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Photo: Stokkete/Shutterstock.com
Photo: Stokkete/Shutterstock.com

Adaptogenic ingredients that increase the skin’s adaptability are the latest trend. AnnonaSense CLR which potently interacts with our skin’s endocannabinoid system, has relevant adaptogenic activity. In addition, it reduces skin sensitivity and itching while improving skin appearance and feel.

According to market research organisations such as Mintel, GlobalData and Euromonitor, skin health and well-being are major drivers of the skin care market. No matter what the claim on the cosmetic package, be it “hydration” or “anti-wrinkle,” the main reason for consumers to buy a cosmetic product is to improve their skin’s health, well-being and overall quality of life. 

What are consumers’ real skin problems and needs? What are the underlying mechanisms in their skin causing these problems? Can we provide consumers with an effective solution? Providing a short-term solution is a lot easier than providing a solution which is both efficacious and sustainable. However, it is the real and fundamental solution consumers are searching for. They are happy to use a cosmetic product once or twice per day, but it should not only be just a “band-aid” masking their problem, providing less than the expected benefits. 

In addition to this, many consumers have problematic skin or perceive their skin to be problematic. In fact, 50% of people in the industrialised world perceive their skin as being sensitive. The prevalence of skin problems related to both skin diseases and systemic diseases is increasing strongly. Virtually everybody suffers from acne at least once in their lifetime. Atopic dermatitis and psoriasis are occurring more frequently. The prevalence of diabetes is growing tremendously as well and can have important negative implications for skin, too. 

Consumers have problems with their skin and want the cosmetic industry to provide them with sustainable problem-solvers. They want skin health and well-being, and they simply want to look good and feel good. 

fig. 1: Agonistic influence on CB2
fig. 1: Agonistic influence on CB2

Adaptability equals health and health leads to well-being

Adaptability is the ability of a system to adapt itself efficiently and quickly to changed circumstances. Our skin is constantly exposed to changing circumstances. External factors such as radiation from the sun, free radicals and environmental humidity can negatively influence the skin. Endogenous factors, such as hormones, also have a strong impact on the skin. Despite these influences, the skin’s adaptability is key for sustaining a healthy balance, a homeostasis in skin. Only when skin is in homeostasis it is healthy. Along with skin health, well-being is achieved. Healthy skin looks good and feels good, which is what satisfies the consumer

fig. 2: Influence on skin sensitivity
fig. 2: Influence on skin sensitivity

Adaptogens increase skin’s adaptability

Adaptogens strengthen biological systems that have been compromised by stress, and have a protective effect on health. They increase skin’s adaptability, which in turn promotes sustainable health. An adaptogenic approach potently and sustainably improves skin health which leads to improved well-being and a satisfied consumer. Adaptogens do not mask problems, e.g. reduce redness, but go to the core of the problem and re-establish a stable homeostatic balance.

□The skin is an endocannabinoid (ECS) or endovanilloid (EVS) system. The ECS and EVS are strongly interwoven, and the ECS is virtually the only biological system in our body which can effectively overrule the detrimental EVS. ECS-induced promotion of homeostasis will reduce EVS-induced problems. These systems are high in the hierarchy of our body’s biological systems and regulate biological systems that are lower in the hierarchy. Regulating the balance between ECS and EVS provides the opportunity to reach a stable homeostatic balance, and also to keep this balance stable. This is the basis of an adaptogenic approach.

Of particular interest are the cellular receptors CB2 (Cannabinoid Receptor Type-2), part of the ECS, and TRPV1 (Transient Receptor Potential Channel, Vanilloid subfamily member 1), part of the EVS. Activation of TRPV1 triggers the production of inflammatory mediators, which are important in skin inflammation. When the TRPV1 on sensory neurons is activated, the cells which make up the sensory nerves in our skin can lead to itching, pain and burning sensations. TRPV1 is one of the key instigators for the loss of skin health and well-being.

Like TRPV1, CB2 is a cellular receptor, which can be found both on keratinocytes and also on sensory neurons in the skin. When CB2 is activated, the human cell reacts, which in turn leads to the deactivation of TRPV1. This restores and maintains a healthy homeostasis. 

fig. 3: Influence on skin appearance
fig. 3: Influence on skin appearance

A new adaptogen for skin health and well-being

Our company has developed AnnonaSense CLR*, an adaptogen to sustainably achieve skin health and well-being by interaction with CB2. 

The agonistic effect of this ingredient on CB2 was proven with various in vitro assays.

293T-CB2 cells were incubated with different concentrations of our ingredient AnnonaSense CLR and a positive control (WIN55, 212-2 [1 μM), respectively, for 10 minutes. The positive control is a specific agonist for CB2. Subsequently the cells were treated with Forskolin (10 μM) for 6 hours. The CB2-induced reduction of Forskolin-induced cAMP production was determined, where the result obtained with the positive control was set at 100%. 

At two different concentrations, treatment with our active ingredient showed a strong agonistic effect on CB2, where the higher concentration of the two outperformed a specific agonist for CB2, see fig.1. 

fig. 4: Perception of skin health and well-being
fig. 4: Perception of skin health and well-being

In vitro proven reduction of TRPV1 activity

In other in vitro studies it was shown that, through its agonistic activity on CB2, our active ingredient was able to reduce the activity of TRPV1. It was shown to reduce TRPV1-induced inflammation and additionally was able to reduce the inflammatory processes induced by histamine, substance P and TNFα. IL-31RA, the receptor for IL-31, was also addressed. 

IL-31 plays an important role in skin diseases, specifically in itchiness and reduced skin health. Our ingredient reduced the expression of IL-31RA, illustrating its potency for improving skin health and well-being.

In vivo assessment of skin sensitivity 

One application of the test product was performed on 17 volunteers for 250 Hz and 18 volunteers for 5 Hz (including 5 with atopic dermatitis, 3 with type IV allergy, 6 with sensitive skin and 1 with diabetes type II). Skin sensitivity was determined by measuring the current perception threshold (CPT) with a Neurometer CPT/C from Neurotron at 250 Hz and 5 Hz before and 30 minutes after application of the test product. Baseline at t = 0 was set at 0%. Values are based on averages of individual results of all volunteers.

The 250 Hz experiment showed that the formulation with our ingredient outperformed the corresponding placebo formulation by more than 35%. The 5 Hz experiment showed even clearer results: the formulation with our ingredient performed more than 60% better than the placebo formulation, see fig. 2. These results show that AnnonaSense CLR clearly makes skin more balanced. 

In-vivo study proves better skin appearance

In a double-blind study, 22 volunteers tested a formulation with AnnonaSense CLR, and 20 tested a placebo formulation. Redness was scored at t = 0 and after 17 days of twice daily application of the test products. Baseline at t = 0 was set at 0%.

An unhealthy appearance of skin can have important negative consequences on a person’s well-being and quality of life. In this study, 17 days of application of the test substance showed that the formulation with our ingredient improved skin appearance. Where the placebo formulation reduced skin redness by 25%, the corresponding formulation containing our ingredient clearly outperformed the placebo formulation and reduced redness by more than 36%, see fig. 3.

Perception of skin health and well-being

The 22 volunteers who applied 3% of our ingredient in an aqueous gel were given a questionnaire after 17 days of twice daily application. They were asked whether a simple aqueous gel, containing 3% of our AnnonaSense CLR, improved skin health and well-being. Almost 75% of the testers found that both the intensity and the frequency of itching were reduced. A clear majority of the users confirmed that the feeling of tension in their skin as well as their quality of life were improved. An even larger majority stated that using the product with our ingredient had improved their well-being, see fig. 4.

Establishes a sustainable homeostatic balance 

The consumer buys cosmetic products mainly to improve skin health and well-being. This requires a potent approach in terms of ingredients. In our studies it was clearly shown that AnnonaSense CLR potently interacts with our skin’s endocannabinoid system and thus has relevant adaptogenic activity. 

The ingredient strongly reduces skin sensitivity and itching. Both are important parameters in achieving skin health. Another parameter is skin appearance. Our ingredient AnnonaSense CLR was shown to improve the parameter of skin appearance as well. In a last study it was shown that users perceived the activity of our ingredient, too. Frequency and intensity of itch were reduced, skin feel was improved, and quality of life and well-being were enhanced.

* INCI name: Annona Cherimola Fruit Extract

AUTHORS:

Harald van der Hoeven, Director Technical

Marketing, Dr Heiko Prade, Director R&D

Chemisches Laboratorium Dr. Kurt Richter (CLR)

Berlin, Germany

www.clr-berlin.com 

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