The Rational Design Approach for a More Efficacious and Sustainable Peptide

Consumers are looking for sustainable, powerful and targeted solutions to address their specific skin care concerns. The Rational Design approach delivers. Today’s consumers are knowledgeable about skincare and focus on routines that meet their specific needs, such as firming, wrinkle reduction or brightening. They actively search for products to meet these needs, reading product labels and researching the ingredients that can provide the benefits they desire. Peptides are often the hero ingredients in these products.

What’s a peptide?​

Peptides are composed of short chains of amino acids that can range from 2-50 amino acids, with peptides cosmetic applications - typically synthetic peptides - ranging from 2-8 amino acids. These short chains of amino acids have a defined structure and mode of action that can have significant and measurable efficacy on skin and hair. Within facial skincare, peptides are commonly found in anti-aging products. Depending on the variable amino acid composition, peptides can also produce many other skin benefits. A wide variety of peptides are key ingredients in many personal care products. According to scientific literature, peptides can be categorized according to their mechanism of action [i] [ii]. These categories include but are not limited to:

• Signal peptides, which for example stimulate matrix protein production (such as elastin and collagen).
• Skin barrier enhancing peptides, which strengthen skin barrier function and increase skin resilience.
• Neurotransmitter-inhibiting peptides, which inhibit the action of acetylcholine, a neurotransmitter responsible for muscle contractions. This reduces expression wrinkles.
• Melanogenesis modulating peptides, which can up or downregulate pigmentation.

What makes a better peptide?​

An ideal method utilized in the creation of peptides with strong efficacy is the Rational Design approach. A key element of this approach is an iterative process that involves the design, synthesis, and testing of biological activity of molecules. As a final step, analysis of the activity of different molecules is used to select the best performing compound, or, as input for further design cycles. Rational design is so effective because it maximizes efficiency by reducing the number of compounds required for synthesis and testing as well as reducing the time required to achieve desired molecular properties. An integral step in the design stage includes researchers identifying key structural features responsible for a molecule’s activity and using this information to design new molecules with the same or even superior performance. Furthermore, in silico predictions can help rank molecules according to their expected activity and help prioritize compounds for synthesis.

There are clearly defined steps that are taken when developing a peptide through Rational Design:

1. Using Artificial Intelligence, identify and model the relevant biological target
2. Design a range of compounds that could interact with this target
3. Measure how well the molecules and enzymes interact with each other
4. Synthesize relevant compounds
5. Perform biological testing

The sustainability factor​

Sustainability is very important to consumers. In a recent beauty consumer survey [iii]of 2,000 females, it was revealed that 74% of respondents associated “sustainability” with ingredients that are renewable, replantable and sustainable. So, it’s no surprise that sustainability has been a focus of the beauty industry for the past few years, and synthetic peptides have been a part of this conversation as well.

There is a misconception among consumers that synthetic peptides are not sustainable. That is not the case. When the 12 Green Principles of Chemistry are closely followed for protein synthesis, great measures are taken in the efforts to prevent waste. Synthetic methods are designed to maximize the incorporation of all materials used in the process into the final product. Efforts are made to reduce energy consumption. Additionally, efforts can be made to minimize toxicity directly by molecular design and design chemical reactions and synthetic routes to be as safe as possible. It is a priority to reduce the environmental impact when chemical synthesis is conducted.

Although some peptides are synthetically produced, the building blocks are still amino acids, which are natural to the environment. Therefore, synthetic peptides are not contributing anything foreign to the ecosystem. Moreover, the use level of peptides is very low, reducing even more the environmental impact about 100 times lower when compared to other bioactives.

Peptides formulated in natural origin solvent (glycerin) meet the natural origin ISO 16128 index, a guideline that offers a framework to determine the natural, natural origin, organic and organic origin content of products based on the ingredient characterization, is very high (99.9%). Naturality is regarded as a positive to many consumers today. And most importantly, peptides, both natural and synthetic, are targeted to achieve a specific benefit so they are especially high in efficacy.

A more focused and sustainable approach for today’s savvy consumer​

Peptides have become an integral part of the consumer skincare routine, and peptides created with the Rational Design approach offer a powerful solution targeted for specific consumer benefits in better performing products with positive sustainability benefits, and this approach also enables ingredient manufacturers to produce peptides with specific benefits more efficiently.

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[i] Errante, Fosca et al. “Cosmeceutical Peptides in the Framework of Sustainable Wellness Economy.” Frontiers in chemistry vol. 8 572923. 30 Oct. 2020, doi:10.3389/fchem.2020.572923

[ii] Lima TN, Pedriali Moraes CA. Bioactive Peptides: Applications and Relevance for Cosmeceuticals. Cosmetics. 2018; 5(1):21. https://doi.org/10.3390/cosmetics5010021

[iii] Global Cosmetic Industry: Consumers’ Sustainable Beauty Attitudes, June 2022