Crystal engineering: Circe Scientific fuses anti-aging blueberry molecule with tryptophan compound for better absorption

13 Sep 2023 --- Harnessing molecular technologies in a budding science called “crystal engineering,” innovators at Circe Scientific have managed to fuse an anti-aging extract of blueberries with a natural molecule found in the human body to create a multifunctional “cocrystal” that stimulates more effective absorption in skin health applications.

“Crystal engineering is a wide technical area in chemistry, focused on the solid (crystalline) forms of molecules,” Fernando Barrera, CEO and co-founder at Circe Scientific, tells Personal Care Insights.

“It is commonly used in the pharmaceutical industry, looking for the more stable soluble crystal form for their active ingredients, normally by studying its polymorphism (the different crystalline forms of each active ingredient).”

Circe Scientific’s cocrystallization is a new field of crystal engineering, Barrera notes. It is a new method that looks for new crystal forms of two or more molecules included in the same lattice. 

Crystal engineering enables the creation of a more readily absorbable and effective form of pterostilbene, a compound in blueberries with photoprotective properties in skin care.The process combines an active ingredient and a coformer. This pairing interacts on a molecular level, resulting in a new crystalline form that contains both molecules.

“This is not a mix of two different crystals but a new crystal containing the two molecules together,” Barrera clarifies.

He adds that in crystallizing two molecules together, they are not chemically changed. “So, when you ingest or dissolve the cocrystal, you have the same unchanged original molecules. We do not modify the molecules; we only find new solid forms for them.”

Circe Scientific says its “re-engineering” of ingredient molecules is applicable for both nutrition and beauty product developments.

Secret to blueberry’s protective properties
Thanks to its fast absorption speed, the company’s new blueberry-based ingredient – branded Pteroyouth – is ideal for both oral and topical products, making it suitable for “beauty-from-within” packs.

The launch comes at a time when the improvement in life expectancy has been increasing, while the ability to find products that help delay premature skin aging has “not evolved as much,” as Circe Scientific communicates.

The secret of the rejuvenating power of blueberries is pterostilbene. The molecule is produced by blueberry plants to ensure survival against exposure to UV radiation, drought, microorganisms and other environmental stressors. 

Pterostilbene can also help human skin to remain smoother, more supple and youthful over the years, details the supplier. However, due to its poor solubility, it is not an easy molecule to use in skin care products.

Circe Scientific spent more than a decade dedicated to crystal engineering research, in developing Pteroyouth.

“After years of research, Circe Scientific has managed to create a product, Pteroyouth, which provides a solution to this need that we detected in the cosmetics industry,” illustrates Barrera.

“Its function is to improve the solubility of pterostilbene, to facilitate its administration, increasing its bioavailability and stability. As a result, we have a revolutionary product that improves the efficacy of cosmetic treatments.”

With headquarters in Palma de Mallorca and Barcelona, Spain, Circe Scientific is focused on furthering the discovery of new solid forms of health-promoting cosmetic and nutraceutical ingredients.Pteroyouth brings various benefits to the skin, reinforcing the body’s antioxidant defenses. It most notably is designed to help the skin maintain a healthy structure when exposed to UVA and UVB rays, while helping skin modulate pigmentation associated with environmental stress and age.  

The ingredient also increases cellular production of Nrf2 and decreases cellular production of NF-kB, which helps the skin to modulate the inflammatory response. It does this while enhancing the activity of sirtuins, the “longevity enzymes,” which regulate cellular activities related to cell vitality and aging.

Crystal engineering mechanics
In producing Pteroyouth through crystal engineering, Circe Scientific combines pterostilbene with picolinic acid, a natural molecule in the human body and a tryptophan derivative that stimulates mineral absorption and the body’s immune response.

“Circe Scientific is not the only specialist in the cocrystallization technology. There are a few crystal engineering contract research organizations working for the pharma industry, but Circe is one of the more specialized in cocrystals. Our teams have developed a proprietary software to predict cocrystal formation,” says Barrera.

“We have been doing cocrystals exclusively for the last ten years. Circe was the only cocrystal specialist in the nutraceutical industry until one Chinese company was founded with the same focus last year.”

With cocrystal coformers there is no “fits all” solution. Barrera explains that each ingredient has “up to hundreds” of potential “coformers” that can form cocrystals with it. However, in the vast majority of potential combinations, a cocrystal will likely be impossible to form. 

“Usually, a coformer that forms a cocrystal with one ingredient won’t work for another one,” he explains. “These other combinations also might not achieve the right properties. So, for each ingredient, we must find the right coformers.”

For the nutraceutical or cosmetics industries, coformers must also be substances that are already approved for, or able to be used by, humans.

“At Circe Scientific we try to go a step further and find a coformer that is also a functional ingredient, looking not only to fit in the cocrystal to modify the undesirable properties of the targeted ingredient but also looking for synergies in health benefits of both ingredients, if possible,” says Barrera.

Cocrystalization has applicability in both the ingestible beauty and topical skin care categories.What’s next in the crystalline pipeline
With headquarters in Palma de Mallorca and Barcelona, Spain, the company is focused on furthering the discovery of new solid forms of health-promoting cosmetic and nutraceutical ingredients, such as pterostilbene, ubiquinol, sitosterol and vitamin D.

“While we are one of the first companies to launch cocrystals to be used in nutraceuticals and cosmetics, an American company introduced the first cocrystal (discovered by a university) in the nutraceutical industry nine years ago,” says Barrera.

“The use of cocrystallization for both topical skin and oral nutrition changes in the sense that you may not be looking for the same improvement function,” he notes. “For example, our Pteroyouth (cosmetics) or Pterovita (nutraceuticals and food) products can be based on the same cocrystal, but the Certificate of Analysis is different, and their formulations would be different to maximize different properties.”

Barrera believes cocrystals can theoretically be created to suit a variety of other functionalities. With time, he states that products created to improve other functionalities like time-release formats or taste will be developed.

“The main function of our technology is to change the physicochemical properties of molecules, which depends on the crystal form used,” he comments. “So, in theory, different functionalities can be developed, such as solubility, dissolution rate (for time release formats), stability, photostability, taste, color and oral bioavailability.”

“We have several products looking to improve different functionalities. Several of these properties can be improved with the same cocrystal.”

By Benjamin Ferrer