Novel Lipid-Free Nanoformulation for Improving Oral Bioavailability of Coenzyme Q10

Abstract

To improve the bioavailability of orally administered lipophilic coenzyme Q10 (CoQ10), we formulated a novel lipid-free nano-CoQ10 system stabilized by various surfactants. Nano-CoQ10s, composed of 2.5% (w/w) CoQ10, 1.67% (w/w) surfactant, and 41.67% (w/w) glycerol, were prepared by hot high-pressure homogenization. The resulting formulations were characterized by particle size, zeta potential, differential scanning calorimetry, and cryogenic transmission electron microscopy. We found that the mean particle size of all nano-CoQ10s ranged from 66.3 ± 1.5 nm to 92.7 ± 1.5 nm and the zeta potential ranged from −12.8 ± 1.4 mV to −41.6 ± 1.4 mV. The CoQ10 in nano-CoQ10s likely existed in a supercooled state, and nano-CoQ10s stored in a brown sealed bottle were stable for 180 days at 25°C. The bioavailability of CoQ10 was evaluated following oral administration of CoQ10 formulations in Sprague-Dawley rats. Compared to the values observed following administration of CoQ10-Suspension, nano-CoQ10 modified with various surfactants significantly increased the maximum plasma concentration and the area under the plasma concentration-time curve. Thus, the lipid-free system of a nano-CoQ10 stabilized with a surfactant may be an effective vehicle for improving oral bioavailability of CoQ10.

Nanoemulsions as delivery systems for lipophilic nutraceuticals: strategies for improving their formulation, stability, functionality and bioavailability

“…A number of researchers have been conducted on the design of nanoemulsions for the encapsulation, protection, and release of CoQ 10 . Zhou et al (2014a;2014b) prepared CoQ 10 -enriched nanoemulsions stabilized with D-a-polyethylene glycol 1000 succinate, polyoxyl 40 hydrogenated castor oil, polyglycerol 10 stearic acid ester, and sucrose palmitate using a high-pressure homogenizer at 60°C. They then evaluated the bioavailability of CoQ 10 after oral administration in rats.…”

Coenzyme Q10 Supplementation for the Reduction of Oxidative Stress: Clinical Implications in the Treatment of Chronic Diseases

“…The uptake and distribution of CoQ 10 after oral ingestion are determined by its lipophilic characteristics, which give it extremely low solubility in water. In this sense, the typical regimen for oral administration of CoQ 10 takes advantage of its lipophilic solubility and recommends co-administration with lipid-rich foods [ 18 ]. Despite these recommendations, research into exogenous CoQ 10 absorption and bioavailability has proved high variability that depends on the type of CoQ 10 preparation studied [ 15 , 19 ].…”

Introduction of Nanotechnology in Herbal Drugs and Nutraceutical: A Review

“…A novel lipid-free nano-CoQ10 system formulated and stabilized by various surfactants and the bioavailability of CoQ10 was evaluated by oral administration of CoQ10 formulation in Sprague-Dawley rats. The formulation can be an effective vehicle for improving oral bioavailability of CoQ10, it was confirmed by the observation of significant increase in the maximum plasma concentration and the area under the plasma concentration time curve [36]. The bioavailability of heptadecanoic acid and CoQ10 was investigated for the influence of droplet size and oil digestibility by a rat feeding study.…”