Crystal engineering breakthough for anti-ageing blueberry molecule

CIRCE Scientific has spent over a decade working on crystal engineering research. The company started this particular project six years ago with the search for a new solid form, a cocrystal, that could solve the water insolubility and poor bioavailability limitations of blueberries. 

Blueberry plants produce pterostilbene to survive exposure to UV radiation, drought, microorganisms and this molecule can also help skin look more youthful. However, due to its poor solubility, it is not an easy molecule to use in skin care products.

 'A multifunctional co-crystal' ​

Using its proprietary co-crystal engineering platform, the company has developed an ingredient that improves the solubility of pterostilbene, to increase its bioavailability and stability.

New ingredient Pteroyouth is a multifunctional co-crystal that combines pterostilbene with picolinic acid, a natural molecule in the human body and a tryptophan derivative, which stimulates mineral absorption and the body's immune response.

Fernando Barrera, Co-founder and CEO of CIRCE Scientific said the ingredient has a fast absorption speed and is ideal for use in both oral nutraceuticals and topical skin care products.

As the co-crystal greatly improves aqueous solubility of pterostilbene, it can be used in aqueous base lotions and creams to create formulations that don’t give an oily texture on the skin.

“Its powerful antioxidant and regeneration activation will protect the skin from all kinds of aggressions,”​ explained Barrera.

“As an example of its protection activity, even if Pteroyouth is not a sunscreen ingredient (its theoretical SPF is just around 20), its powerful activation of cell defence and restoration allows it to outperform the skin protection of sunscreens in the range of SPF 50 to 90. Also, as it comes from within the cells below the skin surface, this protection will not be lost if the skin is washed after the ingredient is applied,” ​he shared.

The company said the ingredient can offer numerous skin care benefits including: helping skin maintain a healthy structure when exposed to UVA and UVB rays, promoting an optimal cellular response so skin maintains its structure when exposed to ionising radiation, reinforcing the body's antioxidant defences, increasing cellular production of Nrf2 and decreasing cellular production of NF-kB – to help skin modulate the inflammatory response, helping skin to modulate pigmentation associated with environmental stress and age, and enhancing the activity of sirtuins (the "longevity enzymes," which regulate cellular activities related to cell vitality and ageing).

Using ​co-crystallisation technology​​

“Co-crystallisation is a new technology that looks to find crystal forms of two or more molecules included in the same lattice,” ​explained Barrera. “It is not a mix of two different crystals, but a new crystal containing the two molecules forming a single crystal (that is composed of the two molecules). This means that the ingredients of a co-crystal can’t be separated without dissolving the crystal again.”​

He continued: “This addition of a second molecule, called a co-former, cannot be ‘forced’, the two molecules must ‘fit’ naturally (their spatial form, charge, distribution, etc.), so a lot of work is necessary to find the right co-former. Each substance may have several good fits but finding the right ones between thousands of possibilities is not easy.”​

Barrera said that finding a viable co-former does not assure the co-crystal will have the desired properties, so it involves screening by trial and error. 

“Once we have got a good co-crystal candidate, the scientific focus goes to test if we have sufficiently improved the desired properties, so different in vitro and in vivo assays are designed and done,” ​he shared. “Finally, the last technical challenge is the production scale-up to an industrial batch size.”​

CIRCE said it now working on the development of new cocrystals to that will improve people’s health and longevity.