In the Zone

Imagine that you are a manufacturer selling amazing widgets. Your soon-to-launch hero SKU has major buzz. Celebrities are talking about it. Consumers are ordering it in droves. You’ve packed up your widgets, and are ready to hit the marketplace. But the delivery truck never arrives; your products never make it to their intended destination.

The same thing can happen in skin care. A formulation can have all the“right” ingredients, but without an effective delivery system, they’re going nowhere.

“Featured ingredients sit proudly on the label of skin care products, and then often sit frustrated on the surface of the skin,” said Mark Chandler, technical manger, skin care innovation with Croda.

What’s worse, your product is doing nothing for consumers either. And now is hardly the time for a misstep, especially in the upper end of the skin care category, a market that has been slowed by the troubled economy. According to data from The NPD Group, Port Washington, NY, October 2009 marked the 12th straight month that prestige skin care sales in the U.S. fell both in dollars and units.“Today’s market is more demanding for quality, immediate performance that can be seen, and cost-effective products,” noted Sam Shefer, executive vice president of Salvona Technologies Inc.
“And, oh yes, now it has to be based on natural or organic technologies,” added Dan Beio, vice president of R&D with RITA Chemical.

In fact, the steady shift toward natural and organic ingredients has put the spotlight on delivery systems.

Noevir’s Brilliant de Peau is an intensive skin renewal system featuring two serums.

“Many natural ingredients are not stable in a formulation and require the protection and long-term stability that delivery system technologies can provide,” noted Melissa Frischling, director, corporate communications and product support, Lipo Chemicals.

Overall, the role of the delivery system has evolved considerably, say industry insiders.

“We know so much more about skin, its issues, potential remedies and where those remedies have to go within the skin network,” said Beio. “We used to only look at physical stability, now we're using more microscopic and biological models to evaluate base delivery system effectiveness.”

“While in the past delivery systems were mainly used to achieve a sort of unspecified effect in terms of increasing bio-availability or slow release, delivery today means to be much more precise in terms of targeted effects,” added Dirk Teichmüller, president and chief executive officer, Rovi Cosmetics International GmbH.“Today, delivery means not just to bring a cocktail of actives into the deeper skin layers, but to bring certain actives to certain skin cells and to activate clearly specified mechanisms there.”

Murad has developed a new anti-aging acne treatment for adult skin that relies on encapsulation for long-term, sustained release of salicylic acid without irritation.

Natural Selection

Finding the most effective delivery system is a top priority for many formulators.

“If you don’t have a superior delivery system, the ingredients just sit on the cells. For skin to repair, there must be communication between cells,” noted Emilia Karsh, founder of EMK Products, LLC, which recently launched Supra high-performance night cream. The principal ingredient in the cream is a biotechnological herbal placental extract. This bio-identical plant-based extract has the same ability to rejuvenate the skin as human placenta, according to EMK. Karsh calls placental extract a superior delivery system as it helps the other ingredients penetrate. “People want instant results,” Karsh added.

Demand for fast, visible improvement is forcing skin care companies to deliver true benefits, not label buzz.

“If you really want performance, the delivery system is critical,” said David Djerassi, founder of Intrachem Technologies, a marketing and scientific consulting firm specializing in the cosmetic and dietary supplement industries.But, Djerassi quickly added: “Still, with most actives, if the levels are very low, at the end of the day, the results will be minute.”

“In the past, some formulators added botanicals at symbolic levels, but now consumers demand results or they return the product for refund. The technical challenge is how to formulate with effective levels, in stable formulas. This is where a good delivery system becomes very useful,” said Shefer of Salvona, which offers SalSphere, a submicron spheres delivery system used to stabilize and enhance the benefits of super fruits extracts. “The uniqueness of this SalSphere technology is that it not only deposits more, the release can be triggered with external heat, such as from a styling agent. The end result is a cost effective system, which can rejuvenate the appearance of hair and scalp,” he said.

Balancing Act

Potent actives deliver results, but the drive for performance must be matched with care, especially when incorporating materials that are effective, but can also be irritating. For example, alpha and beta hydroxy acids are very effective in treating acne and exfoliating skin, but they also may irritate and dry the skin due to low pH.

“Delivery systems that can release the full dosage of the acid at a low rate are very beneficial. The controlled slow release rate allows the skin to rebalance the pH so that the side effects are minimized,” said Shefer.

Finding a delivery system that balanced performance and gentleness was a goal for Murad as it developed a new acne treatment for adult skin. Unlike teenage acne-prone skin, adult skin faces signs of aging from environmental damage, genetic aging and years of what Murad calls “cultural stress,” the pervasive, cumulative stress of modern living.

For its Anti-Aging Acne Line cleanser and treatment, Murad opted for a liposome delivery system that would deliver salicylic acid in a sustained, long term way.According to Jeff Murad, vice president, product development, encapsulation minimizes the risk of irritation as the ingredient is released over an 8-hour period in the treatment while also allowing the acid in the cleanser to remain on the skin after lathering and rinsing.

“It is step forward,” Murad told Happi. “We have been using encapsulation for antioxidants and inflammatories, but this the first time we have for sustained release of salicylic acid.”

Chemists at Lipo have been focused on producing encapsulates that will release their contents in a sustained manner using pH as the trigger mechanism, a technology used in the pharmaceutical industry.

“Basically we are using enteric polymers to coat different hydrophobic and hydrophilic actives, these encapsulates are then formulated into semi-acid cosmetic formulations as the enteric polymers are stable at pH levels below 5.0,” noted Scott Hawkins, director of business operations, Lipo Technologies. “Upon application, the encapsulates are deposited to the skin, there the pH will generally rise to above a pH of 5.0 and this will allow the enteric polymer to begin to swell and release its contents. At this point, the encapsulate becomes a reservoir, slowly releasing the active material to the skin in a sustained release fashion.”

Multiple Benefits

Marketers must also address other aspects a delivery system can offer to their formulation.

“Delivery systems provide cost-enhanced, cost-effectiveness potential,” said Jon Packer, president of Centerchem, noting that with today’s economic pressure, a delivery system can be valuable tool when it comes to maintaining quality. “If you can either lower concentration and get the similar effect, or use a similar concentration and get an added benefit, the well-chosen, correctly utilized delivery system may offer a less expensive product without sacrificing quality,” Packer said.

Among Centerchem’s offerings are Decorinyl, described as a“mimic” tetrapeptide that is incorporated into a liposomal system for enhanced efficacy and penetration. It compensates for the truncated, human Decorin in aging skin, which causes a loss in elasticity and the binding control of fibrillogenesis, according to Centerchem. Decorinyl interacts with the skin fibrils, restores the spacing of collagen fibrils, and increases skin suppleness and strength.

With consumers looking for multi-benefit products, Salvona offers a technology based on MultiSal, used to formulate a multifunctional skin care lotion from a single product. In the system, lactic acid is first released upon gentle rubbing onto the skin. Shortly after, the system releases an anti-wrinkle peptide, followed by a skin-brightening agent. In addition to this multiple step release, spheres with different diameters modulate the targeting of the functional ingredients to different compartments of the skin for better efficiency, according to the company.

Marketers recognize that consumers are keen on longer-lasting skin care products or those that offer added-value attributes.

“New formulations tailored for‘all-day’ benefits may now include a system to better control the delivery of ingredients such as fragrance, moisturizers and other actives,” said Ben Sales, senior scientist, microencapsulation with ISP. According to Sales, ISP Captivates technology—microcapsulates that range from two microns to 2000 microns in diameter and are made with gelatin and a number of natural and synthetic polymers—will accommodate actives and other ingredients into high load formulations.

Product Forms and Function

From serums to sticks to color products with added benefits, skin care has moved far beyond basic creams and lotions. Looking to deliver intensive repair overnight or under other products, skin care brands are rolling out new serums.

For example, Noevir’s Brilliant de Peau is an intensive skin renewal system designed to help stimulate the skin’s natural repair mechanisms and restore its youthful complexion via two serums. The first, Essence for Rejuvenation, contains AC-11—derived from Cat’s Claw extract—which is known to help promote skin’s natural ability to repair itself. It also contains a combination of marine collagen, hyaluronic acid and amino acid (acetyl-tetrapeptide-9) for superior moisture retention while stimulating the skin to boost its structural support. The second serum, Essence for Brightening, contains 13 ingredients that directly target discolored skin, age spots and promote a brighter complexion. The formulation combines vitamins C and E with botanical extracts including gardenia fruit, rose balsam and bergenia root.

Salvona’s MultiSal technology.

“Finding the right delivery system for Noevir’s high performance cosmeceutical and nutraceutical products is considered critical,” said Fumi Ozaki, project coordinator/licensed esthetician with Noevir U.S.A., Inc.According to Ozaki all of the company’s skin care products begin with natural bases—stearic acid and HS lipids derived from soybeans, jojoba oil, beeswax and squalane.

Beio of RITA suggested formulators use a critical eye when matching delivery technology and product form.For example, liposomes work better in serums where the content of emulsifier and/or surfactant is at an absolute minimum. “However, that makes the challenge of coming up with an effective delivery system that can drive the actives into the skin more difficult, as it’s not easy to penetrate the stratum corneum barrier with non-emulsifiers,” he said.

On the other hand, Beio said a more traditional emulsion system designed to offer penetration opportunities for an active will also open the door for other non-actives to penetrate as well, which could result in irritation.“It’s all a very delicate balance and the final product has to deliver many promises, most important of which, it has to feel good on the consumer,” he said.

Others also pointed to the importance of maintaining aesthetics in skin care products. “Consumers are conscious about how products feel, so whatever we do as suppliers, we don’t want to comprise the texture or feel of a product,” said Maria Tolchinsky, global marketing manager, personal care, for AkzoNobel.

In another nod to feel, RITA offers Ritasil entrapped in Polysilicone-11. These natural oils—including shea butter, sunflower seed, safflower seed, sweet almond and sesame seed—are entrapped in a silicone matrix that protects the materials from potential degradation, yet utilizes the spreading properties of silicone to improve their bio-availability. “The final result,” said Beio, “are natural oils which provide essential skin care/skin lipid replenishment in a great feeling silicone format.”

Yet, as much as consumers expect skin care to feel good, they also want it to fit into their lifestyles. Today’s fast-paced society has changed how and where consumers apply beauty and personal care products.

“The rise of on-the-go products—such as treatment sticks, concentrated and specifically targeted silicone-based serums found in cosmeceutical treatments as well as color cosmetics offering skin care benefits—has brought new challenges for cosmetic manufacturers concerning the incorporation of active ingredients, which are for most of them water-soluble, into such anhydrous formulations,” noted Anne Laurie Rodrigues, communications manager at Laboratoires Sérobiologiques (LS), the active ingredient business of Cognis Care Chemicals.

In order to meet this demand, LS has developed Active Powders, which enable the incorporation of water-soluble actives in anhydrous systems. Active Powders contain up to 70% of hydrophilic particles protected by a hydrophobic polymer, according to LS, and each particle contains up to 63% of an aqueous solution of the active ingredient. Possible applications include lipsticks and lip balms, powder form makeup, hot-poured foundations and silicone-based serums as well as treatment sticks, according go the company.

“This technology allows a controlled release of the active ingredient into the skin by diffusion and enhances the bioavailability of the active. Active Powders technology significantly broadens the range of actives that can be used in anhydrous systems and enables more targeted action and varied claims,” Rodrigues concluded.

Finding the Right Technology

Working closely with savvy suppliers to select a delivery system can help companies overcome challenging formulation issues.

“In order to penetrate healthy, intact skin, a compound must be soluble in the formulation. We therefore put the time and art into developing products that are not only easy to formulate with but also carry a potential to reach their target of action in the skin,” said Nava Dayan, PhD, senior principal scientist, research and development, skin care, Lipo Chemicals, citing Lipobrite HCA-4, an hydroxycinnamic acid (HCA) in PEG-4.“HCA is a compound that is very difficult to solubilize and will not penetrate the skin unless is incorporated into a suitable vehicle. Its incorporation into PEG-4 allows for improved activity,” she said.

At Rovi, marketers can turn to its range of “cellular actives.” Based on multiple carrier system technologies, the range includes Aquafill, an Ecocert and NaTrue compliant skin and pore refiner that uses “moisture trap” technology to reduce wrinkles and refine pores immediately and exhibit excellent long-term effect after a one-time application. The carrier system is designed not to penetrate, but to form an occlusive film on top of the skin. “This means we can conserve the skin's moisture for a period of up to 24 hours after one application which is the foundation of Aquafill's outstanding long-term effects,” according to Teichmüller.

In addition, Rovi offers ProContour, which fights the visible signs of cellulite and can be used in slimming formulations, as well as neck and chest care products. “This time, the crucial point was to deliver the actives as quickly as possible to the target site. Therefore, in ProContour we utilize a specific fast penetrating liposome which accomplishes this task,”Teichmüller added.

“From a delivery standpoint, sometimes being old school can be new technology,” noted Beio. He said RITA’s Pationic acyl lactylates, which are Ecocert approved, are gaining momentum in daily skin care systems as well as specialty treatments as they are extremely mild to the skin and form beautiful white emulsions without the use of ethoxylates.

For emulsions, Centerchem touts Plurilamellar Multivesicular Liposomes (PMLs) containing NA-Hyaluronate (.01%), which have the ability to release ingredients into the epidermis. They can be incorporated into emulsions, demonstrating a superior ability for moisture retention, lubrication and sensory skin-feel, as well as the formation of a viscoelastic film that maintains lubricity and smoothness, the company said.

The Norwalk, CT-based firm also offers Xpertmoist molecular film technology, which prevents and repairs the dryness and damage that results when transepidermal water loss occurs. It is both immediate and long-lasting, according to Centerchem.

Bring It On!

While suppliers were eager to speak about current advancements in delivery systems, they also said research is a key element in building sophisticated technologies that will push skin care formulations further.

“As we acquire more knowledge about the skin as a barrier and ways to overcome it, we are trying to fit the systems developed to the findings,” said Lipo’s Dayan. “For example, it only has been recently demonstrated that the distances between corneocytes in the stratum corneum are of nano-scale; 13nm, divided to 5-3-5nm areas between the sheets of the intercellular lipids. This may dictate the size of systems developed for certain applications,” she concluded.

According to Shefer, research will continue on natural polymers and effective functional ingredients from botanical sources, as well as on the development of potent delivery systems for antioxidants such as ascorbic acid, vitamin C and polyphenols.

Teichmüller said that during 2010, Rovi plans to present cellular actives for new hair and sun care products and will roll out products that explore the area of cell-targeted delivery.

Chandler suggested companies consider emulsifier selection too, as it plays a role in aesthetics, delivery and overall performance. “What is necessary is an integrated approach to formulation development to produce a differentiated, aesthetically pleasing, performing, and delivering skin care formulation,” he said, noting that carrier vehicles in Croda’s Arlasolve range are seeing increasing usage in high-performance, cosmetics and OTC formulations.

In the end, experts Happi spoke with agreed that smart selection of delivery systems and greater knowledge about skin’s function are essential to a product’s aesthetics and efficacy.

“Considering skin barrier function, if you understand the intricacies, you can effectively maintain or improve skin health,” said Packer of Centerchem. “A good delivery system will provide you with more tools and planning so you can build products with the correct structure to work with the skin.”