Lean on Science, not marketing

31
May
There is a lot of confusing information out there today that needs clarification. In this postmodern era, it seems as if we are headed backward in many ways, and science, unfortunately, doesn’t seem to be immune. It is particularly perplexing in the health & beauty industry that many professionals and consumers lean on marketing instead of science to guide them.
Some skin experts, so-called authorities, must also be better disciplined in retrieving all of the facts before they speak out. Increasingly, scientific misinformation proliferates and spreads like wildfire in our interconnected world. Could this misinformation be actually ‘disinformation’, and is it caused by greed, dishonesty, or politics? Whatever the reasons, seeing and hearing about the disintegration of established facts is disconcerting. Here are just a few of the untruths.
As aesthetic professionals, one falsehood worthy of our attention is that retinyl palmitate (RP) is weak, meaning it is not as strong or effective as retinol or retinoic acid. This is disturbing as we know the foundation of skin care lies in the regular use of topical vitamin A, which can be tricky with retinol and retinoic acid because they cause irritation. This particular ‘untruth” is only correct when measuring the different forms of vitamin A weight for weight. RP is the ‘origin’ of every retinoic acid molecule (the active form of vitamin A) and is our skin cell’s (all bodily cells) natural storage form of vitamin A.
Vitamin A converts inside each individual skin cell from the natural ester storage form, retinyl palmitate, to the active form, retinoic acid. This occurs constantly and quickly. The ratio of retinyl esters to retinol to retinaldehyde and retinoic acid is kept constant at 91:3:3:3 %. Prof. Des describes this eloquently in a YouTube interview.
Humans have specially dedicated enzymes in every skin cell that perform this conversion from ester to the active form, retinoic acid, on the DNA. If we increase the amount of retinyl esters, we will increase the levels of retinoic acid, resulting in significant benefits. With this understanding, it would be better if we don't focus on concentrations but on the actual vitamin A “power," measured in international units (IU), not percentages. For example, comparing 1000 IU of retinyl palmitate to 1000 IU of retinoic acid, either has equal potency and effectiveness. The only difference between them is weight. This groundbreaking information means we can use skin-friendly fatty forms of vitamin A (esters) more often and in the sun when needed most due to their unique photo-protective properties. In addition, it’s a complete shift in how we have traditionally understood and recommended retinoids that will result in far fewer side effects and greater compliance. This is the key to combatting troublesome skin concerns and preventing non-melanoma skin cancers.
Currently, hydroxypinacolone retinoate is being touted by some as the ideal form of vitamin A for topical formulations. This is due to its uniqueness in not causing retinoid reactions. However, we must delve deeper into why this is the case. This compound may bypass the traditional gateways of retinoid receptors. Nonetheless, what truly matters is still the amount of Vitamin A (in IU) present in the product rather than the specific molecule. It is important to note that claims are generated on the effectiveness of certain forms of vitamin A based on marketing strategies and not with any scientific evidence. It would be a good start to use the correct terms of measurement. Vitamins are not measured in percentages.
A few years ago, a prominent dermatologic researcher in America wrote an article on vitamin A, claiming that only retinol and retinoic acid would produce changes in the skin and that, at best, vitamin A esters ( retinyl palmitate), in particular, are antioxidants. This article was published in a journal that was brought to my attention while visiting a dermatology practice in Washington State. I promptly forwarded the article to Prof. Des and his esteemed colleagues, whom I consider the world experts on vitamin A. The refutation sent to the author and journal is below.
Dear Editor,
All molecular forms of vitamin A, apart from the acid group, are substrates for providing the active acid forms of vitamin A (ligands), which are active on the nuclear vitamin A receptor groups.
None of the substrate molecules, such as retinol, retinyl palmitate, retinyl acetate, or retinaldehyde, have direct retinoid receptor activity.
All vitamin A molecules are equipotent simply because all have common biochemical pathways to the vitamin A acid forms. ( Retinoic acids)
It is misleading to state or imply that one form is more effective.
Of course, they occupy different places in vitamin A's life in human tissue, but they are interchanged systematically to meet cellular demands.
In these pathways, retinol occupies a pivotal position on the way to the irreversible retinaldehyde, retinoic acid, and catabolism via cytochrome P450 in the liver.
Efficacy and potency, molecule for molecule, are the same for all. A single retinol molecule or any storage form can only be turned into a single retinoic acid molecule. As all get formed into retinol before becoming the retinaldehyde, they are equal in effect.
Various forms of vitamin A more easily penetrate the skin than others. In addition, their tendency for irritation and anti-oxidant potential may differ, but never in efficacy as vitamin A.
The science of vitamin A biochemistry in skin is well established. Unless there are new groundbreaking developments to contradict conventional wisdom regarding retinoid nuclear receptors and their complex and varied behavior, I fear the facts presented in the first part of the Q&A are in error or, at best, misleading.
Vitamin A in skincare is a complex subject. The information has been made accessible through a book written by one of the great international experts on vitamin A, Professor Des Fernandes of Cape Town. The book is written for all readers and may be obtained from the publisher at www.fernro.com
Yours sincerely,
Dr Ernst Eiselen
Perth, Western Australia
References
1. Retinoids - A clinician’s Guide - Martin Dunitz - Second Edition 1998
2. Vitamin A - Skin Science Fernro Publishing - First Edition 2015
3. Retinoids: From Basic Science to Clinical Applications - Birkhäuser Molecular and Cell Biology Updates 1994
www.skinscienceauthority.com
Another example of this misinformation (disinformation) in the skincare world came in an email to Prof. Des about a leading Dutch dermatologist who warned about the dangers of using ethyl hexyl methoxycinnamate (EHM) in topical formulations. If more education is unavailable, this misinformation will create a recurrent problem for many valuable ingredients.
One of the most important questions to ask when questioning the safety of any chemical is to know at what dose (concentration) one is using it. Yes, Ethyl hexyl methoxycinnamate can be a hormone disruptor at an inappropriate dose. The individual who did the research in 1999 caused an enormous problem in Europe. Subsequently, Denmark banned all sunscreens containing EHM until actual scientists did a scientific analysis of EHM.
Extrapolating from the research, the ethyl hexyl methoxycinnamate dose for an adult human by mouth would be impossible to eat. You would need to consume a room full of this chemical every month to do potential harm. This is the only way; however, you will be able to detect the hormone disruption that frightens people. At lower doses, it does not work. At doses that your skin gets exposed to in an average sunscreen, in a lifetime of use, you would not absorb the EHM that the lab rats were forced to eat in the trial. From a hormone disruption safety point of view, EHM is unquestionably safe.
It is worth noting that various scientific committees severely reprimanded the person who raised all this nonsense about EHM. Aren’t more pressing public safety concerns, such as the soaring rates of skin cancer, more deserving of our attention?
Ethyl hexyl methoxycinnamate is sometimes used in formulations not as an SPF to protect your skin but instead to protect the product's light-sensitive molecules. This ensures a good shelf life and optimum levels of the active ingredient.
One important thing to remember is that EHM does not block blue light. Protecting skin from blue light is one of the most essential things a skincare regime should do, especially for those battling pigmentation. Blue light is pervasive and almost unavoidable. I ensure that my computer screen blocks as much blue light as possible and use high doses of vitamins A & C and other protective ingredients daily.
The key is knowing the scientific details of the ingredient dosage to determine the safety of any chemical. This is why anyone making a claim about an ingredient needs to check with chemists and qualified experts. This is not a new concept; Paracelsus, who lived about 500 years ago, was an early “chemist” who said: “All things are poison, and nothing is without poison. Solely the dose determines that a thing is not a poison.” Prof. Des adds, “The dose makes the poison.”
Some skin experts, so-called authorities, must also be better disciplined in retrieving all of the facts before they speak out. Increasingly, scientific misinformation proliferates and spreads like wildfire in our interconnected world. Could this misinformation be actually ‘disinformation’, and is it caused by greed, dishonesty, or politics? Whatever the reasons, seeing and hearing about the disintegration of established facts is disconcerting. Here are just a few of the untruths.
As aesthetic professionals, one falsehood worthy of our attention is that retinyl palmitate (RP) is weak, meaning it is not as strong or effective as retinol or retinoic acid. This is disturbing as we know the foundation of skin care lies in the regular use of topical vitamin A, which can be tricky with retinol and retinoic acid because they cause irritation. This particular ‘untruth” is only correct when measuring the different forms of vitamin A weight for weight. RP is the ‘origin’ of every retinoic acid molecule (the active form of vitamin A) and is our skin cell’s (all bodily cells) natural storage form of vitamin A.
Vitamin A converts inside each individual skin cell from the natural ester storage form, retinyl palmitate, to the active form, retinoic acid. This occurs constantly and quickly. The ratio of retinyl esters to retinol to retinaldehyde and retinoic acid is kept constant at 91:3:3:3 %. Prof. Des describes this eloquently in a YouTube interview.
Humans have specially dedicated enzymes in every skin cell that perform this conversion from ester to the active form, retinoic acid, on the DNA. If we increase the amount of retinyl esters, we will increase the levels of retinoic acid, resulting in significant benefits. With this understanding, it would be better if we don't focus on concentrations but on the actual vitamin A “power," measured in international units (IU), not percentages. For example, comparing 1000 IU of retinyl palmitate to 1000 IU of retinoic acid, either has equal potency and effectiveness. The only difference between them is weight. This groundbreaking information means we can use skin-friendly fatty forms of vitamin A (esters) more often and in the sun when needed most due to their unique photo-protective properties. In addition, it’s a complete shift in how we have traditionally understood and recommended retinoids that will result in far fewer side effects and greater compliance. This is the key to combatting troublesome skin concerns and preventing non-melanoma skin cancers.
Currently, hydroxypinacolone retinoate is being touted by some as the ideal form of vitamin A for topical formulations. This is due to its uniqueness in not causing retinoid reactions. However, we must delve deeper into why this is the case. This compound may bypass the traditional gateways of retinoid receptors. Nonetheless, what truly matters is still the amount of Vitamin A (in IU) present in the product rather than the specific molecule. It is important to note that claims are generated on the effectiveness of certain forms of vitamin A based on marketing strategies and not with any scientific evidence. It would be a good start to use the correct terms of measurement. Vitamins are not measured in percentages.
A few years ago, a prominent dermatologic researcher in America wrote an article on vitamin A, claiming that only retinol and retinoic acid would produce changes in the skin and that, at best, vitamin A esters ( retinyl palmitate), in particular, are antioxidants. This article was published in a journal that was brought to my attention while visiting a dermatology practice in Washington State. I promptly forwarded the article to Prof. Des and his esteemed colleagues, whom I consider the world experts on vitamin A. The refutation sent to the author and journal is below.
Dear Editor,
All molecular forms of vitamin A, apart from the acid group, are substrates for providing the active acid forms of vitamin A (ligands), which are active on the nuclear vitamin A receptor groups.
None of the substrate molecules, such as retinol, retinyl palmitate, retinyl acetate, or retinaldehyde, have direct retinoid receptor activity.
All vitamin A molecules are equipotent simply because all have common biochemical pathways to the vitamin A acid forms. ( Retinoic acids)
It is misleading to state or imply that one form is more effective.
Of course, they occupy different places in vitamin A's life in human tissue, but they are interchanged systematically to meet cellular demands.
In these pathways, retinol occupies a pivotal position on the way to the irreversible retinaldehyde, retinoic acid, and catabolism via cytochrome P450 in the liver.
Efficacy and potency, molecule for molecule, are the same for all. A single retinol molecule or any storage form can only be turned into a single retinoic acid molecule. As all get formed into retinol before becoming the retinaldehyde, they are equal in effect.
Various forms of vitamin A more easily penetrate the skin than others. In addition, their tendency for irritation and anti-oxidant potential may differ, but never in efficacy as vitamin A.
The science of vitamin A biochemistry in skin is well established. Unless there are new groundbreaking developments to contradict conventional wisdom regarding retinoid nuclear receptors and their complex and varied behavior, I fear the facts presented in the first part of the Q&A are in error or, at best, misleading.
Vitamin A in skincare is a complex subject. The information has been made accessible through a book written by one of the great international experts on vitamin A, Professor Des Fernandes of Cape Town. The book is written for all readers and may be obtained from the publisher at www.fernro.com
Yours sincerely,
Dr Ernst Eiselen
Perth, Western Australia
References
1. Retinoids - A clinician’s Guide - Martin Dunitz - Second Edition 1998
2. Vitamin A - Skin Science Fernro Publishing - First Edition 2015
3. Retinoids: From Basic Science to Clinical Applications - Birkhäuser Molecular and Cell Biology Updates 1994
www.skinscienceauthority.com
Another example of this misinformation (disinformation) in the skincare world came in an email to Prof. Des about a leading Dutch dermatologist who warned about the dangers of using ethyl hexyl methoxycinnamate (EHM) in topical formulations. If more education is unavailable, this misinformation will create a recurrent problem for many valuable ingredients.
One of the most important questions to ask when questioning the safety of any chemical is to know at what dose (concentration) one is using it. Yes, Ethyl hexyl methoxycinnamate can be a hormone disruptor at an inappropriate dose. The individual who did the research in 1999 caused an enormous problem in Europe. Subsequently, Denmark banned all sunscreens containing EHM until actual scientists did a scientific analysis of EHM.
Extrapolating from the research, the ethyl hexyl methoxycinnamate dose for an adult human by mouth would be impossible to eat. You would need to consume a room full of this chemical every month to do potential harm. This is the only way; however, you will be able to detect the hormone disruption that frightens people. At lower doses, it does not work. At doses that your skin gets exposed to in an average sunscreen, in a lifetime of use, you would not absorb the EHM that the lab rats were forced to eat in the trial. From a hormone disruption safety point of view, EHM is unquestionably safe.
It is worth noting that various scientific committees severely reprimanded the person who raised all this nonsense about EHM. Aren’t more pressing public safety concerns, such as the soaring rates of skin cancer, more deserving of our attention?
Ethyl hexyl methoxycinnamate is sometimes used in formulations not as an SPF to protect your skin but instead to protect the product's light-sensitive molecules. This ensures a good shelf life and optimum levels of the active ingredient.
One important thing to remember is that EHM does not block blue light. Protecting skin from blue light is one of the most essential things a skincare regime should do, especially for those battling pigmentation. Blue light is pervasive and almost unavoidable. I ensure that my computer screen blocks as much blue light as possible and use high doses of vitamins A & C and other protective ingredients daily.
The key is knowing the scientific details of the ingredient dosage to determine the safety of any chemical. This is why anyone making a claim about an ingredient needs to check with chemists and qualified experts. This is not a new concept; Paracelsus, who lived about 500 years ago, was an early “chemist” who said: “All things are poison, and nothing is without poison. Solely the dose determines that a thing is not a poison.” Prof. Des adds, “The dose makes the poison.”