Lecinol S-10S. Primary Emulsifier for Sensitive Skin Care

Transcription

1 Primary Emulsifier for Sensitive Skin Care Oil-in-Water Lecinol S-10S Plant-derived Soy derived EO-free NIKKO CHEMICALS CO., LTD NIHONBASHI-BAKUROCHO, CHUOKU, TOKYO, , JAPAN TEL: FAX: Active delivery Stabilizer Skin friendly

2 Characteristics of Lecinol S-10S Plant-derived Soy derived INCI Name: HYDROGENATED LECITHIN PC (Phosphatidyl choline) content: 25~35%. Natural derived emulsifier (from soy). Liposome former. Promotes percutaneous absorption of actives. Moisturizing effect. Enhances skin barrier function. Reduces skin irritation. Dispersant for pigments.

3 Characteristics of Lecinol S-10S Plant-derived Soy derived Phosphatidyl choline (PC) is present in Lecinol S-10 at 25~35%. This phospholipid accounts for emulsifying properties of Lecinol S-10. Phosphatidyl choline (PC)

4 Hydrogenated lecithin vs natural lecithin Plant-derived Soy derived Oxidation stability of natural lecithin and hydrogenated lecithin (Lecinol S-10). Hydrogenation makes lecithin very stable against oxidation.

5 Promoting percutaneous absorption of actives: test method Active delivery Test substance g Skin model Receptor layer 32 water Mixer Penetration of an active substance is evaluated by HPLC

6 Promoting percutaneous absorption of actives Active delivery Absorption of IM (% of total recovery) % 1% 17% 4% commercial item Lecinol S-10 ointment epidermis dermis Percutaneous absorption behavior of indomethacin (IM; 1.0%) to the cultured 3D skin model Test sample:1.0% Indomethacin

7 Lecinol S-10 S forms liposomes Makes liposomes Microscopic pictures of Lecinol S-10 generated liposomes

8 Moisturizing effect (in vivo) Cream with Lecinol S-10 (0.8%) and control cream (with ethoxylated surfactant) were applied to 5 human subjects and skin moisture was evaluated by SKICON-200. Lecinol S-10 showed immediate effect on barrier improvement and increase of skin s moisture content. Instant hydration NEW DATA

9 New Data: Stinging Stinging test performed Recently, a lot of cosmetic companies in Japan use the words tested for stinging reaction as a marketing claim on the packages and labels of their products.

10 Stinging reaction to cosmetics Stinging has become a major issue in skin care safety assessment in Asia. The latest reports show that 30% of consumers appear to be sensitive to a stinging irritation from cosmetic products. Unlike irritation, stinging is defined in Japan as a slight sensory reaction of mild skin irritation. It does not involve the typical irritation symptoms, such as inflammation, redness, or pain, but is often described as an uncomfortable sensation or very light itch. In Japan, methylparaben is typically used as a positive control in stinging testing of cosmetics. Stinging test performed

11 Definitions of stinging. 肌に対する感覚的な刺激を評価する試験 sensory reaction of skin 非常に弱い ピリピリ ヒリヒリといった刺激感の有無を確認するテスト very light reaction, slight itching itching, uncomfortable feeling. The evaluation uses panelists who are known to show stinging reaction to certain compounds かゆみ ヒリツキ チクチク感などの目には見えない感覚的な刺激の有無を評価する試験です この試験は 一定基準で選別された感覚刺激に対して過敏な人を対象に行います

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13 Explanation of the stinging evaluation (from Shiseido website)

14 From the website of Kao Stinging test Stinging test

15 Recent surveys shows that cosmetic consumers who believe to have a sensitive skin tend to increase year by year. The sensitive skin may be caused by various factors including allergy, stress and environment.

16 Stinging is related to the condition of skin barrier

17 In-vivo Test: Suppression of Stinging Reaction with Lecinol S-10 S (1%) Sample Procedure Negative control: Water Positive control: Methylparaben (MP) solution Panelists known to be sensitive to stinging (called Stingers ) wash their face twice using a specific face wash. Then, pretreatment (using cotton with 0.15% MP solution) is applied to testing site (cheeks) for 1 minute. This procedure is repeated twice to stimulate the initial sensitivity in panelists. Cottons containing with two samples (water as negative control and 0.1% MP solution) are then applied on the testing site of stingers for 1 minute each, and the stimulus of samples is evaluated in five score stages: 1. Nothing is felt. 2. A weak stimulus is felt. 3. A stimulus is felt. 4. A strong stimulus is felt. 5. A very strong stimulus is felt. The Stinging value of each sample is evaluated using an average of the obtained scores. Finally, the whole panel of stingers (n=13) applied a gel with 1% of Lecinol S- 10 twice daily for 7 days, and the same stinging test was conducted to evaluate the change in stinging scores as a result of Lecinol S-10 (Before and After). 2!

18 Stinging evaluation (Formula) Lecinol S-10 1 % Glycerin 10 % PEG-32 2 % Pemulen TR % Arginine 0.2 % Metylparaben 0.05 % Water to make 100 %

19 Anti-stinging effect (in vivo) Weak Strong Average stinging score Before After 1 week application of Lecinol S-10 (1.0%) Water 0.1% methylparaben solution NEW DATA Skin friendly Application of Lecinol S-10 at 1.0% significantly reduces average stinging score against methylparaben solution (after 1 week; n=13). Lecinol S-10 suppresses stinging reaction in humans. Lecinol S-10 S can be used as an additive to reduce stinging of mild irritants (parabens, phenoxyethanol, fragrances, hinokitiol, sodium lactate etc.) Control: Water 0.1% methylparaben solution Number of subjects from stinging panel, who showed reduction of stinging score after 1 week application of Lecinol S-10 (1.0%) 1 (8%) 7 (54%)

20 Appendix: Stinging is often confused with irritation

21 Anti-inflammatory inflammatory effect: inhibition of Prostaglandin E2 (in vitro) Skin friendly NEW DATA

22 Mechanism of Prostaglandin E2 inhibition: prevention of cytokine release from cells via strengthening of cell membrane UV induced ROS OH OOH Lipid peroxidation induced by ROS results in softening of membrane and stronger permeability Cytokines (PGE2, IL-1Alpha, TNF etc) Keratinocyte Cell membrane X Lecinol S-10 replenishes cell membrane to block release of cytokines

23 Enhancement of anti-inflammatory inflammatory actives Skin friendly Lecinol S-10 helps to boost anti-inflammatory effect of Stearyl Glycyrrhetinate. Reduction of edema (%) hour 2 hours 3 hours 4 hours Lecinol S-10 (2%) + SG (0.1%) Nonionic emulsifier + SG (0.1%)

24 Anti-irritation irritation effect Skin friendly Prevention of corneocytes damage caused by Sodium Lauryl Sulfate (SLS). Closed patch (SLS: 5%); after 72 hours. Microscope photograph of corneocytes. Lecinol S-10 protects stratum corneum from damage by strong detergents. Healthy corneocytes Corneocytes treated with SLS (5%): cells are disfigured and nucleated cells can be seen (parakeratosis) Cells treated with 1% Lecinol S-10

25 Anti-irritation irritation effect Skin friendly Prevention of irritation caused by Sodium Lauryl Sulfate (SLS). Number of subjects Lecinol S-10 (1%) No addition - ± + ++ Irritation Reducing Effect Closed patch (SLS 5%); evaluation after 24 hours; 20 subjects -: no irritation ±: slight reddening +: obvious reddening ++: strong reddening/edema

26 Moisturizing Effect (Increase of Moisture in Skin) Long lasting hydration In vivo test: 9 subjects. Gel with 5% Lecinol S-10 and placebo gel applied twice daily. Skin conductance was evaluated by SKIKON 200. Formulation Test gel Placebo 30 Placebo Gel with 5% Lecinol S-10 Lecinol S KOH 0.2 ACRYLATES/C10-30 ALKYL ACRYLATE CROSSPOLYMER 0.5 1,3-Butylene Glycol 5.0 Conductance ,2-Pentandiol 2.0 Methyl paraben Before test After 1 week After 2 weeks Add water to make 100

27 Formulating with Lecinol S-10 Lecinol S-10 can be dispersed in water or oil at room temperature. Lecinol S-10 However, if Lecinol S-10 is added into heated water, it may form clusters, that impair its dispersion. It is important to disperse Lecinol S-10 well before heating. After it is completely dispersed, the emulsification / homogenization is performed at around degrees Celsius. HLB of Lecinol S-10 is around 10. Dispersion in cold water Dispersion in hot water (clusters are formed) To increase Lecinol S-10 s performance as an emulsifier, it is recommended to mix water and oil in the same phase. Such processing helps to achieve (facilitate) a stable orientation of Lecinol S-10 molecules between the water and oil phases.

28 Moisture Cream (MCLS10-1) 1) Preparation 1. Mix A at room temperature and disperse Lecinol S-10 evenly before heating. Heat to 80 Celsius and mix well. 2. Homogenize A at 5000rpm for 5 minutes. 3. Cool while stirring with paddle mixer. Add B at lower than 40 Celsius and finish the procedure at 35 Celsius. A B LECINOL S-10 (Hydrogenated Lecithin) 1.00 Batyl Alcohol EX (Batyl Alcohol) 1.00 MGS-BV2 (Glyceryl Stearate) 1.00 Decaglyn 1-M (Polyglyceryl-10 Myristate) 0.50 Stearyl Alcohol 5.00 NIKKOL Natural Oils-1 (Natural oil blend) 1.00 KF-995 (Cyclomethicone) 4.00 NIKKOL Trifat S-308 (Triethylhexanoin) 2.00 KF-96A-350cs (Dimethicone) 1.00 Carbopol 981 (2%aq) L-Arginine ,3-Butylene Glycol 4.00 Glycerin 3.00 Methylparaben 0.20 Propylparaben 0.10 Phenoxyethanol 0.40 Water Sodium Hyaluronate (1%aq) 1.00 EDTA-2Na 0.05 Water 5.00

29 Moisture Milky Lotion (MLS10-9) A Lecinol S-10 (Hydrogenated Lecithin) 0.30 Batyl Alcohol 100 (Batyl Alcohol) 0.60 Stearic Acid 0.70 Behenyl Alcohol 65 (Behenyl Alcohol) 0.20 Trifat S-308 (Triethylhexanoin) 8.00 Macadamia Nut Oil 5.00 Mineral Oil (#70) 4.00 KF96A-350sc (Dimethicone) 0.50 Propylparaben 0.10 Glycerin 5.00 Methylparaben 0.20 Xanthan Gum (2% aq) Sodium Citrate (1% aq) 1.00 Water Procedure 1. Mix A at room temperature and disperse Lecinol S-10 evenly before heating. 2. Heat to 80 Celsius and mix well. 3. Homogenize A at 5000rpm for 5 minutes. 4. Cool while stirring with paddle mixer.

30 Guidance formulation This formulation uses Lecinol S-10 as the only emulsifying agent. Original texture, good affinity to skin, rich feeling, absence of sticky feel. Nutri Gel (with Lecinol S-10) Phase INCI Name Trade Name % A Carbomer and Water Carbopol 980 (2%) A Trisodium EDTA 0.02 A Butylene Glycol 7.00 A Glycerin 8.00 A Methylparaben 0.15 A Water B Butylparaben 0.05 B Dimethicone 5.40 B Squalane 1.00 B Phytosteryl Hydroxystearate 0.50 B Cetostearyl Alcohol 0.35 B Hydrogenated Lecithin Lecinol S B d-delta tocopherol 0.10 B BHT 0.02 C Potassium Hydroxide (5% aq. solution) 4.00 Procedure: Prepare A and mix well. Heat to 70 degrees. Heat B to 80 degrees and dissolve. Mix A at 3000 rpm, then increase speed to 7000 rpm and add B into A. After adding B keep rotating for 2 min. Add C and keep stirring at 7000 rpm for another 2 min. Then cool while stirring by regular mixer at 100 rpm (use cool water 25 degrees).