Intense Hydration
Series
Granactive Retinoid
THE POWER OF RETINOL WITHOUT THE IRRITATION
GRANACTIVE RETINOID:
THE NEXT STEP IN VITAMIN A CHEMISTRY
Granactive Retinoid is Hydroxypinacolone Retinoate, a cosmetic grade ester of all-trans retinoic
acid. This skin care active ingredient belongs to a class of chemical compounds termed retinoids,
which are natural and synthetic derivatives of Vitamin A capable of binding to retinoid receptors.
The binding of retinoid receptors can enhance gene expression, which effectively turns key cellular
functions on and off. When skin cell retinoid receptors are bound with retinoids, a cascade of
mechanisms that benefit skin complexion are switched on. This can result in enhanced cell prolif-
eration, biosynthesis of extracellular proteins and glycans, and improved cellular turnover. Stimu-
lating these age defying processes in the skin is critical for fighting and reversing signs of aging.
BIOLOGICAL PATHWAYS TO YOUTHFUL SKIN
WITH GRANACTIVE RETINOID
Stimulating cell proliferation and cell turnover are important for normalizing cell renewal and re-
pair processes. As we age our skin becomes thinner and less elastic, leading to skin with a loose,
Texture Transformations
sagging, and wrinkled appearance. Granactive Retinoid helps renew skin plumpness, elasticity,
and hydration to provide a radiant and fresh appearance. Moreover, Granactive Retinoid stim-
ulates skin cell proliferation; restoring thickness to skin that has become thinner over time. These
FEATURING GRANSIL VX-418 AND ICE CREAM REPAIR
processes help fill in lines and wrinkles to give a youthful appearance, while safeguarding skin
from further wrinkle development. The effectiveness of Granactive Retinoid at filling lines and
wrinkles can be seen in Image 1. Granactive Retinoid is highly recommended for promoting clear
skin when used in conjunction with monographed anti-acne treatments. This cosmetic ingredient
promotes cell turnover and renewal, which translates to improved skin clarity and the appearance
of a healthier complexion.
Image 1. Dramatic reduction of lines and wrinkles was observed after 14 day Granactive Retinoid application.
CHALLENGES WITH OLDER GENERATION
VITAMIN A CHEMISTRIES
Although the benefits of retinoids have been known for decades, skin irritation, photochemical
instability, and toxicity concerns have hindered their use. Retinoic acid is a topically applied ingre-
dient recognized for its anti-aging benefits, however it can be irritating to skin and is sold as a pre-
scription medication. Instead in recent years, milder synthetic and natural derivatives have become
popular alternatives to Retinoic acid. These derivatives are metabolized to the active form by skin
cells. Retinol (Vitamin A) is the most popular topical retinoid used to date, but its skin irritancy and
instability to sunlight has limited its scope and appeal. Retinol esters are often used to lower the
irritation potential and increase stability, but a tradeoff is decreased retinoid activity and benefits.
GRANACTIVE RETINOID ADVANCES OPPORTUNITIES
IN VITAMIN A SKIN CARE
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Granactive Retinoid is a next-generation anti-aging product, delivering the performance of retinol
and retinoid derivatives with significantly lower irritation potential, thus supporting clear, visibly
more youthful looking skin with
FEATURING better consumer
GRANSIL VX-418 acceptance. The mechanism
AND ICE CREAM REPAIR of action of Granactive
Retinoid is advanced compared to retinol derivatives. To interact with retinoid receptors, retinol must
first be metabolized to more active forms, such as retinaldehyde and retinoic acid using several
enzymatic steps. Granactive Retinoid is unique in that it processes innate retinoic activity, binding
directly with retinoid receptors without the need for metabolic breakdown to more biologically active
forms. Granactive Retinoid is dermatologically tested to offer less irritation potential than retinol,
providing a gentle, safe and effective anti-aging retinoid.
GRANACTIVE RETINOID ACTIVE - CLINICAL RESULTS
Assay Subject Result
Cumulative irritation patch Human clinical panel No irritation
Local irritation and sensitization potential assay Human clinical panel No adverse experiences
Skin roughness Human clinical panel 50% improvement
Skin surface scaling Human clinical panel 40% improvement
Skin irritation potential vs. retinol Human skin cells Lower irritation potential
Toleration under environmental stresses vs. retinol Human skin cells Better toleration
Retinoid gene expression modulation Human skin cells Typical retinoid expression
In vitro percutaneous penetration Human skin Better toleration
In vivo percutaneous absorption Human skin Passed – proven safe
These results add credence to the beneficial safety and irritation profile of Granactive Retinoid as a
topical cosmetic. The low irritation profile of Granactive Retinoid versus retinol was demonstrated
on a 24 hour occlusive patch test and can be seen in Image 2.
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FEATURING GRANSIL VX-418 AND ICE CREAM REPAIR
GRANACTIVE RETINOID RETINOL
Image 2. After application on a 24 hour occlusive patch test, Granactive Retinoid demonstrated a significantly lower irritation profile
versus retinol. Test samples were 0.5% retinoid in Gransolve DMI (dimethyl isosorbide).
PERFORMANCE
Granactive Retinoid combats the appearance of fine lines and wrinkles for a younger appearance
while increasing skin elasticity for firmer, smoother skin texture. Overall skin clarity and appear-
ance is enhanced for a healthier complexion. Dark spots and skin imperfections are reduced for a
more even skin tone to give a brighter and more luminous appearance to skin. Reduction in pore
size is observed leading to overall skin clarity. Granactive Retinoid delivers high performance
compared to retinol derivatives, but with a significantly lower irritation potential.
FORMULATION
Granactive Retinoid is intended to support anti-aging and anti-acne beauty treatments by provid-
ing low irritating, effective active delivery in daily maintenance applications. Granactive Retinoid
is available as a concentrated and easily formulated anhydrous matrix containing 10% of the
retinoid active in a premium delivery solvent. This offers easy formulation into oil-in-water emul-
sions, water-in-oil emulsions, and other formula types. Applications include (but are not limited to)
skincare, color cosmetic, and body care formulations. For anti-acne claims, the retinoid must be
co-formulated with an approved anti-acne active as subject to regional laws. Granactive Retinoid
should be added to the oil phase of all emulsion types with a clinical use level of 1-2%, but higher
levels are possible without irritation, depending on the formula. It is recommended to formulate
this product in a manner that avoids infusing air/oxygen into the final cosmetic product. Like all
retinoids, the highly specific set of conjugated double bonds are susceptible to oxidation; anti-ox-
idants like Vitamin- E and BHT/BHA are suggested.
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FEATURING GRANSIL VX-418 AND ICE CREAM REPAIR
RETINOID SERUM
Part Ingredient INCI Name % (wt)
A DEIONIZED WATER Water 27.00
NATROSOL 250 HHR, 2% Water & Hydroxyethylcellulose 10.00
AQ SOL.
CARBOPOL ULTREZ-10 Water & Carbomer 5.00
POLYMER, 2% AQ SOL.
BUTYLENE GLYCOL Butylene Glycol 10.00
GLYCERIN Glycerin 5.00
TWEEN 20 Polysorbate 20 0.30
PLANTAREN 2000 N Decyl Glucoside 0.10
TEA, 99% Triethanolamine 0.10
JEECIDE CAP-5 Phenoxyethanol & Caprylyl Glycol & Potassium Sorbate & Water & 1.00
Hexylene Glycol
B CETIOL LC Coco-Caprylate/Caprate 5.00
DIMETHICONE, 5CST Dimethicone 5.00
WICKENOL-131 Isopropyl Isostearate 2.00
ALCOLEC BS Lecithin 0.30
GRANACTIVE RETINOID Dimethyl Isosorbide & Hydroxypinacolone Retinoate 2.00
GRANSIL SIW-066 Dimethicone & Polysilicone-11 & Butylene Glycol & Water & Decyl Glucoside 20.00
GRANSIL PSQ Polymethylsilsesquioxane 5.00
GRANSIL 530 Dimethicone 1.00
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RHEOSOL AVH
ARISTOFLEX AVC
Sodium Polyacrylate & Ethylhexyl Stearate & Trideceth-6
Ammonium Acryloyldimethyltaurate/VP Copolymer
1.00
0.20
FEATURING GRANSIL VX-418 AND ICE CREAM REPAIR
Total: 100.00
Procedure
1. Weigh Phase A in the main kettle equipped with side sweep. Mix well.
2. Weigh Phase B in a side kettle and mix well.
3. Slowly add Phase B to Phase A with mixing.
4. Mix until homogeneous.
G1351-1938.01
NIGHT LITE REPAIR CREAM
Part Ingredient INCI Name % (wt)
A DEIONIZED WATER Water 50.60
CARBOPOL ULTREZ-10 Carbomer 0.20
POLYMER
TEA 99% Triethanolamine 0.20
PROCOL SA-21 Steareth-21 2.00
GRANSIL VX-418 Bis-Stearyl Dimethicone 20.00
GLYCERIN Glycerin 3.00
BUTYLENE GLYCOL Butylene Glycol 2.00
B GRANPOWDER USQ Polymethylsilsesquioxane & HDI/Trimethylol Hexyllactone Crosspolymer 5.00
GRANSURF 50C-HM Dimethicone & PEG/PPG-18/18 Dimethicone 1.00
GRANACTIVE RETINOID Dimethyl Isosorbide & Hydroxypinacolone Retinoate 1.00
DIMETHICONE, 5CST Dimethicone 6.00
JEECHEM GMS-165 Glyceryl Stearate & PEG-100 Stearate 1.00
PROTACHEM CS-50 Cetearyl Alcohol 2.00
C GRANSIL EP-9 Polysilicone-11 & Water & Laureth-12 & Phenoxyethanol & Ethylhexylglycerin 5.00
D EUXYL PE 9010 Phenoxyethanol & Ethylhexylglycerin 1.00
Procedure Texture Transformations Total: 100.00
1. Combine Phase A in the main kettle and heat to 70~75oC, prop mix until uniform.
FEATURING GRANSIL VX-418 AND ICE CREAM REPAIR
2. Combine Phase B in support kettle and heat to 70~75oC. Mix until uniform.
3. Add Phase B into the main kettle while mixing. Continue to mix for 15~20 minutes.
4. Add Phase C into the main kettle while mixing and mix until uniform.
5. Start cooling with side sweep.
6. Add Phase D at 40~45oC and continue to cool until 30~35oC.
G103-382.01
Contact us today to discover the ways we help ensure your product’s performance is flawless, or learn more at www.grantinc.com.
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