silanoltechnology: delivery vehicle and skin structuring agent · young aged silanol cells cells...

Silanol Technology:

Delivery Vehicle and

Skin Structuring Agent

Integrity Ingredients Corporation

04.11.2018

Silanol Technology

Silanol Technology:

Ø Bioavailable molecular structure centered around the Si atom

Ø Readily accepted by the skin’s own connective tissue

Ø Supports skin’s architecture and functions

Ø Capable of delivering active compounds and enhancing their activity

Silanol Technology

Silicon : the atom

Silicon14Si

28.1

Silanol Technology

Silicon for Skin & Hair

Si element

Epidermis

Dermis

Hypodermis

DEJ

- Active part of pathway for synthesis of structure proteins- Important for activation of enzymes

- Shown to be vital for skin strength & elasticity- Silicon content in hair correlates with lower rate of hair loss and increased brightness

De Araujo, et al, “Use of Silicon for Skin and Hair Care”, An. Bras. Dermatol. 2016. 91(3): 331-335.

Silanol Technology

Silicon for Skin & Hair

Si element

Epidermis

Dermis

Hypodermis

DEJ

Silicon has been found to play a vital role in the formation and maintenance of connective tissue

Barel, et al, Archives of Dermatological Research 2005. 297(4): 147-153.

Silanol Technology

With age, the amount of silicon in connective tissue decreases **

Si-dependent pathways slow down

Skin architecture starts to decline

** Jugdaohsingh, et al, “Decrease in Silicon Concentration of the Connective Tissues with Age”, Bone 75 (2015), 40-48.

Silanol Technology

Silanol is stabilized in its monomeric active form by attaching

bioactive molecules

Silanol is prone to polymerization into biologically inactive silicone

Si

CH3

OHHO

OH

Bioactive molecule

Bioactive molecule

Bioactive molecule

Si

CH3

OHHO

OH

Si

CH3

OO

OH

Si

CH3

OH

Si

CH3

OO

OH

Silanol stabilization reaction

Core Silanol

Silanol Technology

Exzymol’s original SilanolSilanol core stabilized with Alginic Acid

Si

CH3

OHHO

OH

Alginic Acid

Alginic Acid

Alginic Acid

METHYLSILANOL MANNURONATE

Silanol Technology


Silanol improves skin’s architecture by:

Ø Stimulating collagen production

Young Aged Silanolcells cells 2.5%in FCS in FCS

Young skin Aged skin Aged skin 31 yr old 51 yr old + Silanol treatment 4 %

High collagen density as large bundles in young skin

Silanol Technology


Silanol improves skin’s architecture by:

Ø Increasing skin cell proliferation

Ø Improving cellular communication –increases Keratinocytes’ ability to support Fibroblast activity

Control Silanol SilanolFCS 0.01% 0.1%

Control Silanol treatment HRE 5 %

A B C D

A = Fibroblasts alone, FCSB = Keratinocyte action addedC = Silanol added 1%D = Silanol added 1.5%

Silanol Technology

Active Silanols – Global Skin Care Benefits:Epidermis, DEJ, Dermis & Hypodermis

Epidermis

Dermis

Hypodermis

DEJ

Epidermis

Dermis

Hypodermis

DEJ

Epidermal thickening & elasticity, hydration & protection, increased HA production, tyrosinase inhibition.

Microcirculation, lipolysis for firming & slimming, reduced lipogenesis.

Improved cell communication and cohesion between layers. Increased expression of DEJ constituents: Laminin 5, Perlecan, Collagens IV and VII. Inhibits DEJ-originating age spots.

Collagen production and organization for boosting firmness, density, elasticity and flexibility. Moisturization & Osmoregulation. Delayed fibroblast senescence.

Silanol Technology

Epidermis

Dermal-Epidermal Junction

Dermis

Staining : Masson’s TrichromeNuclei in blue / blackCytoplasm in pinkCollagen fibers in blue green

Silanol Technology

ACTIVE SILANOLS TARGETING EPIDERMIS

Active Pendant Groups:

• Hyaluronic Acid – low MW (150-600 kDa)

• Hyaluronic Acid – high MW (> 2 MDa)

• Ascorbic Acid

• Salicylic Acid

• n-Acetyl Tyrosine

• Hydrolyzed Collagen

• Hydrolyzed Pearl Powder

Silanol Technology

Silanol core stabilized with low MW Hyaluronic Acid (150-600 kDa)

Si

CH3

OHHO

OH

Low MW Hyaluronic Acid



SILANETRIOL (and) HYALURONIC ACID

Silanol Technology

Silanol increases keratinocyte proliferation in HRE

Ker

atin

ocyt

e pr

olife

ratio

n(%

of c

ontro

l)

Control Si (50mg/L)

25

0

50

75

100

125+20%

Fibr

obla

stpr

olife

ratio

n(%

of c

ontro

l)

Aged cellsFCS 2%

Si (10mg/L)FCS 2%

Si (15mg/L)FCS 2%

20

0

40

60

80

100

Silanol increases keratinocytes’ ability to support fibroblast proliferation

(cellular communication)

+32%

+85%


Silanol Technology

Silanol increases HA production by keratinocytes

HA

(% o

f con

trol

)

Control Si (50mg/L)

25

0

50

75

100

125

+75%150

175


Silanol Technology


Silanol-HA 5%

Silanol-HA

Silanol Technology


Silanol-HA 5%

Control Silanol-HA

Control Silanol-HA

Silanol Technology


Test Vehicle

WaterCetearyl Alcohol, Polysorbate 60Cetyl PalmitateSilanol-HAPhenoxyethanol

5% Si-HA gel-cream

IN-VIVO Study

Evaluations

v Dermatologist assessmentv Visia CR Imagingv Primos Optical 3D

Silanol Technology


Silanol Technology

DIMETHYLSILANOL HYALURONATE

Silanol core stabilized with high MW Hyaluronic Acid (> 2 MDa)

Si

CH3

OHHOHigh MW

Hyaluronic AcidHigh MW

Hyaluronic Acid

CH3

Silanol Technology


High-MW HA Silanolü Restructuring activity of the Silanolü Moisturizing properties of the Hyaluronic Acid

Sum

mar

y of

Tes

t Res

ults

Silanol Technology


Days

hMW-HA-Si

High-MW HA SilanolØ Improves hydration better

than pure HA Ø Continues over 9 days after

end of treatment

[Infra-red spectrometry]

Silanol Technology

Silanol core stabilized with Ascorbic Acid

Si

CH3

OHHO

OH

Ascorbic Acid

Ascorbic Acid

Ascorbic Acid

ASCORBYL METHYLSILANOL PECTINATE

Silanol Technology


Silanol technology:

Ø Delivers stabilized Ascorbic Acid to Epidermis

Ø Reinforces cell membranes against free radical activity

Ø Optimizes cutaneous restructuring effects of Ascorbic Acid

Ø Delivers tyrosinase inhibition

Silanol Technology


Protects cutaneous cells:ü Higher bioavailability of ascorbic acidü Free radical scavengingü Strengthens cell membranes

ESR study

Silanol Technology

ACTIVE SILANOLS TARGETING DEJ

Active Pendant Group:

• Rhamnose

Silanol Technology

Silanol core stabilized with Rhamnose:Enables expression of specific DEJ functions

ü Restores Dermal-Epidermal cohesion and thicknessü Increases keratinocyte proliferation in DEJü Boosts expression of Laminin-5, Perlecan, Collagens I, IV and VIIü Reduces formation of age spots originating in DEJ

Si

CH3

OHHO

OH

Rhamnose

Rhamnose

Rhamnose

SILANETRIOL (and) RHAMNOSE

Silanol Technology


Young Aged

Lamina densa Anchoring fibers

TEM of DEJ transformations in aging skin

v Thinning of the lamina densav Loss of anchoring proteinsv Decreased skin cohesionv Impaired cell communication

Silanol Technology


Young Aged

Lamina densa Anchoring fibers

TEM of Explant: Treatment with Si-Rhamnose

Si-Rhamnose5%

Si-Rhamnose10%

Silanol Technology


Si-Rhamnose (5%)Control

Laminin-5 (green)

Si-Rhamnose (5%) Si-Rhamnose (5%)

Silanol Technology


Collagen IV (green)

Si-Rhamnose (5%)Control

Si-Rhamnose (5%)

Si-Rhamnose(5%)

Silanol Technology


Si-Rhamnose (5%)

Age spot mechanisms: • KGF• Melanin leakage

Si-Rhamnose:• Reinforces DEJ• Prevents melanin

leakage• Stimulates Perlecan

(scavenges KGF)

Silanol Technology

5% Si-Rhamnose gel-cream

IN-VIVO Study

Evaluations

v Dermatologist assessmentv Visia CR Imagingv Primos Optical 3D


Summary of Results

ü Skin relief – ave 45% improvementü Firmness – ave 10% increaseü Elasticity – ave 15% increaseü Redness reduced ave 19%ü Brown spots reduced ave 13%ü Luminosity improved ave 33%

Silanol Technology


T 0 T 28

Primos imaging:Improvement in skin architecture – significant wrinkle reduction and smoothing

Silanol Technology


Visia analysis:Reduction in brown spots

Ø Average 13%Ø Maximum 30%

T0 T28

Silanol Technology

ACTIVE SILANOLS TARGETING Dermis


• Hydroxyproline

• Lactic Acid

• Trehalose

Silanol Technology

Silanol core stabilized with Hydroxyproline(a precursor of collagen)

Ø Optimizes tissue production (e.g. for scars)Ø Tissue reinforcement for elasticity (anti-stretchmark)Ø Body firmingØ Delays fibroblast senescence

Si

CH3

OHHO

OH

Hydroxyproline

METHYLSILANOL HYDROXYPROLINE ASPARTATE

Hydroxyproline

Hydroxyproline

Silanol Technology


Delays fibroblast senescence

Si-HPr (0.4%)

Silanol Technology


Optimizes skin reparation

Aged skin+ Hydroxyproline+ Si-HPr + Si-HPr

+ Hydroxyproline

Collagen fibers are packed, the skin less elastic

Restoration of an optimal inter-fibrillar space for improved skin elasticity and flexibility

Silanol Technology

ACTIVE SILANOLS TARGETING Hypodermis


• Caffeine

• Theophylline Alginate

• L-Arginine

• Acefylline (Acetyloxy Theophylline)

Silanol Technology

Silanol core stabilized with Caffeineü Slimming & Anti-Celluliteü Firming & Tightening – body, face, neckü Eye Contouringü Activates microcirculation

Si

CH3

OHHO

OH

Caffeine

SILOXANETRIOL ALGINATE (and) CAFFEINE

Caffeine

Caffeine

Silanol Technology


Caffeine Si-Caffeine Caffeine Si-Caffeine

Control Caffeine Si-Caffeine

Bioavailability vs Caffeine

Silanol Technology


Control Si-Caffeine3%

Si-Caffeine

Lipolysis Activation

Lipogenesis Inhibition

Silanol Technology


4% Si-Caffeine gel-cream

IN-VIVO Study10 women25-43 y.o.

10 weeks

Circ

umfe

renc

e (c

m)

Silanol Technology

Active Silanols – Global Skin Care Benefits:Epidermis, DEJ, Dermis & Hypodermis

Epidermis

Dermis

Hypodermis

DEJ

Epidermis

Dermis

Hypodermis

DEJ

Epidermal thickening & elasticity, hydration & protection, increased HA production, tyrosinase inhibition.

Microcirculation, lipolysis for firming & slimming, reduced lipogenesis.

Improved cell communication and cohesion between layers. Increased expression of DEJ constituents: Laminin 5, Perlecan, Collagens IV and VII. Inhibits DEJ-originating age spots.

Collagen production and organization for boosting firmness, density, elasticity and flexibility. Moisturization & Osmoregulation. Delayed fibroblast senescence.

Acknowledgements


ι ◦ 2 “Where Quality and Service Meet”

Emmanuel Coste, PhD – Technical Director, Exsymol Monaco

Celeste Whritenour – General Manager, Biosil Technologies

David Howell – President, Integrity Ingredients Corporation


silanoltechnology: delivery vehicle and skin structuring agent · young aged silanol cells cells...

Documents