CLINICAL EFFICACY ON CHALLENGED SKIN2

Placebo

Determination of the Antioxidant Power (AP):4 this in vitro standard diagnostic,

benchmarked to vitamin C, has allowed to determine the antioxidative capacity and
reactivity of Hi-Quercetin. It has shown an antioxidant capacity that was fully
maintained inside a cosmetic formulation (O/W emulsion) even after 48h at 40C
storage.
Protective effect against UV induced oxidative stress:5 when applied to a stabilized
human keratinocytes cell line, Hi-Quercetin was shown to significantly inhibit
UVA induced ROS production al all tested dosages. Specifically, at the 0.05 mg/ml
dosage and with the highest energy challenge (5J), ROS production was still
reduced by 39.87%, overperforming by far ascorbic acid tested as positive
benchmark.

30 subjects
-14

-12

-10

-8

-6

-4

-2

% OF WHEAL SIZE REDUCTION (T30)

TEWL variation from SLS challenge

80

*** p<0.0001
** p<0.001
*p<0.01

75
70
65
60
55

50
45
35
30

**

positive benchmark
Hi-Quercetin
placebo
untreated

40

***
***

T120

T60

T0

Inhibition of basophil degranulation

% OF INHIBITION

100
90

83.6%

80
70

Hi-Quercetin
positive benchmark (HA)

60
50

1.25 g/ml

2.5 g/ml

5 g/ml

10 g/ml

Skin antioxidant power

SKIN ANTIOXIDANT POWER %

140

Hi-Quercetin 0.5%
positive benchmark Tocopherol 1%
placebo

130

* p<0.05

120
110
100
90

10 min

30 min

60 min

120 min

Inhibition of UVA induced ROS release

40

% OF INHIBITION OF ROS RELEASE

Determination of the Skin Antioxidative Protection (SAP):4 Hi-Quercetin was

tested for its ability to permeate the epidermis and enhance the skins antioxidative
defence system by 17% at the given concentration (0.5%) in a inert delivery system.
It even overperformed the positive benchmark tocopherol (1%) by 125% (AUC).

**

Untreated

ANTIOXIDANT CHALLENGE AND INHIBITION OF ROS

Different tests aiming at the determination of the antioxidative efficacy of HiQuercetin in cosmetic applications, were performed. The antioxidant capacity,
reactivity, oxidation resistance and long term stability is to be evaluated with relevance
to cosmetic formulations, skin intrinsic antioxidant capacity and ROS release inhibition.

**p<0.001

Hi-Quercetin

IN VITRO INHIBITION OF BASOPHIL DEGRANULATION

Aim of this test was to evaluate the capacity of Hi-Quercetin to inhibit basophil
degranulation.3 Basophil degranulation is induced by specific allergens interacting
with the IgE receptor located on the granulocyte surface. Basophil degranulation
was compared to a positive benchmark (Hyaluronic Acid, HA) and b-hexaminidase
was quantified as a marker of degranulation. Hi-Quercetin resulted effective in a
dose dependent way in inhibiting basophil degranulation up at a level of 83.6% (at a
10g/ml), overcoming the performance of the positive benchmark.

**

Positive control

TEWL (g/h/m2)

A single blind, placebo controlled human trial on 30 subjects has been

conducted by inducing specific skin challenges causing redness, skin barrier
disruption and allergic-like challenges following to the exposure to the
following conditions: histamine(1%); UV irradiation; exfoliation induced by
glycolic acid; skin barrier disruption induced by SLS. The Hi-Quercetin
soothing efficacy (in a 1% formulation) was tested at different times (according
to the challenge model) and compared to the blank sample and a positive
reference. In the histamine challenge, the wheal size was 13.25% smaller
(p<0.001), even smaller than the positive benchmark. The redness following to
UV challenge in the treated area was over 10% less intense compared to the
placebo area (p<0.01). The SLS challenge has induced a skin barrier disruption
evaluated by TEWL, and at 4 hours from the challenge and products application
TEWL was 38.10% lower (p<0.001), overperforming the positive benchmark.
Finally the challenge induced by glycolic acid, measured by Mexameter,
decreased by almost 17% (p<0.0001). All other assessed parameters have been
ameliorated, i. e. reported itch on the prick test, skin hydration, redness, in all
challenges have been reported to significantly ameliorate skin conditions.

Wheal size reduction following to prick test (histamine)

* p<0.05
30

1J
3J
5J

20

10

0
Ascorbic acid
0.15 mg/ml

DID YOU KNOW...

Hi-Quercetin 1%
emulsion 0.02 mg/ml

Hi-Quercetin 1%
emulsion 0.05 mg/ml

Hi-Quercetin 1%
emulsion 0.1 mg/ml

Quercetin is a powerful antioxidant, reported to be more potent than ascorbic acid and tocopherol. 6It is also a powerful enzyme
manipulator being a selective inhibitor of pro-inflammatory metabolites. 9 Also, it is one of the most abundant and ubiquitary secondary
metabolites of the whole botanical kingdom,7 where it also plays the role of a pigment to attract pollinators.

1.ISO/FDIS 16128-1, 2014. - 2. IARC Monographs, Vol 73, 1999. - 2. Abich report REL/533/2015/CLI/SAB, 2015. - 3. Abich report