Formulation and evaluation of ubidecarenone transdermal delivery systems Ubidecarenone transdermal delivery systems

Abstract

Purpose: This study is aimed to examine the feasibility of developing ubidecarenone (coenzyme Q10, CoQ10) transdermal delivery systems (TDS). Method: In vitro permeation study using solution formulation and pressure-sensitive adhesive (PSA) TDS and in vivo pharmacokinetic study were conducted. Results: When using solution formulations, isopropyl alcohol (103.39 ± 1.61), ethyl alcohol (81.55 ± 7.27), and the mixture of diethylene glycol monoethyl ether (DGME)propylene glycol monolaurate (PGML) at the ratio of 60:40 (91.08 ± 26.07) showed high flux (μgcm2hour). The addition of fatty acids to DGME-PGML failed to show profound enhancing effects; only unsaturated fatty acids such as linoleic acid and oleic acid at 3 and caprylic acid at 3 and 10 slightly increased permeation flux. CoQ10 from the acrylic PSA TDS showed biphasic permeation profile that was permeated very rapidly up to the first 12 hours, and after that, permeation rate became slower. Overall, 6 fatty acids showed high permeation rates and the highest maximum flux of 9.3 μgcm2hour was obtained with a formulation containing 6 lauric acid in DGME-PGML (60:40). The in vivo pharmacokinetic study using TDS with 6 fatty acids in DGME-PGML (60:40) showed that the absorption of CoQ10 decreased in the following order: TDS containing linoleic acid > oral dosage form > TDS with oleic acid > TDS with lauric acid > TDS with caprylic acid > TDS with capric acid. TDS containing oleic acid showed preferable pharmacokinetic profile with respect to lower Cmax, comparable AUC, and prolonged t12 and Tmax compared to oral administration of drug. Conclusions: For effective transdermal delivery system of CoQ10, 6 linoleic acid or oleic acid in DGME-PGML (60:40) could be employed. © Informa UK, Ltd.