence to the treatment. In order to satisfy the high-level requirements in adult patients and offer them a more comfortable way of treatment, a new oral CoQ10 dosage form was developed and evaluated.As CoQ10 is practically insoluble in aqueous solutions because of its lipophilic nature, oleogels were proposed to dose CoQ10 by its dissolution in medium-chain triglyceride (MCT) oil, using ethylcellulose for gelling and sorbitan monostearate (SMS) as surfactant. Thermoreversible oleogels with a maximal amount of 1g of CoQ10 were developed with proved stability during at least 12 months of storage at 25.0°C. SMS allowed high stability to oxidation of the MCT-oil retained by the gel network, as well as low syneresis. Plastic deformation of oleogels without fracture was determined under compression, which can emulate the deformation behavior of the material into the oral cavity. The bioavailability of CoQ10 after oral intake of oleogel containing 1g of CoQ10 was compared with the commercial capsule in a preliminary pharmacokinetic study involving 7 healthy subjects. Comparison of main pharmacokinetic parameters showed similar maximal concentration and half-life of CoQ10 after intake of both formulations and a non-significant increase in the area under the curve with the oleogel when compared with the commercial capsule.In conclusion, the use of oleogels could promote the adherence to the treatment, ameliorating the discomfort perceived during swallowing by these patients and could be a useful alternative for the treatment of adult patients with high CoQ10 requirements.