Actiwhite

by Beauty Creations
™

The tailor-made whitener and spot preventer to improve skin appearance

Lightening the skin complexion and giving skin back its original glow are the major
challenges for the cosmetic world, as they target all generation.
Reduction of the age spots consists of decreasing the melanin present in the skin,
preventing its formation and diminishing its transport. Although many depigmentation
ingredients act on melanin formation inhibition through tyrosinase, few of them combine
rapidly visible in vivo effectiveness, compliance with Asian regulatory requirements and
high-cutaneous tolerance.
Recognized depigmentation substances are either unstable in formulation, cytotoxic like
hydroquinone, or even sensitizing such as kojic acid.
These disadvantages have given us the foundations for a new strategy of depigmentation
ingredient development.

BASF Beauty Creations has chosen a new target involved in the biogenesis of
melanosome and melanins: the PMEL-17 gene ☐.
Our strategy has led to the development of Actiwhite™, which inhibits the
maturing of melanosomes through reduction of the expression of gene PMEL-17
and deactivates tyrosinase in vitro .

☐
see glossary

ActiwhiteTM
Melanogenesis regulator
Actiwhite™ with a good cutaneous tolerance, is a water-dispersible white powder which is easy
to formulate in all formulation types (4<pH<8).
Actiwhite™ is a synergistic complex of sucrose dilaurate and pea extract that is in line with the
regulatory requirements of the Chinese and Japanese Quasi-Drug markets.
Actiwhite™ has been subject to two clinical studies demonstrating its skin-lightening effect and
ability to correct age spots.

Properties
• Inhibitor of PMEL-17 gene expression, implicated on the melanosomal maturation.
• Inhibitor of tyrosinase activity.

Applications
• Brightening, anti-dark spots and body care.
• Radiance care: complexion perfector.
• Express spots eraser for face and hands.
• Concentrated lightening care for neck and cleavage.
 Synergy of ActiwhiteTM components
The combination of the pea extract and sucrose dilaurate has a greater inhibiting effect compared
to the same raw material tested individually.

120

100
Results in % / control

*/Co
80
**/Co

60
+ 33 % effectiveness in
**/Co
*/Sdl
 33%
* combination.
40

20

0
Tyrosinase activity

Control (Co)
Kojic acid at 0.03%
Pea extract at 0.001%
Sucrose dilaurate (Sdl) at 0.01%
Pea extract
+ sucrose dilaurate at 0.001% + 0.01%

Mean of 1 assay in triplicate - Paired Student’s t test - *: p<0.05 - **:p<0.01

In vitro study on B16 melanocytes.

Tyrosinase activity measurement by optical density.

Regulation of gene PMEL-17

120

100
PMEL-17 gene expression

- 23%
80
in % / control

60 Decrease of PMEL-17
40
gene expression.
20

0
Control Actiwhite™
at 0.0013%

Actiwhite™ has reduced the expression of gene PMEL-17, involved in both maturing melanosome
and synthesising melanins.

In vitro study on human epidermal melanocytes.

A melanogenesis specific DNA chip was used and the variations in expression of the PMEL-17 gene were
confirmed by qRT-PCR.
 Tyrosinase inhibitor

120
Significant reduction of
100
tyrosinase activity.
Results in % / control

*
80
**
60

40

20

0
Control Kojic acid Actiwhite™ at
at 0.03% 0.0167% 0.033%

Mean of 4 assays in triplicate – Paired - Student’s t test - *: p<0.05 - **:p<0.01

The anti-tyrosinase activity of Actiwhite™ is similar to kojic acid.

In vitro study on B16 melanocytes.

Tyrosinase activity measurement by optical density.

Melanogenesis reduction

Significant reduction
of the released
100
Released melanin
melanin quantity.
75
Results in % / control

* - 65%
50
Intracellular melanin
**
25

** *
**
0
Control Kojic acid Actiwhite™ at Control Kojic acid Actiwhite™ at
at 0.03% 0.0082% 0.0165% at 0.03% 0.0082% 0.0165%

Mean of 5 assays in triplicate - Student’s t test - *: p<0.05 - **: p<0.01

In vitro study on B16 melanocytes.

Measurement of the proportion of released and intracellular melanin by optical density.
 Clinical evaluation of lightening efficacy

After 12 weeks...
Skin appearance looks
lighter. ActiwhiteTM is
20 perfectly tolerated.
Pigmentation index (% of decrease/ baseline)

18
***
16
14
12
10 ***
8 *** Statistics:
** Control Mean on 26 volunteers
6
Hydroquinone at 2% Student's t test / control
4 ** p<0.01
Actiwhite™* at 1.7% *** p<0.001
2
0
-2 After 6 weeks After 12 weeks

* This clinical study was conducted with sucrose dilaurate and pea extract at a dose equivalent to ActiwhiteTM at 1.7%.

After 6 weeks of treatment, the lightening effect of Actiwhite™ is equivalent to the hydroquinone
our reference substance which is tested under the same conditions. Actiwhite™ does not cause any
cutaneous irritation.
After 12 weeks of treatment, our results with Actiwhite™ are still significant. The tolerance of
Actiwhite™ is optimum.

In vivo study
Randomized trial on 26 Asian female volunteers, aged between 18 to 45, with dark or very dark skin on the
outside forearm.
Twice a day application of an emulsion containing 1.7% ActiwhiteTM or 2% hydroquinone. Non treated area is
used as control. Measurement of pigmentation index by Mexameter®.
 Clinical study: anti-age spot effect

new
Colorimetric mesurements
Lightening parameter (∆ITA)
Age spots
3.5 *** Kojic acid at 2%
*** +14.7%
3 Actiwhite™ at 2%
+13%
2.5
Statistics:
After 14 days, age spots
2 °
***
Mean of 25 (Actiwhite™)
or 27 (kojic acid) volunteers
ANOVA (mixed GLM)
are significantly
1.5 +7% with Dunnett post-hoc test
° 0.05≤p<0.1 lighter.
1 * p<0.05
° *** p<0.001
0.5 +3%

0
D14 − D0 D56 − D0

Evaluation by a dermatologist
D14 D56 D14 D56 D14 D56
0 After 56 days,the
11% 9%
* *
15% 14%
dermatologist evaluated
0.5
35% 32%
11%
13%
*** ***
that age spots are:
Delta clinical score

***
1 *** *** ***
- less numerous,
1.5
47%
- less visible,
***
50%
***
- smaller.
2
36%
2.5 37%
***
***

3 Number of Color intensity Color intensity

pigmented of the pigmented of the spotless
spots spots area
Statistics:
Kojic acid at 2%: Actiwhite™ at 2%: Mean of 25 (Actiwhite™)
D14-D0 D14-D0 or 27 (kojic acid) volunteers
D56-D0 D56-D0 Wilcoxon’s T test / D0
* p<0.05
*** p<0.001

Self-assessment
Number of dark spots Size of dark spots
20 Kojic acid at 2% 20 Kojic acid at 2%
ActiwhiteTM at 2% ActiwhiteTM at 2%
with the statement «The number of dark spots is important»
Number of volunteers that agree strongly and very strongly

Number of volunteers that agree strongly and very strongly

with the statement «The size of dark spots is important»

18 18
18 18
16 17 16 17

14 14 - 61%
- 61% - 53% - 53%
12 12

10 10 - 67%
- 77% - 71% - 71%
8 8
8 8
6 7 6 7
6
4 5 4 5
4
2 2

0 0
D0 D14 D56 D0 D14 D56 D0 D14 D56 D0 D14 D56

Color intensity of dark spots Statistics:

Percentage calculed
25 on the basis of the answer
with the statement «The color intensity of dark spots is important»

Kojic acid at 2% Actiwhite TM

at 2%
Number of volunteers that agree strongly and very strongly

obtained on 25 (Actiwhite™)
or 27 (kojic acid) volunteers
20
20
19
- 59%
- 58%
15

- 74%
10 - 68%

8 8
After 2 months, up to 80% of
5
5
6 women noticed an age spot
reduction.
0
D0 D14 D56 D0 D14 D56
 Clinical study: skin complexion

new
Colorimetric mesurements
Lightening parameter (∆ITA)
3 Pigmented spot - Spotless area

2.5 ***

** Kojic acid at 2%
2 °
*
+15.9%

+16.1%
Actiwhite™ at 2% After 56 days, skin
1.5
+14.7%
Statistics:
complexion is more
1
Mean of 25 (Actiwhite™)
or 27 (kojic acid) volunteers homogeneous.
ANOVA (mixed GLM)
with Dunnett post-hoc test
° 0.05≤p<0.1
0.5 * p<0.05
+2.6% ** p<0.01
*** p<0.001
0
D14 − D0 D56 − D0

Evaluation by a dermatologist
3
Complexion Skin clarity/
homogeneity brightness
2.5 After 14 days, the
dermatologist evaluated
Delta clinical score

***
2 ***

***
49% 48% that the skin is more
1.5
32% 34%
***
luminous and has
1 uniform color.
***
***
0.5 * 16% 14%
*
7%
6%
0
D14 D56 D14 D56

Statistics:
Mean of 25 (Actiwhite™)
Kojic acid at 2%: Actiwhite™ at 2%: or 27 (kojic acid) volunteers
D14-D0 D14-D0 Wilcoxon’s T test / D0
D56-D0 D56-D0 * p<0.05
*** p<0.001

Self-assessment
Skin complexion Skin brightness
Number of volunteers that agree moderately strongly and very strongly

25 Kojic acid at 2% 25 Kojic acid at 2%

ActiwhiteTM at 2% ActiwhiteTM at 2%
very strongly with the statement «The skin is bright/luminous»
with the statement «The complexion is uniform/homogenous»

Number of volunteers that agree moderately strongly and

+ 124% + 147%
20 20
20 20
+ 183%
+ 129%
15 15 17
16

+ 12%
10 + 29% 10 + 10% + 50%
9 10
8 9
7 9
5 5 6 9

0 0
D0 D14 D56 D0 D14 D56 D0 D14 D56 D0 D14 D56

Statistics:
Percentage calculed
on the basis of the answer
obtained on 25 (Actiwhite™)
or 27 (kojic acid) volunteers

At 2%, the effects of ActiwhiteTM

and kojic acid are considered to
be comparable.
 Clinical study

After 14 days... new

Visible effect confirmed by users.

Visualization

D0 D14 D56

D0 D14 D56

In vivo study
Randomized trial on 25 Asian female volunteers between 18 to 70 years old of having a phototype III and IV, all
skin types. The specific requirement was the presence of well-defined pigmented spots on each side of the face
associated to a spotless area.
Twice a day application for 8 weeks of an emulsion containing 2% ActiwhiteTM or 2% kojic acid. Evaluation by
colorimetric measurement (∆ITA☐), dermatologist, self-assessment and macrophotograph of visibility, size and
number of the age spot, skin complexion.
Summary datasheet
REFERENCE ActiwhiteTM PW LS 9860

DESCRIPTION Synergistic complex of pea extract and sucrose dilaurate.

DOSE OF USE 2%

Regulatory data
INCI (US) Maltodextrin , Sucrose Dilaurate , Sodium Cocoyl Glutamate , Pisum Sativum (Pea) Extract
CAS 9050-36-6, 25915-57-5, 68187-32-6, 90082-41-0
EINECS 232-940-4, 247-345-5, 269-087-2, 290-130-6
China All the raw materials comprising the INCI name ActiwhiteTM are listed on the
"International Cosmetic Ingredient Standard Chinese Name"(2007 version).
Japanese Cosmetic Denomination
Marutodekisutorin(556716), Jiraurinsansukurohsu(005227), Kokoirugurutaminsan Na(502046),
Endouekisu(532281). Each of the ActiwhiteTM ingredients complies with Japanese Standard of Quasi-
Drug Ingredients (JSQI) or the corresponding monograph for quasi-drug additive use (Maltodextrin is
covered in JP by Dextrin, 1422).
Preservative None
Natural label Raw material conform to Ecocert standards of Natural and Organic cosmetics.

Preliminary specifications
Organoleptic characteristics white powder, low odor
pH 4.5 - 6.5 (product at 2%)
Water content ≤ 5.0%
Total nitrogen 0.35 - 0.60%
Sucrose dilaurate 27.0 - 39.0%
Free sugar 55.0 - 65.0%
Microbiological control Upon request
Formulation
Solubility Dispersible in water.
Mode of incorporation Incorporated into the water phase at 80°C, or at room temperature for
cold processing.
Recommended pH 4 - 8

Patent APPLICATION EP1993508 (DE, FR, IT, GB, ES) and its equivalents in KR, JP, US

CUSTOMS CODE 38 24 90 97

STORAGE At ambient temperature (15-25°C), in its original packaging, protected from mois-
ture and light.

SHELF LIFE 24 months

MANUFACTURER
BASF Beauty Care Solutions France SAS
3 rue de Seichamps - 54425 Pulnoy
(France)

Commercial sample of Actiwhite™ and examples of

formulation (at 2% in a hydrogel and an emulsion).
GLOSSARY
qRT-PCR: "quantitative Reverse Transcriptase - Polymerase Chain Reaction" is a
method of quantifying the expression of genes.

PMEL-17 gene: gene coding for the Premelanosomal protein Pmel-17 involved in
melanosome biogenesis, the seat of melanin synthesis.

B16 melanocytes: melanocyte cellular line classically used to test melanin ratios.

∆ITA (Individual Typological Angle): the skin color is defined according to its
luminosity L and its ITA. It defines the degree of pigmentation of the skin of an individual.
The higher the ITA, the lighter the skin.
EUROPE
BASF Beauty Creations
49, avenue Georges Pompidou
92593 Levallois-Perret Cedex
FRANCE
Tel: +33 (0) 1.49.64.53.97
Fax: +33 (0) 1.49.64.53.85
bcs-europe@basf.com

AMERICAS
BASF Corporation
361 Sheep Pasture Road
East Setauket, NY 11733
USA
Tel: +1 (631) 380 2652
bcs-nafta@basf.com

JAPAN & ASIA-PACIFIC

BASF Japan Ltd.
21F Roppongi Hills Mori Tower,
6-10-1 Roppongi, Minato-ku,
Tokyo, 106-6121
JAPAN
Tel: +81 (0) 3-3796-9214
Fax: +81 (0) 3-3796-9299
bcs-asia@basf.com

Edition April 26, 2012

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