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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
METHYLSILANOL MANNURONATE
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
METHYLSILANOL MANNURONATE
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
Low MW Hyaluronic Acid
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%
SILANETRIOL (and) HYALURONIC ACID
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
SILANETRIOL (and) HYALURONIC ACID
Silanol Technology
SILANETRIOL (and) HYALURONIC ACID
Silanol-HA 5%
Silanol-HA
Silanol Technology
SILANETRIOL (and) HYALURONIC ACID
Silanol-HA 5%
Control Silanol-HA
Control Silanol-HA
Silanol Technology
SILANETRIOL (and) HYALURONIC ACID
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
SILANETRIOL (and) HYALURONIC ACID
Silanol Technology
SILANETRIOL (and) HYALURONIC ACID
Silanol Technology
SILANETRIOL (and) HYALURONIC ACID
Silanol Technology
SILANETRIOL (and) HYALURONIC ACID
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
DIMETHYLSILANOL HYALURONATE
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
DIMETHYLSILANOL HYALURONATE
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
ASCORBYL METHYLSILANOL PECTINATE
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
ASCORBYL METHYLSILANOL PECTINATE
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
SILANETRIOL (and) RHAMNOSE
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
SILANETRIOL (and) RHAMNOSE
Young Aged
Lamina densa Anchoring fibers
TEM of Explant: Treatment with Si-Rhamnose
Si-Rhamnose5%
Si-Rhamnose10%
Silanol Technology
SILANETRIOL (and) RHAMNOSE
Si-Rhamnose (5%)Control
Laminin-5 (green)
Si-Rhamnose (5%) Si-Rhamnose (5%)
Silanol Technology
SILANETRIOL (and) RHAMNOSE
Collagen IV (green)
Si-Rhamnose (5%)Control
Si-Rhamnose (5%)
Si-Rhamnose(5%)
Silanol Technology
SILANETRIOL (and) RHAMNOSE
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
SILANETRIOL (and) RHAMNOSE
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
SILANETRIOL (and) RHAMNOSE
T 0 T 28
Primos imaging:Improvement in skin architecture – significant wrinkle reduction and smoothing
Silanol Technology
SILANETRIOL (and) RHAMNOSE
Visia analysis:Reduction in brown spots
Ø Average 13%Ø Maximum 30%
T0 T28
Silanol Technology
ACTIVE SILANOLS TARGETING Dermis
Active Pendant Groups:
• 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
METHYLSILANOL HYDROXYPROLINE ASPARTATE
Delays fibroblast senescence
Si-HPr (0.4%)
Silanol Technology
METHYLSILANOL HYDROXYPROLINE ASPARTATE
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
Active Pendant Groups:
• 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
SILOXANETRIOL ALGINATE (and) CAFFEINE
Caffeine Si-Caffeine Caffeine Si-Caffeine
Control Caffeine Si-Caffeine
Bioavailability vs Caffeine
Silanol Technology
SILOXANETRIOL ALGINATE (and) CAFFEINE
Control Si-Caffeine3%
Si-Caffeine
Lipolysis Activation
Lipogenesis Inhibition
Silanol Technology
SILOXANETRIOL ALGINATE (and) CAFFEINE
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
Integrity Ingredients Corporation
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
Integrity Ingredients Corporation