AQUANOVA AG has announced new human clinical data showing that its NovaSOL micellar delivery technology can significantly increase the bioavailability of xanthohumol compared with the native form of the hop-derived bioactive.
The findings come from a randomised, controlled crossover trial published in Molecular Nutrition & Food Research, which investigated the influence of formulation and dose on xanthohumol absorption in 12 healthy adults.
Micellar formulation increases plasma exposure
Participants received 86 mg or 172 mg of either native xanthohumol or xanthohumol formulated using NovaSOL technology.
Micellar xanthohumol produced significantly higher area under the plasma concentration-time curve (AUC), maximum plasma concentration (Cmax) and apparent bioavailability than the native ingredient.
At the 172 mg dose, NovaSOL xanthohumol generated approximately 3.2 times greater 24-hour plasma exposure than the equivalent dose of native xanthohumol.
Cmax was also substantially higher, reaching 2379 nmol/L compared with 249 nmol/L for native xanthohumol.
The researchers reported that micellation was the main factor influencing bioavailability, with bioavailability approximately nine times higher following consumption of micellar xanthohumol than the native form across the doses tested.
The micellar formulation also reached peak concentrations more rapidly.
At 86 mg, peak total xanthohumol concentrations were reached at approximately 58 minutes, compared with 148 minutes for native xanthohumol.
What is micellation?
Micellation is a formulation approach used to improve the solubility and absorption of poorly water-soluble compounds.
In simple terms, micelles are tiny structures that can surround and carry lipophilic ingredients, helping them disperse more readily in an aqueous environment such as the gastrointestinal tract.
This can make it easier for the compound to come into contact with the intestinal surface and be absorbed.
For ingredients such as xanthohumol, which have poor water solubility, micellation can therefore be used as a delivery strategy to increase the amount of the active that becomes available for absorption, without chemically modifying the ingredient itself.
AQUANOVA's NovaSOL technology uses micellar solubilisation to formulate lipophilic bioactives — such as xanthohumol — into a more water-dispersible form.
Delivery technology targets formulation challenges
Xanthohumol is a prenylated chalcone found primarily in hops (Humulus lupulus). It is hydrophobic, which creates a formulation challenge because of its limited aqueous dispersibility and oral bioavailability.
AQUANOVA's NovaSOL technology aims to use micellar solubilisation to disperse lipophilic compounds in liquid colloidal formulations, using food-grade components and avoiding chemical modification of the active ingredient or nanomaterials.
This new study also adds to AQUANOVA's recent focus on clinical evidence for micellar delivery.
Last year, research involving NovaSOL astaxanthin also examined the pharmacokinetic performance of a micellar formulation against standard astaxanthin.
AQUANOVA will be showcasing its formulation technologies at this year's SupplySide Global show, held from October 26-30 at the Mandalay Bay Convention Center in Las Vegas.
