A Peptide to Influence the Melanogenic Symphony of Skin Pigmentation

Nov 1, 2010 | Contact Author | By: Estelle Loing, PhD, and Isabelle Lacasse, Unipex Innovations
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Title: A Peptide to Influence the Melanogenic Symphony of Skin Pigmentation
skin lighteningx encapsulated oligopeptide-68x microphthalmia-associated transcription factor (MITF)x melanogenesisx constitutive and facultative pigmentationx
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Keywords: skin lightening | encapsulated oligopeptide-68 | microphthalmia-associated transcription factor (MITF) | melanogenesis | constitutive and facultative pigmentation

Abstract: Inspired by the roles of transforming growth factor-β and MITF in skin pigmentation, an active based on oligopeptide-68 was developed to influence these entities. In vitro, oligopeptide-68 is shown to abrogate the stimulatory effects of α-MSH on melanin pigment formation. In addition, clinical results demonstrate the peptide imparts significant and progressive whitening/lightening effects on skin.

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E Loing and I Lacasse, A peptide to influence the melanogenic symphony of skin pigmentation, Cosm & Toil 125(11) 36-44 (Nov 2010)

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Skin pigmentation is a major concern for most humans. It not only provides information about race, age, gender, social status, culture, habits and level of health, but it also is a major determinant of physical attractiveness. Not long ago, tanned skin was the gold standard in the United States for women and men seeking a better, healthier look. However, both physicians and consumers have since learned that exposure to UV radiation to achieve skin tanning can result in a number of negative effects, specifically more wrinkles, the appearance of skin pigmentation, and an increased risk of skin cancer.

Today’s society has experienced the return of a trend for whiter skin. The phenomenon is spreading worldwide, although for different reasons. In Asia, where its citizens are affected early by uneven skin tone, whitening products are popular. These products are used daily by a broad range of consumers to preserve the appearance of healthy skin, especially on the face. In countries such as India, there is strong social pressure for paler skin, which is considered more beautiful. Lightening products are also gaining popularity in the Western world. Caucasian consumers, however, are more concerned with the appearance of age spots on their hands, décolleté and cheeks. This is a different market, mainly composed of older consumers.

The global skin lightening and whitening market is expected to reach US $10 billion by 2015. This demand certainly warrants a better understanding of the skin pigmentation processes, which is described here. Further, it supports the R&D strategy to develop actives that provide skin-whitening effects in personal care products, such as the peptide discussed below.


Lab Practical: Using Encapsulated Oligopeptide-68

  • Encapsulated oligopeptide-68 should be incorporated at the end of the manufacturing process, at a temperature below 40°C.
  • To preserve the liposome integrity, it is better to work at low temperature (< 50°C) with a pH 4–8.
  • Surfactants capable of solubilizing phospholipids should be avoided.
  • Alcohol should be used carefully (10% max.) in the formula.
  • Salts affect liposome stability and should be avoided.
  • Liposomes should be introduced into emulsions or soft creams with minimal mixing, preferably at the last step.

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Table 1. Skin-lightening agents and their various modes of action

Table 1. Skin-lightening agents and their various modes of action

Given the complexity of the pigmentation process, it seems appropriate to target multiple mechanisms to lighten or whiten skin since inhibiting a single performer would not be sufficient for a noticeable decrescendo of the music. Such a strategy would obviously involve various materials and address several processes; some of which are listed here.

Figure 1. Pathways in the control of skin pigmentation

Figure 1. Pathways in the control of skin pigmentation

Convergence of the facultative (MC1-R) and the constitutive (TGF-ß1) pathways at MITF level in the control of skin pigmentation

Figure 2. Western Blot analysis

Figure 2. Western Blot analysis

Western Blot analysis of B16F10 cells treated with 0.1 µg/mL oligopeptide-68

Figure 3. RT PCR analysis

Figure 3. RT PCR analysis

RT PCR analysis of F10 cells treated with encapsulated oligopeptide-68

Figure 4. Oligopeptide-68 dose-dependently decreases melanin synthesis in melanocytes.

Figure 4. Oligopeptide-68 dose-dependently decreases melanin synthesis in melanocytes.

As expected, α-MSH treatment of the melanocytes resulted in increased melanin deposition, as shown here.

Figure 5. Dermatologist evaluation

Figure 5. Dermatologist evaluation

Dermatologist evaluation of the skin-lightening effect of encapsulated oligopeptide-68

Figure 6. Encapsulated oligopeptide-68 reduced the appearance of pigmented spots.

Figure 6. Encapsulated oligopeptide-68 reduced the appearance of pigmented spots.

Before-and-after photograph of a volunteer from the described study; the green arrow points to a hyperpigmented area that was monitored throughout the study. At day 56 of treatment with encapsulated oligopeptide-68, a noticeable reduction in the contour and color of the selected spots was observed for this volunteer.

Footnotes [Loing 125(11)]

a β-White (INCI: Water (aqua) (and) Butylene Glycol (and) Hydrogenated Lecithin (and) Sodium Oleate (and) Oligopeptide-68 (and) Disodium EDTA) is a product of Unipex Innovations, Québec, Canada.

Formula 1. Brightening serum

Water (aqua) qs to 100.00% (w/w)
Butylene glycol 12.00
Triethylhexanoin 6.00
Cetyl ethylhexanoate 4.00
Glycerin 3.00
Glyceryl stearate (and) PEG-100 stearate 1.50
Glyceryl stearate 1.20
Stearic acid  1.00
Hydrogenated polydecene 0.60
Cetearyl alcohol 0.50
Microcrystalline wax  0.50
Polysorbate 60 0.50
Dimethicone  0.40
Sorbitan olivate  0.30
Methylparaben  0.20
Arginine 0.12
Carbomer 0.12
Ethylparaben  0.10
Butylparaben  0.10
Fragrance (parfum 0.08
Propylparaben  0.05
Glycine soja (soybean) oil  0.05
Hydrogenated lecithin 0.05
Butylated hydroxyl toluene 0.02
Oligopeptide-68 0.005

 

 

            

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