CoQ10 gets formulation boost in beta-cyclodextrin
The solubility of CoQ10 in water was increased by a factor of at least 100 on complexation with cyclodextrin, according to findings published in the Journal of Inclusion Phenomena and Macrocyclic Chemistry.
Furthermore, scientists from Slovenia’s National Institute of Chemistry, report that complexation improved the stability of CoQ10 to light and heat, with over 64 per cent of CoQ10 unchanged after heat and light treatments.
Igor Pravst, PhD, from the R&D department of Slovenian company Valens told NutraIngredients.com that complexation of Q10 with cyclodextrins was first studied in mid-nineties.
Previously, researchers from Wacker-Chemie reported improved bioavailability for CoQ10 when complexed with gamma-cylcodextrin.
“The basic problem of Q10-gamma-CD was, and still is, that gamma-CD not very common in food products and also banned in many types of food products within some countries,” he said.
On the other hand, Dr Pravst said that beta-CD is the most wide used cyclodextrin that is very common in food and pharmaceutical industry.
Complexation between CoQ10 and bCD was developed and patented by Slovenia’s National Institute of Chemistry, he said, and Valens has the exclusive licence to production and distribution of CoQ10-bCD.
Delivery is key
There is an ever-growing body of scientific data that shows substantial health benefits of CoQ10 supplementation for people suffering from angina, heart attack and hypertension. Clinical trials have also reported benefits for cardiomyopathy and congestive heart failure.
However, the formulation of the CoQ10 is known to play a key role in its bioavailability. Since the coenzyme is lipophilic (fat-loving) its absorption is enhanced in the presence of lipids. Therefore, when taken as a supplement apart from meals, the absorption of some formulations is lower.
Trials with CoQ10 supplements in powder and oil-suspension forms are reported to result in small or negligible responses in plasma CoQ10 concentrations.
Cyclodextrin complexes
The NIC researchers used the ‘co-precipitation’ method to complex CoQ10 with beta- and gamma-cyclodextrin. They found that the solubility of CoQ10 in water increased with temperature and pH, with the water solubility at room temperature and pH 6.5
Improved by a factor of at least 100, they said.
When exposed to a combined UV light and temperature treatment, pure CoQ10 was found to degrade significantly, with only 27 per cent unchanged after the treatment.
When complexed with the cyclodextrin, over 64 per cent of the CoQ10 remained unchanged, wrote the researchers, led by Mirko Prosek.
“The complex formation leads to an increase in the water solubility, thermo- and photo-stability,” wrote Prosek and his co-workers. “The complex of CoQ10 with b-CD seems to be suitable as a pharmaceutical ingredient and food additive.
“It is already successfully used as a pharmaceutical ingredient in soft-capsules and syrup, and as a food additive in milk, yogurt, kefir, jam, marmalade and honey,” they added.
Availability
Pravst added that Q10vital is a sold as a liquid (7.5 per cent CoQ10) or as a powder (15 per cent CoQ10).
The first finished products were launched in 2006, said Pravst, with the ingredient still used in CoQ10-fortified milk, and dietary supplements, such as multivitamin effervescent tablets with Q10.
Source: Journal of Inclusion Phenomena and Macrocyclic Chemistry Published online ahead of print, doi: 10.1007/s10847-009-9555-4"Studies of CoQ10 and cyclodextrin complexes: solubility, thermo- and photo-stability" Authors: M. Milivojevic Fir, A. Smidovnik, L. Milivojevic, J. Zmitek, M. Prosek
