Vitamin A was first tested in the 1940’s for use in treating acne, but early testing found it to be too irritating. While testing of Vitamin A for acne and a range of other skin conditions continued (and continues to this day) its potential to irritate hampered its usefulness.
So how did a promising yet flawed ingredient go from being too irritating to use, to today’s frontline ingredient recommended for use in anti-ageing, acne, and (pustular) Rosacea!?
It all started as an acne medication
It all started with Albert Kligman, who is often referred to as the father of modern dermatology. He set out to find a concentration and formulation of Retinoic Acid (a.k.a. Tretinoin – a form of Vitamin A) for the treatment of acne, that could be tolerated. His experiments with Vitamin A (amongst other things) on prisoners at Holmesburg Prison is both the biggest blight on his career but also led to the development of a Retin-A. Licensed by Johnson and Johnson in 1967, Retin-A found an “acceptable” trade-off between irritation and effectiveness of Retinoic Acid and it is still used today under prescription for the treatment of Acne!
…which seemed to reduce skin ageing
Not long after the release of Retin-A, mature users of the medication started (quite excitedly) to report general improvements in their skin including a reduction in wrinkles, roughness and pigmentation. They came in for an acne treatment and ended up looking years younger! Remember that back in the 60’s there were no effective anti-ageing treatments…
These reports prompted Kligman and others to start trials on Retinoic Acid for treatment of premature skin ageing. The success of these new trials resulted in Vitamin A being identified not only as the frontline ingredient for treatment of acne but for skin ageing too. And in 1995, Tretinoin was approved by the FDA as a medication for reducing wrinkles, pigmentation and hyperpigmentation.
But while Kligman’s formulation reduced the irritation of Retinoic Acid, for many it is still too irritating. This led Kligman and others to look for alternate forms of Vitamin A, which were well tolerated and still effective.
Brief interlude: The dietary journey of Vitamin A
Vitamin A is used in our bodies for a number of functions including vision, cell growth and differentiation and plays a critical role in the maintenance of a number of organs including the heart, lungs and kidneys. Its role in cell differentiation and growth is what makes it such an effective ingredient in the skin.
We consume Vitamin A in our diets from a number of sources (eg. liver, sweet potatoes, carrots, cheese, fish and sweet melon). These forms of Vitamin A are converted to Retinol and Retinyl esters which are stored in our bodies.
In order to convert the stored forms of Vitamin A into the two forms of Vitamin A which are actively used in our bodies, Retinyl esters are converted first into Retinol. Retinol is then oxidised into Retinal (used amongst other things in vision) which is then oxidised into Retinoic Acid.
Can we hack the dietary path of Vitamin A to find an effective and gentle form?
Since the 1960’s, researchers have been looking for alternate forms of Vitamin A that would be effective and gentle. Since Retinol is stored in the body and is converted into Retinoic Acid, it was both easily analysed and studied. From the mid 1980’s, when formulation techniques improved to increase its stability it started to be used in commercial products. The problem? The two-stage conversion of Retinol to Retinoic acid means that it needs to be used in concentrations of at least 10 times those of Retinoic acid to get results! And while the irritation of Retinol at these higher concentrations again starts to become an issue, we still just don’t have great evidence for its effectiveness. However, its widespread availability and use in commercial products has seen it becoming ever more popular in recent times.
In the late 1990’s, as the knowledge of the Vitamin A conversion chain became better understood, the ability to synthesize chemicals improved (remember unlike Retinol, Retinal is not stored in the body), and the search for an effective and non-irritating form of Vitamin A continued, trials on Retinal started. Since then, the evidence has shown that due to its efficient conversion to Retinoic Acid and possibly also in part to its own properties, it is the most effective and best tolerated form of Vitamin A. However as things stand, due probably to its expense, difficulty to sourcing and stabilise, it is still very rare to find Retinal in skin care products.
And that’s how…
From a beginning of frustration and irritation, through a validation process which has us squirming in our chairs, to unanticipated user feedback leading to new lines of investigation. Vitamin A first identified as an ingredient of interest in the 1940’s has finally made it to the top of the online skin care ingredient searches. Though while that search term is “Retinol”, we’re predicting that the skin care industry will catch up to the evidence and start searching for “Retinal”.
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Reduce wrinkles, fine lines and hyperpigmentation. Improves skin barrier function. Retinal at 0.1%, Niacinamide 4% and Glycolic Acid 2% for use on thicker, oilier or acne prone skin. Higher concentration of Retinal and Glycolic Acid combine for better results in managing acne.