2014-02 VC-IP Concept Book MASTER FILE VER 001.pdf 1
2014-02 VC-IP Concept Book MASTER FILE VER 001.pdf 1
vitamin C derivative
VC-IP
Anti- Age Spots
Pigmentation
Anti- DNA
oxidation Protection
2014-02
TABLE OF CONTENTS
1 About VC-IP
2 Efficacy
z Anti-pigmentation (UV-induced)
z Anti-pigmentation (Age spots)
z Skin Penetration
z Anti-Acne
z Anti-aging
z DNA protection
3 Safety tests
4 Stability
5 Formulation guidelines
2014-02
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RO
OR
1 About VC-IP
CH CH O R
2
O O
Multi-functional Vitamin C Derivative H
OR
Effect Characteristics
Odorless
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Pigment cell
active factor
Rective Inhibition
oxygen Inhibition
1
Inhibition
Peroxidation Tyrosinase activity
Dendricity
2 Suppression
DNA lesion
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2 Efficacy
Anti-Pigmentation ( Tyrosinase Inhibition )
VC-IP was added into mouse melanoma cells (B16-4A5) at various concentrations.
After a 72-hour cultivation, the cells were dissolved and extracted. L-Dopa was then
added to the extract. After 60 minutes at 37 degrees Celsius, the amount of
dopachrome formed by the activity of tyrosinase was evaluated by measuring its
absorbance at 540 nm. Figure below shows that at a concentration of 0.02% and
above VC-IP inhibited the activity of intracellular tyrosinase.
100
Tyrosinase Activity (%)
90
80
70
60
50
0 0.02 0.05 0.1
VC-IP (%)
100
80
60
40
20
0
0 0.005 0.01 0.1 0.2
VC-IP (%) VC-IP(%)
2014-02
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2 Efficacy
Anti-Pigmentation ( Dendricity Suppression )
Placebo:
Ethylhexyl
Palmitate
(100%).
Control (0% VCIP)
Test
samples:
VC-IP 2%
In Ethylhexyl
Palmitate.
2 % VC-IP
Anti-Pigmentation ( UV-induced )
Clinical In-Vivo Study on VC-IP: Reduction of
UV-induced pigmentation (3%)
Number of volunteers: 30
Testing site: Inner side of volunteer’s upper arm
Testing period: 3 weeks
Procedure: For the first step of the test, minimal erythema dose (MED) of each volunteer is
measured using solar simulator. Briefly, 6 dosed of UV ray are irradiated to the inner side of
right upper arm. After 24 hours from irradiation, MED is judged. For the second step, 1.5 MED
of UV ray is irradiated on the inner side of left upper arm of each volunteer in order to make
pigmentation. Sample application is started just after irradiation. Sample is applied twice a
day during test period. Sample application sites are randomly changed in every volunteer in
order to do justice.
Placebo 3% VC-IP
12
After 56 days
18
Before
18
After 56 days
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2 Efficacy
Superior Skin Penetration
The upper part (Stratum Corneum) of the 3D skin model was treated with a formulation
containing 10% VC-IP for a 48 hour period, and HPLC analysis was performed.
It was confirmed that as an active pro-vitamin and ester of vitamin C, NIKKOL VC-IP
permeates the skin and is converted in the skin into vitamin C by esterase and other enzymes.
VCIP showed higher uptake in human cell culture compared to pure ascorbic acid
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Subjects: 8.
Test site: forearm.
3cm
6cm
Amount of VC-IP and Ascorbyl Glucoside collected by tape stripping is evaluated by HPLC
450 700
300 600
Collected amount
250
(mg)
550
(mg)
200 ** **
150 500
100
450
50
0 400
2-5 6-10 11-15 16-20 Total score
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2 Efficacy
Anti-aging Properties
Pigment cell
active factor
Rective Inhibition
oxygen Inhibition
Inhibition
Tyrosinase activity
Peroxidation
DNA
Damage
Pigment cell Epidermal cell
VC-IP was added at various concentrations to human fibroblasts (NB1RGB). After 3 days
of cultivation, the cell growth rate was measured by MTT reduction assay. As shown below,
VC-IP proliferated human fibroblasts. And the result was dose-dependent.
Cell Proliferation Rate (%)
160
140
120
100
80
60
40
20
0
0 0.00625 0.025 0.1
VC-IP (%)
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Anti-aging Properties
Promotion of Collagen Synthesis
Proline involved in collagen synthesis was labeled by 3H and added to human dermal
fibroblasts (NHDF) with various concentrations of VC-IP/L-ascorbic acid and cultivated for 24
hours. Then collagen fractions were obtained. The amount of 3H taken into the collagen
fraction was measured by using a liquid scintillation counter and slot blotter. As shown
below, VC-IP significantly promoted collagen synthesis.
4
L-ascorbic acid
Amount of collagen
3 VC-IP
Control
2
0
0 10 20 50
Concentration (μ mol/L)
100
80 MMP-2
MMP-9
60
Activity of Enzyme (%)
40
20
0 10 20 50 20 50 (μmol/L)
Anti-acne
Clinical In-Vivo Study on VC-IP: Reduction of Acne (10%)
VC-IP (10% in mineral oil) was applied to the inner forearms of 6 volunteers. UVB (2.05
J/cm2) was used to irradiate the test site 4 hours after application. Then the
production rate of squalene peroxide was measured as an indicator of sebum
oxidation. As shown below, VC-IP inhibited the production of squalene peroxide at
the same level as the control without UVB irradiation.
7
Squalene Peroxide
6
Production (%)
5
4
3
2
1
0
No UVB UVB Irradiation UVB Irradiation +
VC-IP
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DNA protection
(VC-IP protects skin from UVB)
VC-IP (%)
UV Irradiation
80
VC-IP and L-ascorbic acid were added
60
at the concentration of 10μmol/L to
epidermal cells. The cells were then 40
irradiated with UVB. After a 24-hour 20
cultivation, cell survival rate was
measured by WST-1 assay. Protective 0
effect of VC-IP was higher than that of No UVB 20 40
L-ascorbic acid due to the fact that the UVB (mJ/cm2)
conversion rate of VC-IP into the cells is L-ascorbic acid VC-IP
higher than that of pure ascorbic acid.
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The comet assay, also called the 'Single Cell Gel Assay', is the technique to detect DNA
damage and repair at the level of single cells. The comet assay or single cell gel
electrophoresis assay is based on the alkaline lysis of labile DNA at sites of damage.
'Comet Assay' is one of the most popular tests of DNA damage detection (e.g., single-
and double-strand breaks, oxidative-induced base damage, and DNA-DNA/DNA-protein
cross linking ) by electrophoresis, developed in recent years.
Comet Assay has very high sensitivity to detect DNA damage.
Idea
Strong alkali
T C
A T
A C A
DNA loses one chain and
T T G T A G A disintegrates
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100
*
*
DNA migration (μm)
80
*
*
*
60
40
No UVB Control VC-IP Vitamin C VC-PMG Ascorbyl
Glucoside
UVB10mJ/cm2
DNA damage was evaluated by the comet assay. HaCaT keratinocytes which were
treated with VC derivatives for 24 h, were exposed to UVB at 100 mJ/cm2.
UVB 10mJ/cm2
UVB 10mJ/cm2 +
VC-IP (100 mM)
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0 hr 2 hr 0 hr 2 hr
0.5 hr 4 hr 0.5 hr 4 hr
1 hr 8 hr 1 hr 8 hr
HaCaT cells were treated with 80 μM VC-IP. After UVA irradiation, DNA fragmentation was
detected by nick end labeling method (TUNEL). VC-IP significantly suppressed DNA
fragmentation (shown with fluorescent staining).
*UVA dosage of the test on this page is 100 mJ/cm2.
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Solubility of VC-IP
The solubility of VC-IP in various cosmetic raw materials was measured at 25, 50 and 75
Celsius. VC-IP is soluble in most oils, whether polar oil or non-polar, except polyhydric
alcohols. (S: Soluble; I: Insoluble).
Procedure
1. Heat and dissolve A and B respectively.
2. While keeping 80oC, add B to A little by little with stirring and emulsify.
3. Cool with stirring and add C at 50oC. Cool to 35oC.
2014-02
Elegant “Wavy” Whitening Cream
Lot 08-WC-SBP-09
This cream was designed for high moisture and high aesthetics- it
creates a wavy swirl & high gloss that is beautiful when you open a jar.
A “Kansei” whitening formulation!
Ingredient wt.%
A BUTYLENE GLYCOL 6.00
GLYCERIN 4.00
PHENOXYETHANOL 0.40
XANTHAN GUM 0.08
CARBOMER 0.66
ACRYLATES/C10‐30 ALKYL ACRYLATE CROSSPOLYMER 0.24
THIOTAINE (ERGOTHIONEINE) 0.15
PENTASODIUM PENTETATE 0.20
SODIUM HYALURONATE (and) PHENOXYETHANOL (and)
2.00
WATER
WATER 49.27
B ARGININE 0.10
WATER 0.90
C TOCOPHEROL 0.10
NIKKOL VC‐IP (ASCORBYL TETRAISOPALMITATE) 30.00
CYCLOPENTASILOXANE 5.00
NIKKOGUARD 88 (ETHYLHEXYLGLYCERIN (and)
0.40
GLYCERYL CAPRYLATE)
Hexaglyn PR‐15 (POLYGLYCERYL‐6 POLYRICINOLEATE) 0.50
Total 100.00
Procedure
1 Mix A until uniform at room temperature.
2 Add B into A and mix until uniform.
3 While stirring with paddle mixer at 200 rpm, add C into A+B
gradually then emulsify for 10min. (200 g scale)
2014-02
Brightening Sleep Mask (2% VC-IP)
This soft cream can be layered on to your skin as your last step.
This formula seals in moisture and corrects uneven skin tone while
you sleep. Nikkol SMT is added to make the formula rinsable the
next day.
Ingredient wt.%
A Mineral Oil 10.00
NIKKOL Triester F‐810 (Caprylic/Capric Triglyceride) 5.00
NIKKOL VC‐IP (Ascorbyl Tetraisopalmitate) 2.00
Vaseline 3.00
Stearyl Alcohol 3.00
NIKKOL MGS‐BV2 (Glyceryl Stearate) 2.20
NIKKOL MYS‐55V (PEG‐55 Stearate) 0.80
Dimethicone 0.50
NIKKOL N‐SPV (Cetyl Palmitate) 2.00
Tocopherol 0.10
Propylparaben 0.10
B Hydroxyethylcellulose, water 10.00
Methylparaben 0.20
Butylene glycol 5.00
Glycerin 7.00
Phenoxyethanol 0.30
Water to 100.00
C Titanium Dioxide 2.00
NIKKOL SMT (Sodium Methyl Stearoyl Taurate) 0.05
Citric Acid, Water 1.00
EDTA‐2Na 0.05
Water 10.00
Total 100.00
Procedure (for 300 g scale)
1 Heat A and B to 80 degrees Celsius and mix well. Stir C at room
temperature with dispersing mixer for 3 minutes and 2500 rp
2 Keeping 80 degrees Celsius, while stirring slowly, add B into A very slowly
with small portions. Then stir with homogenizer at 5000 rpm for 7 minutes.
3 Add C and homogenize for 2 minutes at 5000 rpm.
4 After cooling to 30 degrees Celsius, adjust water content and finish the
procedure.
2014-02
VC-IP 20% Boosting Essence
Lot. 8-AML- 08
Ingredient wt.%
A NIKKOL VC‐IP (ASCORBYL TETRAISOPALMITATE) 20.000
TOCOPHEROL 0.100
(PRESERVATIVE) q.s.
B NIKKOL TGI‐20 (PEG‐20 GLYCERYL TRIISOSTEARATE) 0.100
ACRYLATES/C10‐30 ALKYL ACRYLATE CROSSPOLYMER 0.200
SODIUM HYDROXIDE 0.015
WATER to 100.000
C WATER 15.000
DISODIUM EDTA 0.050
BUTYLENE GLYCOL 2.000
(PRESERVATIVE) q.s.
Total 100.000
Procedure
1 Heat A and B to dissolve.
2 Add A to B while homogenizing B (4,000rpm).
3 Emulsify (5,000rpm, 3min./200g).
4 Cool down to room temperature, then add C to B.
5 Remove air by defoaming machine.
2014-02
Brightening Toner (1% VC-IP)
Lot. 10-SEK-05
Watery translucent toners can be made with Soluble VCIP.
Brightening effect is enhanced with 1% Botanical Extract Complex,
a blend of botanicals with 5 different anti-pigmentation actions.
Ingredient wt.%
A WATER to 100.000
GLYCERIN 1.000
BUTYLENE GLYCOL 2.000
PEG‐6,PEG‐32 0.500
DISODIUM EDTA 0.020
BETAINE 0.500
CITRIC ACID 0.003
(PRESERVATIVE) q.s.
B NIKKOL Soluble VCIP (ASCORBYL
TETRAISOPALMITATE,PPG‐8‐ CETETH‐20,BUTYLENE 5.000
GLYCOL, PPG‐4‐CETETH‐20,GLYCERIN, WATER)
SODIUM HYALURONATE,WATER (1% a.q.) 0.500
BOTANICAL EXTRACT COMPLEX(B)‐BG (GLYCYRRHIZA
GLABRA (LICORICE) ROOT EXTRACT,ARTEMISIA
CAPILLARIS FLOWER EXTRACT,MORUS ALBA ROOT 1.000
EXTRACT,ZIZYPHUS JUJUBA FRUIT EXTRACT,SCUTELLARIA
BAICALENSIS ROOT EXTRACT,BUTYLENE GLYCOL, WATER)
WATER 5.000
C DIPOTASSIUM GLYCYRRHIZATE 0.200
WATER 2.000
D ALCOHOL 5.000
NIKKOL TL‐10 (PEG‐20 SORBITAN COCOATE) 0.500
FRAGRANCE 0.030
Total 100.000
Procedure
1 Dissolve A, B, C and D separately.
2 Add B, C to A while mixing A with paddle mixer, and dissolve completely.
3 Add D to A gradually and mix well to dissolve.
2014-02
Lip Brightening Stick (VC-IP 3%)
Estimated SPF 10-15/ Lot 21 DCL-10
Procedure
1 Mix A at room temperature.
2 While stirring, add B into A until uniform.
3 Heat C to 85‐90oC to dissolve.
4 Heat A+B, D and E to 80oC, then add each of them into C, then finally
add F.
5 Pour into a mold then cool down in refrigerator.
Spot Correcting Stick (50% VC-IP)
This stick formulation highlights the oil-soluble property of VC-IP:
how easy it can be incorporated in waxy formulations without any
discoloration from high temperature heating.
Total 100.00
Procedure
1 Heat A and mix till uniform. Then pour in mold and leave for 5 min at RT.
2 Remove excess from top of the mold and refrigirate for 10 min.
3 Remove the product from mold.
Ingredients wt%
VC‐IP (Ascorbyl Tetraisopalmitate) 20.00
Macadamia Nuts Oil 0.50
Syncelane 4SP (Hydrogenated Poly‐C6‐12 Olefin) 8.80
A
Nikkol Trifat S308 (Triethylhexanoin) 35.00
Tocopherol 0.50
Total 100.00
Procedure
1 Mix all ingredients with a paddle.
2014-02
Smoothening Correcting Line Filler (1% VC-IP)
02-VCIP-WC-0702
This silky-feel matte silicone gel-emulsion fills and smoothen lines &
blurs out uneven spots. VCIP adds a treatment function to the
formula.
Ingredient wt.%
<Procedure>
1. Heat A to dissolve.
2. Stir well B at RT until even.
3. Add A into B and mix until even using a paddle mixer.
4. Add C and mix till a homogenous silicone gel is made.
5. Add D until an even paste is made.
2014-02
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