Lecinol SLecinol S--1010

Skin friendly

Stabilizer

EO-free

Active delivery

Soy derived

Oil-in-Water

Plant-derived

Primary Emulsifier for Sensitive Primary Emulsifier for Sensitive Skin CareSkin Care

N I K K O C H E M IC A L S C O . , L T D .1-4-8 NIHONBASHI-BAKUROCHO, CHUOKU, TOKYO, 103-0002, JAPANT E L : 8 1 - 3 - 3 6 6 1 - 1 6 7 7 F A X : 8 1 - 3 - 3 6 6 4 - 8 6 2 0E - m a i l : i n t e r @ n i k k o l . c o . j p w w w. n i k k o l . c o . j p

Characteristics of Lecinol SCharacteristics of Lecinol S--1010

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.

Soy derived

Plant-derived

Characteristics of Lecinol SCharacteristics of Lecinol S--1010

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)

Soy derived

Plant-derived

Hydrogenated lecithin Hydrogenated lecithin vs natural lecithinvs natural lecithin Soy derived

Plant-derived

Oxidation stability of natural lecithin and hydrogenated lecithin (Lecinol S-10). Hydrogenation makes lecithin very stable against oxidation.

Active deliveryPromoting percutaneous Promoting percutaneous absorption of actives: test methodabsorption of actives: test method

Receptor layer

32℃ water

Skin model

Test substance 0.01 - 0.05g

Mixer Penetration of an active substance is evaluated by HPLC

Test sample：1.0% Indomethacin

epidermis

dermis

Abs

orpt

ion

of I

M(%

of t

otal

reco

very

)

Active delivery

Percutaneous absorption behavior of indomethacin (IM; 1.0%) to the cultured 3D skin model

Promoting percutaneous Promoting percutaneous absorption of activesabsorption of actives

10

15

20

3%

17%

4%

0

5

commercial item Lecinol S-10 ointment

1%

Lecinol SLecinol S--10 forms liposomes10 forms liposomes

Microscopic pictures of Lecinol S-10 generated liposomes

Makes liposomes

Moisturizing effect (in vivo)Moisturizing effect (in vivo) Instant hydration

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.

NEW DATA

NEW NEW DATADATA

“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.

New Data: StingingNew Data: Stinging

““StingingStinging”” reaction to cosmeticsreaction to cosmetics

“Stinging test performed”

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.

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

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。

… itching, uncomfortable feeling. The evaluation uses panelists who are known to show stinging reaction to certain compounds …

… very light reaction, slight itching …

Definitions of stinging ….

Explanation of the stinging evaluation (from Shiseido website)

From the website of Kao

Stinging testStinging test

Stinging testStinging test

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.

Stinging is related to the Stinging is related to the condition of skin barriercondition of skin barrier

InIn--vivo Test: Suppression of Stinging Reaction with vivo Test: Suppression of Stinging Reaction with Lecinol SLecinol S--10 (1%)10 (1%)Sample Negative control: Water

Positive control: Methylparaben (MP) solution

Procedure 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!

Stinging evaluation (Formula)Stinging evaluation (Formula)

Lecinol S-10 1 %

Glycerin 10 %

PEG-32 2 %

Pemulen TR-2 0.4 %

Arginine 0.2 %

Metylparaben 0.05 %

Water to make 100 %

AntiAnti--stinging effect (in vivo)stinging effect (in vivo) Skin friendlyNEW NEW DATADATA

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 SLecinol S--10 can be used as an 10 can be used as an additive to reduce stinging of mild additive to reduce stinging of mild irritants (parabens, phenoxyethanol, irritants (parabens, phenoxyethanol, fragrances, hinokitiol, sodium lactate fragrances, hinokitiol, sodium lactate etc.)etc.)

Control: Water0.1%

methylparabensolution

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%)

1

2

3

Water 0.1% methylparaben

solution

Ave

rage

stin

ging

sco

re

Before

After 1 week application of Lecinol S-10 (1.0%)

Wea

k

Stro

ng

Appendix: Stinging is often confused with irritationAppendix: Stinging is often confused with irritation

AntiAnti--inflammatory effect:inflammatory effect:inhibition of Prostaglandin E2 (in vitro)inhibition of Prostaglandin E2 (in vitro)

Skin friendly

NEW NEW DATADATA

Mechanism of Prostaglandin E2 inhibition: prevention of cytokineMechanism of Prostaglandin E2 inhibition: prevention of cytokinerelease from cells via strengthening of cell membranerelease from cells via strengthening of cell membrane

Cytokines (PGE2, IL-1Alpha, TNF etc)

UV induced

ROS

OH

OOHLipid peroxidation induced by ROS results in softening of membrane and stronger permeability

XLecinol S-10replenishes cell membrane to block release of cytokines

Keratinocyte

Cell membrane

Enhancement of antiEnhancement of anti--inflammatory inflammatory activesactives

Skin friendly

Lecinol S-10 helps to boost anti-inflammatory effect of Stearyl Glycyrrhetinate.

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1 hour 2 hours 3 hours 4 hours

Red

uctio

n of

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(%)

Lecinol S-10(2%) + SG(0.1%)

Nonionicemulsifier +SG (0.1%)

Prevention of corneocytes’ damage caused by Sodium Lauryl Sulfate (SLS). Closed patch (SLS: 5%); after 72 hours. Microscope photograph ofcorneocytes.

Lecinol S-10 protects stratum corneum from damage by strong detergents.

Cells treated with 1% Lecinol S-10

Healthy corneocytes Corneocytes treated with SLS (5%): cells are disfigured and nucleated cells can be

seen (parakeratosis)

AntiAnti--irritation effectirritation effect Skin friendly

Irritation Reducing EffectClosed patch (SLS 5%); evaluation after 24 hours; 20 subjects－: no irritation ±: slight reddening ＋: obvious reddening＋＋: strong reddening/edema

AntiAnti--irritation effectirritation effect Skin friendly

Prevention of irritation caused by Sodium Lauryl Sulfate (SLS).

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12

－ ± ＋ ＋＋

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f sub

ject

s Lecinol S-10 (1％)No addition

0

10

20

30

Con

duct

ance

Before test After 1 week After 2 weeks

Placebo Gel with 5% Lecinol S-10

Moisturizing Effect Moisturizing Effect (Increase of Moisture in Skin)(Increase of Moisture in Skin)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

Lecinol S-10 5.0 0.0

KOH 0.2

ACRYLATES/C10-30 ALKYL ACRYLATE CROSSPOLYMER

0.5

1,3-Butylene Glycol 5.0

1,2-Pentandiol 2.0

Methyl paraben 0.2

Add water to make 100

Long lasting hydration

Formulating with Formulating with LecinolLecinol SS--1010LecinolLecinol SS--1010

Dispersion in cold water

Dispersion in hot water (clusters

are formed)

Lecinol S-10 can be dispersed in water or oil at room temperature.

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 60-70 degrees Celsius.

HLB of Lecinol S-10 is around 10.

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.

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) 10.00 L-Arginine 0.20 1,3-Butylene Glycol 4.00 Glycerin 3.00 Methylparaben 0.20 Propylparaben 0.10 Phenoxyethanol 0.40 Water 59.55 Sodium Hyaluronate (1%aq) 1.00 EDTA-2Na 0.05 Water 5.00

B

A

Moisture Cream Moisture Cream (MCLS10(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.

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) 10.00 Sodium Citrate (1% aq) 1.00 Water 64.40

A

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.

Moisture Milky Lotion (MLS10-9)

Nutri Gel (with Lecinol S-10)

Phase INCI Name Trade Name %A Carbomer and Water Carbopol 980 (2%) 23.00A Trisodium EDTA 0.02A Butylene Glycol 7.00A Glycerin 8.00A Methylparaben 0.15A Water 49.41B Butylparaben 0.05B Dimethicone 5.40B Squalane 1.00B Phytosteryl Hydroxystearate 0.50B Cetostearyl Alcohol 0.35B Hydrogenated Lecithin Lecinol S-10 1.00B d-delta tocopherol 0.10B BHT 0.02C Potassium Hydroxide (5% aq. solution) 4.00

Guidance formulationGuidance formulationThis formulation uses Lecinol S-10 as the only emulsifying agent.Original texture, good affinity to skin, rich feeling, absence of sticky feel.

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).