HYACTIVE
very low molecular weight sodium salt of hyaluronic acid
An active ingredient of biotechnological origin for the cosmetic industry
PRODUCT DESCRIPTION
Hyaluronic acid (HA) is a linear polysaccharide built from regularly alternating units of glucuronic acid and N-
acetylglucosamine.
The degree of polymerisation is in the order of 102 to 103 units. This implies that molecular weight is in the range
from tens of thousand up to several hundred thousand Daltons. HA is the most hydrated biopolymer known (see
booklet - SMW Hyaluronic Acid). In living tissue it serves as a water reservoir. In water solutions, HA molecules give
rise to spherically coiled structures nesting about 99% of immobilised water. Due to the polyanionic nature of HA, its
properties are very sensitive to pH and to the ionic strength of the solution. Since HA is normally found in the body, it
is free of immunogenic activity. HA forms cellular coats and it is a normal component of blood lymph and connective
tissue.
Trade name: HyActive
Chemical name: poly(sodium-β-D-glucuronate-[1-3]- β-N-acetyl-D-glucosamine-[1-4])
Other names: sodium hyaluronate, hyaluronan, hyaluronic acid
CAS No: 9067-32-7
INCI name: Sodium Hyaluronate
EINECS/ELINCS: 232-678-0
Structural formula:
Source: HyActive is produced by fermentation. As a starting material we use Hyaluronic acid with
low molecular weight, which is split by a controlled combination of different physical
methods to desired molecular weight.
As the combination of biotechnological and physical methods is used to produce HyActive,
the product is free of contaminants such as glycosaminoglycans and proteins of animal
origin. GMO’s are not used during the production process.
Solubility: • dissolves rapidly in water.
• soluble in mixtures of water with ethylalcohol, isopropylalcohol, propylene glycol and
butylene glycol at the concentration of organic solvent up to 70%
• insoluble in non-water miscible solvents
Compatibility and processing:
HyActive solution is
• relatively stable. Only small changes in molecular weight occur while heating at extreme
pH values.
• very sensitive to free radicals
• incompatible with cationic substances, e.g quaternized polymers or proteins
(Quaterniums, Polyquaterniums, etc.)
Toxicological data: • non-irritating
• non-cytotoxic
• non-phototoxic
• non-mutagenic
Supplied forms: powder
Specification:
HyActive, powder
Appearance: white to slightly yellow powder or granules
Appearance of 1% aqueous solution clear to slightly opalescent, colourless solution
Clarity of 1% aqueous solution (660 nm, 1cm) < 0,01
pH of 1% aqueous solution: 5,0-8,0
Residue on drying: > 90,0 %
Ash: < 10,0 % calc. on dry basis
Uronic acid (UA): > 45,0 % calc. on dry basis
Sodium hyaluronate: > 93,0 % calc. on dry basis
Protein: < 0,2 % calc. on dry basis
Preservatives: none
Total microbial count: < 100 CFU/g
Molecular weight: 10-20 kDa *
* most commonly used range of molecular weight
HyActive can be supplied with any molecular weight in the range of 10-150 kDa.
USE IN COSMETICS
Daily skin care 0.01 - 0.20%
Night and reparative preparations 0.02 - 0.20%
After sun 0.02 - 0.50%
Pre-shaves/After shaves 0.005 - 0.05%
EFFICACY DATA
ANTI-AGEING
A 24 hours-treatment of HaCaT cultures with 24 kDa
HyActive (500 µg/ml) stimulates gene expression of
epidermal growth factor and hyaluronan synthase-2. At the
same time, gene expression of matrix matelloproteinases 1
and 3 is decreased.
A 48 hours-treatment of keratinocyte cultures with 12.7 kDa
HyActive (1000 µg/ml) stimulates gene expression of tissue
metalloproteinase inhibitor 1 in addition to hyaluronan
synthase-2.
Due to its relatively small molecule, HyActive is able to
penetrate stratum corneum. A 14 day-treatment of skin in
vivo with 12 kDa HyActive showed reduced gene expression
of hyaluronidase-1 and increased expression of serine
protease inhibitor (Kazal-type 5), which protects desmosome
junctions in deeper epidermal layers from proteolysis and
premature desquamation.
On the molecular level, HyActive stimulates β-gluco-
cerebrosidase activity within the stratum corneum in vivo,
even after skin irradiation with UVB/UVA light. Ceramides
released from their glucosylated precursors are incorporated
into lipidic bilayers between corneocytes and strenghten the
epidermal barrier function.
After 21 days of pretreatment (1% HyActive, 37 kDa), skin
areas were irradiated with 1.5 MED (UVA+UVB). Next day,
β-glucocerebrosidase activities were determined by the tape
stripping method. Pretreatment by HyActive prior to the skin
UV-irradiation stimulated the enzyme activity in contrast to
untreated skin.
Elasticity improvement after a long-term application of HyActive
When the skin is submitted to a sudden and sustained strain under conditions of elasticity measurement (Corneometer
SEM 575), three successive phases of skin deformation are found: purely elastic phase I, phase II with variable creep
and phase III with constant creep. Elderly skin shows low elastic phase (low parameters R5 and R7) and considerable
creep phases (high parameters R6 and R8).
A long-term application of HyActive shows a decrease of
elasticity parameter R8, thus, the skin is more flexible in
comparison to control preparation without HyActive.
EPIDERMAL RENEWAL AND INTEGRITY SUPPORT
A long-term application of HyActive in vivo results in
accelerated stratum corneum turnover, which was estimated
by the measurement of decreased colour intensity of
dihydroxyacetone-stained skin surface.
HyActive significantly accelerated corneocyte shedding even
after several days of treatment.
After a 20-day treatment period, sizes of corneocyte
aggregates collected from skin surfaces of volunteers were
estimated by direct laser measurement (Ankersmid CIS-
100). Their aggregation is displayed in distribution curves,
where percentages of total corneocyte area are calculated
for separated ranges of corneocyte sizes. The lower area
under the curve, the less of large aggregates were present in
stripped stratum cornemum samples.
Data collected from volunteers show lower areas under
curves corresponding to skin sites treated with HyActive
in comparison to their controls, which confirms lesser
corneocyte sizes and lowered aggregation in the skin treated
with HyActive.
Such effect can only be obtained by stimulation of proteolytic reactions in superficial layer of stratum corneum, which
leads to the disruption of corneocyte bindings. In conclusion, long-term application of HyActive results in accelerated
desquamation. In contrast to AHA, which causes invasive desquamation or even peeling, the effect of HyActive is
gentle, and dermally safe. Final cosmetics preparations containing HyActive can be used in daily cosmetics without any
risk of skin irritation.
HyActive stimulates desquamation only in superficial layers
of stratum corneum while deeper epidermal layers keep
unchanged integrity. Cohesivity of stratum corneum was
tested by stripping after 21 days of HyActive application.
Total protein content was measured in the third to eighth
strip.
After treatment period, when old and abnormally thickened
corneocyte scales peel off, more cohesive layers of new
corneocytes with more regular run of desquamation appear.
Decreased protein content in deeper strips confirms this
hypothesis, as well as represents the evidence of unaffected desquamation in these layers.
The effect of HyActive lies in normalizing of superficial stratum corneum desquamation, which is down-regulated
predominantly in elderly skin.
OXIDATIVE STRESS REDUCER
Changes of UV-induced catalase activities in the presence of 1% HyActive in vivo
Catalase is an enzyme eliminating hydrogen peroxide generated in tissue upon oxidative stress. After skin irradiation
with UV light, its activity is initially suppressed. Only after several hours enzyme activity reaches the original level and
then increases.
The skin of volunteers was treated for 21 days with 37 kDa
HyActive and then irradiated by UVA/UVB (1,5 MED). 24
hours later, an increase in the catalase activity over control
was found in the HyActive treated skin by tape stripping
method, which means a better ability of skin to resist free
radicals.
CPN spol. s r.o.
Dolní Dobrouč 401
561 02 Dolní Dobrouč
Version: E-01/2006
Czech Republic
T: +420 465 520 035
F: +420 465 524 098
[email protected]
www.hyaluronan.cz
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AND
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