Sophisticated cosmetic ingredients: even the most demanding consumers can find effective anti-aging cosmetics, thanks to a wide array of novel active materials.

MOST COMPANIES understand the concept of selling benefits. Through the years, products in the marketplace focused primarily on characteristics that identified them on the basis of features and functions. Consumers are now demanding product satisfaction via the delivery of intended performance attributes and desired benefits that add value to their life. Crafty product claims backed by sloppy claim support may still attract initial purchase for the sake of trial for a new product. But longevity in the marketplace still depends on consumer-perceived overall satisfaction with that new product. Nowadays, it is hard for established companies to compete only on the basis of a successful recognized brand. The brands need a constant boost with innovative products that deliver benefits.

There is more pressure on suppliers to develop active ingredients and raw materials that help marketers create skin care products that mimic the effects of aggressive skin treatments such as botox and dermabrasion. In recent years, actives such as palmitoyl oligopeptide, palmitoyl tetrapeptide-3 and acetyl hexapeptide-3 are added to a new generation of personal care products which has industry observers asking themselves: "Is it a cosmetic or a drug?"

This year, the Food and Drug Administration (FDA) reviewed labels and websites of anti-aging products and issued warning letters to some marketers after the agency determined that their products are promoted with claims that cause the products to be drugs under section 201 (g)(1)(C) of the Federal Food, Drug, and Cosmetic Act (the Act) (21 U.S.C. 321(g)(1)(C)).

As skin care products edge closer to making dermatological claims, the FDA is turning a more critical eye on the skin care market. Luckily the CTFA strives to keep options open for cosmetic formulators and raw material suppliers by preparing legal memorandum responses to Federal Register notices. There is now a complex balancing act between satisfying the consumers demand for perceived product benefits and avoiding FDA's ire.

Performance-driven Ingredients

Nanolipo-hGH from Regeron, a Korean company that focuses on "reverse-aging biotechnology," is billed as the world's first cosmetic human growth hormone. This raw material is a bioactive hGH stabilized in nano-sized liposomes for ready use in cosmetic formulations. The liposomes facilitate skin permeation of hGh and enhance effects of keratolytic treatments due to hGH. The company also markets nanolipo-hGH Retinol Plus for enhanced anti-wrinkle treatment with minimal irritation. (1)

Adhesives Research, Inc. manufactures custom-coated products, specialty films, pressure-sensitive adhesives (PSAs) and laminates for transdermal drug delivery applications for the pharmaceutical industry. The company has developed unique multi-functional patches and hybrid systems for the targeted delivery of therapeutic skin agents and cosmetic ingredients. Adhesives Research can formulate dissolvable films and multi-functional patches with precise functional properties, including film thickness, loading level, tensile strength and dissolution rate. Key ingredients can be incorporated into a dissolvable film that provides localized delivery through topical or oral delivery methods. These films offer many of the same benefits of traditional delivery methods, such as targeted delivery and controlled ingredient releases, while providing the added advantages of customizable properties for localized topical delivery, portability and ease of use.

I-Spheres is a patent-pending delivery system that is said to improve penetration and transportation of actives. It consists of aqueous suspensions of spherical 50-500nm thermostable nanoparticles which can be loaded with customized lipophilic actives, allowing for controlled release of the encapsulated ingredients. The degree of release can be adjusted through the types of waxes in the system. This technology is available from New Paradigm Technologies, a division of Tri-K industries.

Stableact, a new polyol-in-silicone multi-phase emulsion system system is also available from New Paradigm. This system can be added directly to an already formed oil-in-water emulsion at 35-40[degrees]C. A three-phase system can then be created in which the labile soluble active is located in the polyol phase and remains protected from the aqueous phase by the surrounding silicone region.

Matrix metalloproteases are naturally-occurring zinc dependent endopeptidases which catalyze the breakdown of connective tissue or extracellular matrix by hydrolyzing various components of the tissue matrix. New matrix metalloprotease inhibitors are available from Bioderm Research. They inhibit tyrosinase production, enhance wound healing, control body odor and clarify acne-prone skin. Resacetophenone is a tyrosine active-site deactivator that provides skin brightening properties. (2)

The cost and effectiveness of preservation systems has always been an issue with product formulators. Dermosoft Octiol (INCI: Caprylyl Glycol) is a multifunctional additive that regulates viscosity and improves wetting. Its compatibility with many cosmetic ingredients and its pH-independent broad efficacy against germs allow for the use in tenside products and emulsions. The addition of 0.3% Dermasoft Octiol shows remarkable improvement of the antimicrobial activity of traditional preservatives. Including this multifunctional additive in the cosmetic formulation should permit the reduction of commonly used preservatives with less irritation. The U.S. representative is Kinetik Technologies, Inc., Hazlet, NJ.

Salvona is developing and manufacturing nanotechnology and patented delivery systems including microspheres, nanospheres and complex systems to provide specific performance features. They deliver a wide array of functional and active ingredients to enhance product efficacy and cost effectiveness. NanoSal is distinct from other microspheres, nanospheres, nano-capsules or lipospheres. The active is uniformly dispersed in a customized blend of a solid polymeric matrix system with a 50% payload. The matrix retains the active, preventing pre-mature release. The system is said to be more stable than liposomes. The surface of these sub-micron spheres can be made cationic or bioadhesive to adhere to human endothelium cells or to hair. This technology provides stable deposition and slow release of various anti-aging actives. MultiSal is a free-flowing powder with high concentrations of functional ingredients encapsulated in nanospheres. Hydrosal technology is a recent controlled-release encapsulation system from Salvona that allows encapsulation of various functional ingredients at very high payloads. It can be incorporated in water, alcohol and hydro-alcoholic products. It consists of nanospheres that are coated with a polymeric layer. (3)

Nanoemulsions are becoming increasingly popular as potential vehicles for the controlled delivery of cosmetics and for the optimized dispersion of active ingredients in skin layers. The traditional method of preparing nanoemulsions using high pressure homogenization requires high energy with limited practical applications. The block co-polymer nonionic emulsifier PPG-20 tocophereth-50 was found to produce stable nanoemulsions of mean droplet diameters ranging from 204 to 499 nm. The emulsification method of high-speed stirring at the theta-point using PPG-20 tocophereth-50 was found to be very effective for the preparation of stable nanoemulsions useful for applications in skin care cosmetics, cosmeceuticals and drugs. (4)

Vitabrid-C is a stabilized form of vitamin C. The material was developed by Nanohybrid Inc. and is marketed by Colorado Synthetics Inc. Vitabrid-C is a hybridized form of L-Ascorbic acid with bio-compatible inorganic material on a nanometer level. It delivers controlled release of the encapsulated vitamin C from biocompatible inorganic matrix. IAA-Brid is a nanohybrid of indole-3-acetic acid. IAA is a plant growth hormone widely present in plants and which is introduced as an anti-wrinkle agent supposed to be more effective and less irritating than retinol. Both products use nanoencapsulation to provide controlled release and protection from oxygen, light and moisture.

Ivrea Laboratories, Inc. is devoted to the development and production of unique cell and drug delivery systems for aged, damaged or diseased human tissue. The company has developed a delivery system that increases the stability and decreases the irritation of selected cosmeceutical ingredients such as retinol. According to Ivrea, nanoparticles can be "hot spots" on the skin which cause irritation. To reduce these hot spots, Ivrea entraps nanoparticles in a chitosan bipolymer (Chitospheres) to avoid direct contact with the skin and for optimal delivery to the skin layers. Chitosan is a glycosaminoglycan with a high affinity for lipids and hydrophobic molecules that results in active complexation and stability enhancement. Chitosan has humectant properties and significant bioadhesiveness to epithelial cells which leads to a controlled release of the active. (5)

Improving Hair Health

Skin remodeling copper peptides (SRCP) are the latest candidate being tested for the improvement of hair health. While the search for methods to restore healthy, younger hair is ancient, the reality is that, even today, in the era of minoxidil (Rogaine) and finasteride (Propecia), all existing therapies provide, at best, a marginal restoration of hair health. SRCPs are based on a human copper peptide complex called glycyl-l-histidyl-l-lysine:copper (II) (GHK-Cu). GHK-Cu is a normal component of human blood plasma, urine, and saliva. (1) It is a key ingredient in anti-aging products. SRCPs have actions similar to GHK-Cu, including anti inflammatory effects, skin repair actions and the ability to increase the size of hair follicles. It should be emphasized that not all copper-peptides have such positive actions; indeed, some copper-peptides can inhibit these effects. (6)

Back to Nature

In the early nineteenth century, the pharmaceutical industry did not exist and there were no man-made medicines for treating skin disorders; instead, people turned to nature. This is true even today when we have such a variety of skin care products available to us, which claim to have the latest discovery in creating a flawless complexion.

Safflower oil triglycerides form the basis of a natural approach to cosmetic emulsification in Lonza's patented DermaSphere technology with Safflower Oleosomes--Natrulon OSF. Oleosomes are their own emulsifiers. The material has a hydrophilic outer shell made of protein, a phospholipid layer and a hydrophobic core. Natrulon OSF is isolated naturally as 75% O/W emulsion and can emulsify other oil phase ingredients. This is one material which does the job of an emulsifier, emollient and moisturizer. (7)

Eclaline, developed by Silab Research, France, is an active ingredient rich in lipophilized Lupine peptides. This ingredient is recommended for use in cosmetic products to improve radiance. The activity is due to stimulation of vascular epidermal growth factor that oxygenates and nourishes the skin making it less dull, more uniform and radiant. Eclaline has an effect on skin microcirculation, cutaneous cellular activity and oxygenation.

Bacopa (Bacopa monniera) is found throughout India and Pakistan. It is an Ayurvedic herb used in rasayana formulas for improved brain function. Studies have shown that it has powerful antioxidant free radical scavenging capacity and protects DNA. (8) The herb contains the alkaloids brahmine, hersaponin, monnieren, bacoside A and bacoside B. The other phytochemicals, betulinic acid, wogonin and oroxindin, are isolated from the aerial parts of Bacopa monniera and showed significant antifungal activity. The cell membrane lipid protective properties of bacocalmine at 0.5% concentration was demonstrated by a decrease of the quantity of 4-hydroxynonenal and malonaldehyde formed due to lipid peroxidation with UVA radiation. Bacoside was also shown to have anti-irritation properties. (9)

Acmella oleracea (Paracress) plant extract from Gattefosse is rich in isobutylamides, unsaturated alkamide Spilanthol and nonvolatile sesquiterpenoids. This natural extract is being considered for use in anti-aging products as a safe alternative to Botox. It is a powerful topical active with muscle relaxing activity and is useful in smoothing fine lines and wrinkles. The extract has applications in facial skin care products such as emulsions, microemulsions, serums and gels.

Consumers have become more sophisticated and more informed about various cosmetics and toiletries. They are always searching for products that give more value for money and deliver benefits. Today, many suppliers are delivering effective ingredients that exceed even the most sophisticated consumer's expectations.

References

(1.) Human Growth Hormone (hGH). Product brochure: Regeron--Reverse-Aging Biotechnology, Kangwon-Do, South Korea.

(2.) Gupta, S., Bioderm Research. New Matrix Metalloprotease (MMP) inhibitors and their application in cosmetic and OTC drug formulations, PCITX Conference, New York, NY, April 26, 2005

(3.) Shefer, S., Salvona Technologies Inc., Nanotechnology for skin care. PCITX Conference, New York, NY, April 26, 2005.

(4.) Kim, Y., Kim, J., Cho, I., Kim, K.; A novel nanoemulsification method of stirring at the point with the tocopherol-based block co-polymer nonionic emulsifier PPG-20 Tocophereth-50. International Journal of Cosmetic Science, April 2005, Vol. 27, No. 2, pp. 144-144(1).

(5.) Cuttaneo, M., Ivrea Laboratories Inc. Chitosphere Topical Delivery System. PCITX conference, New York, NY, April 2005.

(6.) Pickart, L., Dr. Straetmans Chemische Produkte GmbH. Improving hair growth with skin remodeling copper peptides. Cosmetics & Medicine (Russia) July 2004.

(7.) Guth, J., Lonza Inc. Oleosomes: The natural way to formulate. PCITX Conference, New York, NY, April 26, 2005.

(8.) Russo, A., Izzo, A., Borrelli, F., Renis,M., Vanella,A., Free radical scavenging capacity and protective effect of Bacopa monniera L. on DNA damage. Department of Biochemistry, Medical Chemistry and Molecular Biology, University of Catania, V.le A. Doria 6, 95125, Catania, Italy

(9.) Chamberlin, C., Mondon, P., Lamy, F., Peschard, O., Litner, K. Sederma Sensitive skin, a cosmetic approach. PCITX Conference, New York, NY, April 26-27, 2005.

VISPI KANGA was a principal global technology manager at Unilever and has over 25 years of experience in product development in skin care formulation, project planning, supplier networking and development of skin care products from concept to commercial production. He is founder of Cosmet-Pharm Consultants, LLC, a Cresskill, NJ-based firm dedicated to the needs of the cosmetic, personal care and OTC topical drug products industry both domestically and globally. Cosmet-Pharm provides technical knowledge, customized training and knowledge management through on-site training seminars, presentations and product related short courses. It also provides services in product development, technology assessment, cost savings and supply chain issues. More info: [e-mail] or Tel: [phone].