Novel solid self-emulsifying drug delivery system of coenzyme Q10 with improved photochemical and pharmacokinetic behaviors

The present study was undertaken to develop a solid self-emulsifying drug delivery system of coenzyme Q10 (CoQ10/s-SEDDS) with high photostability and oral bioavailability. The CoQ10/s-SEDDS was prepared by spray-drying an emulsion preconcentrate containing CoQ10, medium-chain triglyceride, sucrose ester of fatty acid, and hydroxypropyl cellulose, and its physicochemical, photochemical, and pharmacokinetic properties were evaluated. The CoQ10/s-SEDDS powder with a diameter of ca. 15 μm was obtained by spray-drying, in which the CoQ10 was mostly amorphized. The CoQ10/s-SEDDS exhibited immediate self-emulsification when introduced to aqueous media under gentle agitation, forming uniform fine droplets with a mean diameter of ca. 280 nm. There was marked generation of reactive oxygen species, in particular superoxide, from CoQ10 exposed to simulated sunlight (250 W/m2), suggesting potent photoreactivity. Nano-emulsified solution of CoQ10 under light exposure underwent photodegradation with 22-fold higher degradation kinetics than crystalline CoQ10, although the CoQ10/s-SEDDS was less photoreactive. After the oral administration of CoQ10/s-SEDDS (100 mg-CoQ10/kg) in rats, enhanced exposure of CoQ10 was observed with increases in both Cmax and AUC of ca. 5-fold in comparison with those of orally administered crystalline CoQ10. From the improved physicochemical and pharmacokinetic data, the s-SEDDS approach upon spray-drying might be a suitable dosage option for enhancing nutraceutical and pharmaceutical values of CoQ10.

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