Hope in a Jar — Cosmeceutical Science : Fact or Fiction – Part 1

Down the way from my office in Beverly Hills sits a stately Neiman Marcus store. As the double doors to the first floor open before me; I am inundated by the sights, sounds and smells of the cosmetic counter. What they offer is simple: promises of eternal youth and beauty. Each counter is manned by an army of young men and women dressed in long white lab coats. One wonders what medical training they must have to go through to don such spiffy uniforms. As a customer approaches a counter they are greeted by these so-called medical experts who are eager to explain how their concoctions and potions promise to repair your DNA, RNA, and all other portions of your body. I wonder if I could use some of these things to repair my automobile?

If Ponce De Leon knew of these miles of aisles of miracles he could have saved a lot of time by hopping a plane from Madrid to LA. If that is not enough; a lot of these potions are emblazoned by the names of Doctor’s who inhabit the pages of woman’s beauty magazines. Do these Physicians have large bubbling cauldrons where they brew their liquids with the help of their faithful assistant Igor in some distant part of Transylvania? Then late at night and on places like QVC and the Home Shopping Network we find another group: celebrities, sports heroes, physicians and an occasional unknown offer monthly supplies of the latest discovery of the fountain of youth fluid, cream, capsule or drink that you positively cannot live without…. at last we have the brew that is true!

Açaí berry

Presently the rage centers on the purple açaí berry that hangs from towering trees deep inside the rainforests of Central and South America. It has found its way into a myriad of foods and anti-aging creams. While this berry contains super high levels of antioxidants; its ability to return a youthful glow to the skin remains unsubstantiated. Open up any Sunday paper supplement, health or women’s magazine and you’ll be inundated with headlines like “Lose weight with Hollywood celebrities favorite diet secret!” or “Eat nature’s superfood!” Oprah Winfrey, who has information on her Web site about açaí attributed to Drs. Nicholas Perricone Mehmet Oz, is so concerned that her name has been misused to promote açaí products across the Internet that a disclaimer was added to her Web site. Still, the information remains on her site there while there is no proven benefit of rubbing this berry on your skin or eating it. In 2008 alone there were over 50 new açaí products introduced in the United States.

But is there a way to tell reality from the next ‘Emperor’s new berry’? Indeed there is, but it will take a bit of your time for me to explain. Let me start out by stating that there are no miracle lotions, food or ointments to restore your skin to that of a newborn. However, there are a few products that do some good things; a lot that do nothing and some that do more harm then good. Rather than sell you a line of 16 agents for a second mortgage on your house; you first should understand basic skin care.

Skin care can be summed up by 3 steps; minimal cleansing; moisturizing as needed and photoprotection (avoiding sun damage.) Once the basics are covered should one then consider: agents that supposedly repair damaged skin; start a regimen of antioxidants that protect your genetic material or consider the use of decorative agents.

Dermatology for the cosmetic consumer

To understand how agents work we must first understand the structure of the stratum corneum also known as the outer layer of the skin. This is simply a group of dead cells which are called corneocytes that are embedded in lipids or oils. An easy way to think of these cells is to imagine them as “bricks” held together by the lipids or oils.

The dead cells contain a low molecular weight mix called the Natural Moisturizing Factor or NMF. The NMF is a mix of various agents such as lactic acid which is the body’s own alpha hydroxy acid, urea that the sweat glands produce and amino acids. It is this NMF that holds water in the skin. Finally these cells are surrounded by a mortar that contains fats or oils. These oils have one end that loves water and one end that hates water but loves oil. The water loving end helps keep water in the skin and the other end holds this mortar together. The oils are made of 1) cholesterol, 2) fatty acids and 3) ceramides which are lipid molecules that form the basic structure of the top layer of skin.

When 1, 2, and 3 are thrown together they spontaneously form alternating layers due to the water loving and hating regions. These lipid bi-layers form the water-barrier of the skin and also control the movement of water (Trans Epidermal Water Loss = TEWL) and form a seal around the dead cells locking in their NMF. That is why when you are on cholesterol lowering agents it lowers the cholesterol in your skin and with less lipids to hold water in your skin your skin can become dry. Folks with asthma, hayfever and the like lack a normal NMF and tend to get dry skin.

The stratum corneum is topped by an acid mantle which is a very fine, slightly acidic film on the surface of the skin acting as a barrier to bacteria, viruses and other potential contaminants that might penetrate the skin.

Another thing to remember is the fewer agents we use on our skin the better. Albert Kligman my teacher from Penn and the brightest dermatologist next to me, of course (only kidding) did a study on Japanese women; who are known to have sensitive skin. The study found that these women used on average 8 different products on their skin. (For comparison US women use about one product.) When the number of products the Japanese women used was reduced to one there skin was no longer sensitive.

Cleansers (with and without active agents)

Basic hygiene dictates that it is necessary to remove make-up, environmental dirt, skin secretions and microorganisms that cause odor and disease. However of all things we do to the skin, cleansing it is overdone. Cleansers damage the skin by disturbing the mechanism by which the outer protective layer of the skin retains moisture. UV exposure, soaps, detergents, water exposure all increase water loss and decrease moisturization of the stratum corneum and all of us have seen what happens to brick walls where the mortar has been compromised; they don’t stand up for too long. Ideally the moisture of the skin should be 10%. So it is the presence of water in the skin that creates moist skin. Oil on the skin does not penetrate and soaking in a tub of water does not penetrate the skin. We all know after soaking how prunish our fingers become.

Soaps are alkaline and can irritate the acid mantle of the skin. The acid mantle, as stated before is a very fine, slightly acidic film on the surface of the skin acting as a barrier to bacteria, viruses and other potential contaminants that might penetrate the skin. The pH of the skin is acidic. These contaminants and other chemicals are primarily alkaline in nature and the skin’s moderate acidity helps to neutralize their chemical effects. So to prevent the irritancy of alkaline soaps alternative cleansing agents were created. Syndets or synthetic cleansing bars like Dove, Aveeno or liquid cleansers like Oil of Olay are the best to use for cleansing. Remember if you really used a shampoo that cleaned your hair it would look like a straw broom, so we want to use mild cleansing agents especially on your face so as not to irritate it. Liquid cleansers like Cetaphil are gentle and they clean without fats (i.e. soap.) Cetaphil has sodium laurel sulfate and propylene glycol which can irritate some skins. These agents are not found in Aquanil. Both are great cleansers. At times an agent with a low concentration of an agent like Benzyl peroxide can be added to a cleanser as is found in the Proactive brand cleansing products to treat acne.

Toners were designed to remove soap film but if you are not using soap to cleanse with who needs a toner? Abrasive scrubbers and exfoliants are best for cleaning the floor and can actually harm the skin. Beads, walnut husks, brushes, and rough sponges all belong in the trash and not on your face.

Moisturization

The Purpose of moisturization is to keep the brick and mortar layer supple and flexible. It also increases desquamation (exfoliation) so visible flakes are not seen or felt. Optimal moisturization allows a more effective degradation of the thin fibers that hold the oldest top layer dead cells to the rest of the stratum corneum.

While moisturizers may contain a sunscreen to protect the skin it is better to select your sunscreen independently. Moisturizers frequently contain humectants which draw water into the skin but be careful because with low humidity they can cause water loss. Some products claim to be a Hydrophilic blanket containing agents like hyaluronic acid etc to provide a blanket against water loss. Often times they contain a botanical (aloe vera) or collagen to impart smoothness to the skin. Newer moisturizers exist with liposomes. These are ultra small bodies that are able to carry with them enclosed substances into the dermis and to the individual cells.

The ability of phospholipids to act as the carrier sphere’s that are capable of transporting active ingredients directly to the cell (liposomes) has extensive implications for cosmetics and has started a revolution in drug delivery. By themselves they are absolutely non-toxic and cause no skin irritations, not even around the eyes. Their small size enables them to pass through the skin. The development of liposome technology offers the potential for many beneficial cosmetic and medical products. There is a theoretical danger, however, in their ability to carry toxic or contaminated substances into the cells.

Pharmaceutical companies need to plan very carefully the selection of raw materials and the question of the biological fate of the preparation. The microspheres themselves are constantly undergoing changes due to thermal activity during preparation and storage. As a result, each ingredient of the preparation can end up inside the microspheres over time. Many cosmetic products contain toxic substances that if used in liposome products will eventually become part of the inclusion inside liposomes. Those toxic substances, in turn, will get inside your skin cells. Therefore you must be wary of products with liposomes that also contain certain preservatives which fall into this hazardous category.

Cosmeceuticals

Cosmeceuticals was a term coined by Albert Kligman in 1980. The term describes the marriage of cosmetics and pharmaceuticals. They exist somewhere between the continuum of drugs and cosmetics. A cosmetic does not effect the structure and function of the skin while a drug does. One note to make is that the area of cosmeceuticals; not all products may be regulated by the FDA. This may confuse consumers since the term is used regularly by cosmetic companies to imply that the product has been “approved.” Cosmeceuticals implies a mild degree of pharmacological action not only at the level of the stratum corneum but also suggests action at the level of the epidermis as well as the dermis. Examples of Cosmeceuticals are:

Retinoids

Retinoids were developed in Europe but most of the work on acne and photo aging was performed by Albert Kligman at the University Of Pennsylvania School Of Medicine’s Durhing labs. Trenitoin (Retin-A) has been studied for over 37 years. It is the prototype agent of all Cosmeceuticals. However unlike almost all the other products it has a supporting evidence-based medical background that is not seen with any other agent. Besides its efficacy in acne it also improves pigments, very fine wrinkles, dryness and erythema. Retinoids have the ability to repair Atypical DNA. It is also used to repair non-photo damaged skin and pure age related changes. Retinoids can irritate so consumers must ease into their use by staggering use over the first week then increasing use on the second to build up to every day use by the third week.

While some like to apply it like toothpaste the secret is to use a small amount and can be mixed with hydrocortisone. Apply it all over your face. My personal preference that I prescribe to my patients are:

A)Tretinoin (Retin-A) (Renova)
B)Adalapene (Differin) (less irritating)
C)Tazarotene (Tazorac) (more irritating-always dilute and use 0.05 concentration)

Having used retinoids in clinical practice for 38 years there is nothing that comes close in the area of cosmeceuticals. The uses of retinoids require a committed regimen by the patient. Many products these days contain Vitamin A. This Vitamin A is Retinol which is the alcohol form of Vitamin A. It is a precursor of Retinoic acid and conversion occurs in the skin. Some feel irritation is necessary for indication that the product is effective. It is 10 times less potent than Retinoic acid and is an unstable molecule that can be destroyed by light and oxygen. A good example of a product like this is Retinol SA from the Ageless Intensive Line by Neutrogena. Its concentration of retinol is high enough to be effective (i.e. converted to retinoic acid.) The issue I have with the Neutrogena product is that there are all these weird add add-ons that come with the product such as the facial vibrator and cleansing pads one is suppose to use. Why? Buying a new cream becomes tantamount to buying a new car. Why they can’t simply sell the cream?

Alpha Hydroxy Acids

Alpha Hydroxy Acids (AHA) AHAs were first used by Cleopatra. There is literature supporting their efficacy but it is not anywhere close to that associated with retinoids. Furthermore, one should not use at them at the same time as Retinoids. One can be used in the am and one in pm. While they create certain degree of photosensitivity; irritation is less than that associated with retinoids. In studies 8% lactic acid improved thickness, pigment, sallowness and roughness of the skin but the changes seen with the retinoids are not observed. Glycolic is the best known member of this class. It is produced by many companies.

Beta Hydroxy Acid

Beta Hydroxy Acid The old standby salacylic acid. This seems to have been used forever in dermatology. Evidence presented stating it “improves” the global skin’s appearance. Honestly this is not really a Beta-Hydroxy acid because it has a Benzene ring. This is what has been used on corns and plantar warts for years, yet it has been renamed to this class because of the popularity of the AHA’s.

Vitamin C

Numerous skin preparations exist that contain Vitamin C but one must realize that the skin does not have Vitamin C receptors. These products are very common but they are far more hope than actual help.

Vitamin C in solution is unstable and no data exists that shows the active agent is absorbed. Patients tend to like Vitamin C products in that they produce redness of the skin. One study showed an improvement in fine wrinkles but true controlled studies currently don’t exist.

Vitamin E

Vitamin E protects membranes of fats or cellular lipids from oxidation. While it reduces potentially damaging free radicals after UV exposure there are no controlled studies to show effects on sun damaged skin or wrinkles. Naturally occurring Alpha- (or α-) tocopherol vitamin E is the only form that is recognized to meet human requirements. Double-blind study on scars evidenced contact dermatitis and worsening of scars in 90% of cases. Futhermore there was a 33% incidence of contact dermatitis. In cosmetics d-alpha-tocopherol acetate and alpha-tocopherol succinate are utilized to decrease contact allergy.

VIitamin K

Topically does not gets rid of leg veins.

Topical efficacy remains in question.

Does not decrease bruising in patients prior to treatment with injectables or laser procedures.

Vitamin K applied topically to the skin has not been shown to be effective.

Matrixyl

Matrixyl (Palmitoyl Pentapeptide-4) is said to stimulate collagen formation to erase wrinkles from within and thicken the skin. The additional component in Matrixyl 3000 (Palmitoyl Tetrapeptide-7) suppresses the body’s production of excess interleukins (like DHEA) preventing even reversing glycation. Glycation is sun damage to collagen with resultant loss of youthful contours and uneven skin tone. So much of the aging is caused by shifting of fat deposits and agents such as DHEA produced by the adrenal gland that it is hard to believe all these claims. While clinical data is encouraging they are no home runs. One study demonstrated that palmitoyl pentapeptide-4 was as effective as retinol in repairing sun-damaged skin but was devoid of side-effects. Most other studies showed at least some improvement in various objective and subjective measures of wrinkles. No side effects have been reported.

Unfortunately, the clinical data is still too skimpy to view palmitoyl pentapeptide-4 as a proven anti-wrinkle treatment at this time. So, should you wait? Or is palmitoyl pentapeptide-4 worth a try today? There is no universal answer to this question. If your skin care budget is tight, you may not want to spend your hard earned cash on “perhaps-effective” products. On the other hand, if you have cash to burn and/or other alternatives didn’t work, palmitoyl pentapeptide-4, with its good safety profile, may be worth a try. Palmitoyl pentapeptide-4 may also be considered as a nonirritating fall back option for people who develop skin irritation in response to retinoids or alpha-hydroxy acids.

If you decide to try palmitoyl pentapeptide-4, keep in mind that its concentration in a product should be sufficiently high (e.g. matching the levels used in the clinical studies). There is a large price variation between different palmitoyl pentapeptide-4 products, although none are dirt-cheap. The price does not always reflect the concentration of the active ingredient. It may reflect prestige of the brand, advertising overhead, sophistication of packaging and so forth. Be wise. Make sure you are paying a fair price per until of the pentapeptide.

Vitamin B5

This vitamin attracts water from the dermis into the epidermis, increasing water content in the epidermis.

When humidity is higher than 70 percent, humectants can also attract water from the atmosphere into the epidermis increasing the pliability and flexibility of the skin, preventing it from cracking. It is simply an elegant moisturizer.

Topical Estrogen (Known as Estradiol)

With 0.3% solution Estradiol modest literature exists. There are comparative studies available; a 6 month open label study comparing 0.01% Estradiol and 0.3% Estradiol. The study showed decreased wrinkling with increased elasticity and firmness yet no or little systemic effect. Recently Murad has released a line called Resurgence with plant-based ingredients, like Soy, Wild Yam and Clover Flower Extracts. Murad claim such ingredients are proven to combat the visible effects of menopause and hormonal skin aging and will result in a notable difference almost immediately. There is no data supporting the ability of the Soy based estrogen products to act like true human hormones.

Fragrance

Fragrance ingredients are the most common cause of allergy in patients who use cosmetics. Very little is known about individuals strategies to manage this issue and the effect it has on their daily lives. Many patients with fragrance allergy succeeded in finding some scented products which they could tolerate by use of ingredient labeling. A significant proportion of allergic consumers continue to have skin problems. Almost half of the patients perceived that fragrance allergy significantly affects their daily lives.

Hypoallergenic

Hypoallergenic is a term coined by advertisers. It was first used in a cosmetics campaign in 1953. It is used to describe items (especially cosmetics) that cause or are claimed to cause fewer allergic reactions. While the term lacks a real medical definition; it is in common usage and found in most standard dictionaries. In some countries, there are allergy interest groups that provide manufacturers with a certification procedure including tests that ensure a product is unlikely to cause an allergic reaction, but products which fail or are not tested are usually described and labeled using other but similar terms. So far, public authorities around the world have not provided an official certification that an item must undergo before being described as hypoallergenic. The cosmetic industry has been trying for years to establish an industry standard for use of the term but mostly it applies to agents without a scent.

Global qualities of any product must address dryness, texture, wrinkles, and pigmentary unevenness. Products or Cosmeceuticals must be elegant and associated with little irritation or have methods of use that make them tolerable. One must also remember a patient’s perception of benefit is often not based on scientific data.

Another factor which dictates good or bad skin is smoking. In short; don’t smoke! In relationship to food research a diet rich in vitamin C and low in fats and carbohydrates may promote younger looking skin. Antioxidants protect cells from the damaging effects of free radicals, which are molecules that contain an unshared electron. Free radicals damage cells and might contribute to the development of skin aging and possibly skin cancer. Unshared electrons are highly energetic and react rapidly with oxygen to form reactive oxygen species (ROS). The skin forms free radicals in response to pollution, and ultraviolet radiation from the sun.

Hopefully this first part of my article has provided you information, given you cause to pause, think and rethink about cosmetics and cosmeceuticals. I will continue with Part Two of this article in the next week or so. If there are topics you would like me to cover please let me know by composing a response to this article.

by Dr. Arnold Klein, Professor of Medicine and Dermatology at UCLA’s David Geffen School of Medicine

January 22, 2010 11:55 PM