Kobo DeliverySystems Glycosphere

Delivery Systems
Glycospheres
Softspheres™
2/27/2018
www.koboproducts.com
Why Use Delivery Systems?
• Target certain areas of the skin

• Protect active ingredients from degradation when formulated
• Protect formula from degradation / discoloration due to active
ingredients
• Make formulation easier (ex. insoluble active)
• Reduce irritations or allergies (limit dermal penetration)
• Marketing advantages (ex. pack actives in aesthetically
pleasing, easily seen particle)
Glycospheres
Submicron Particles for Protection and Delivery
Glycospheres - Structure
Stable Porous Core Covalently Bonded Polar Lipids Layer(s)
(Quaternarized, Lipid Layer (Hydrogenated Lecithin)
Cross-linked Starch) (Fatty Acid Esters)
Hydrophilic
Lipophilic
Hydrophilic
Size: 200 nm
Suspension in Polar Solvents (Water / Glycols)
INCI : Palmitoyl Hydroxypropyl Trimonium / Glycerin Crosspolymer (And)
Hydrogenated Lecithin
Comparison with Liposomes
Liposome Glycosphere
ENCAPSULATION: ENTRAPMENT:
Non Specific Retention Specific Ionic Bonds between Actives
Possible leakage if lipid and Cationic Core
bilayer is weakened Actives stay entrapped as long as
ionic bond is stable
Entrapment : Release Mechanism
Low Ionic Strength: High Ionic Strength:

No Release Controlled Release
Low Water Content / High Ionic Strength

conditions prevail in the Stratum Corneum
Entrapment & Release Conditions (1)
Ultrafiltration (0.1µm filter)
Glycospheres ( ) ● 1 2 3
are too large to go
through the filter;
entrapped colorant
stay in the top
compartment
Filter
Filter
Non-entrapped or
released colorant
(●) goes through
the filter and 1. Non-entrapped colorant goes through the filter
moves to the 2. Colorant entrapped in Glycospheres stays in the top
bottom compartment at low ionic strength (water)
compartment
3. When salt is added to the suspension (1M NaCl),
colorant is released and moves through the filter to
the bottom compartment.
Other Entrapment Mechanism
Lipophilic molecules
are loaded within
the lipid layers
Physical Characteristics
SEM Picture (Freeze Cracking) Stability Over Time

(DLS measurement)
Time Average
S.D. (nm)
(years) Size (nm)
0 205 65
1 215 69
3½ 202 74
5 181 86
Average Size and Standard Deviation of
Lecithin layers Glycospheres in Suspension at Room
Freeze-cracked Temperature
starch core
Glycospheres are extremely stable (> 3 years at RT);

They are also stable at high temperature, low and high
pH and in presence of surfactants (data not shown)
Skin Adhesion & Penetration
• Glycospheres were tagged with a
fluorescent probe, then added to a
lotion.
• The lotion was applied to the skin.
• After 1 hour, the skin surface was
washed.
• Layers of Stratum Corneum were
stripped with an adhesive film
• Each layer was observed with a
fluorescence microscope to
determine if Glycospheres stay on
the skin after washing and how deep
Fluorescent Gs (bright white dots) in
a stratum corneum layer they penetrate.
Glycospheres only penetrate into the top layers

of the skin (0 - 15 µm)
Protection of Formulas
Entrapment and Protection of Procyanidolic Oligomers (PCOs)
Stability of PCO in Emulsion
Polyphenolic compounds. (6 months / 40°C)
Extracted from plants

(ex. grape seed, pine bark).
Extremely high free-radical

scavenging activity
Low stability (discolor over time)
After 6 months at 40°C

non-protected PCOs are
polymerized (discoloration
& low activity).
When entrapped and

protected within
Glycospheres, they remain
stable and active.
Protection of Formulas
In Vitro Tests In Vivo Activity of Formulated
NBT & DPPH PCO Dithranol Test
NBT Test DPPH Test
.-
(O2 ) (OH.)
Non-Entrapped PCO 100 467
Entrapped PCO 147 513
Non-Entrapped Vit E -27 154
Entrapped Vit E -17 149
• More active than Vitamin E (variable, depending on test method)

• Still active when entrapped
• Stable under UV Light (NBT Test)
Stabilization of Ascorbic Acid
Entrapped vs. non-entrapped

Ascorbic Acid in suspension at high
temperature (40°C / 40 days)
Gs-Vit.C Vit.C
Glycospheres stabilize Ascorbic Acid even at
high temperature
Stabilization of Papain
• Papain is an enzyme present in the

fruits of Papaya carica, the Papaya tree.
• It is a proteolytic enzyme which breaks
down proteins.
• In skin care products, it can be used to
hydrolyze stratum corneum proteins and
promote the elimination of dead skin
cells (enzymatic peeling).
• Other uses include revitalizing hair and
restoring shine, tyrosinase inhibition (in skin
whitening products), and promotion of fast
cell turnover (proteolytic activity).
Three-dimentional
structure of Papain
Proteolitic Activity and Tyrosinase Inhibition
Proteolytic Activity at 40°C Tyrosinase Inhibition at 40°C
150 120
125 100
Proteolytic activity (%)
Tyrosinase activity
100 80
75 60
50 40
25 20
0 0
0 2 4 6 8 10 12 0 10 20 30 40 50 60 70
Months Days
Papain Gs-PPY Papain Gs-PPY
The proteolytic activity in solution or entrapped in The capacity of papain to inhibit melanin synthesis by
Glycospheres was tested in vitro (on L-BAPA). deactivating tyrosinase was tested in vitro, using
Glycosphere-PPY and Papain in an aqueous solution tyrosinase and L-DOPA. Glycosphere-PPY and Papain in
(as control) were kept at 40°C and their activity was an aqueous solution (as control) were kept at 40°C and
measured regularly over a period of one year. their activity was measured regularly over a period of
two months.
Papain in solution rapidly loses its activity, but papain

protected by the Glycosphere core retains its activity over
time at elevated temperatures.
Effect of Gs-PPY on Hair Cuticle
Untreated Hair treated Hair treated with
hair with Papain solution Gs-PPY
To evaluate the effect of papain on hair cuticles, tresses were soaked in

either water, a papain solution or Gs-PPY. SEM pictures of the cuticle surfaces
were then taken. Water and papain solution treatments show rough surface
with lifted cuticles, but Gs-PPY treated hair has a smoother surface, which
should result in silky and shiny hair.
Glycospheres - Summary
• Chemically stable sub-micron particles

• Penetration limited to the first layer of the skin
• Entrapment of both hydrophilic and lipophilic actives
• Protection of labile molecules from degradation and
reaction with formulas
• Available as suspensions in either water, water and butylene
glycol, or water and glycerin
• Two preservative systems are available:
1. Phenoxyethanol (And) Parabens
2. Pentylene Glycol (And) 1,2-Hexanediol (And) Caprylyl Glycol
Examples
Trade Names Trade Names Active Ingredient Carrier
with Preserv. #1 with Preserv. #2
● Cn-HAHWS Sodium Hyaluronate Water
Cn-PS2 ● - Water
● Cn-UR1000S Urea Water
Gs-AHP ● Acetyl Hexapeptide-8 Water
Gs-BC ● Beta-Carotene Water
Gs-GT ● Green Tea Polyphenols Water
Gs-PCOg ● Grape seed PCOs Water
Gs-PPY ● Papain Water
Gs-RES ● Resveratrol Water
Gs-SA2B ● Salicylic acid Butylene Glycol + Water
Gs-VA100C ● Retinol Butylene Glycol + Water
Gs-VACE ● Ascorbic acid + Tocopherol + Retinol Butylene Glycol + Water
Gs-VC40 ● Ascorbic acid Butylene Glycol + Water
Gs-VC2500GDC Ascorbic acid Glycerin + Cyclosiloxane
Gs-VC5000 ● Ascorbic acid Glycerin + Water
Gs-VE ● Tocopherol Water
Preservatives: 1- Phenoxyethanol (And) Parabens ● Available as special order
2- Pentylene Glycol (And) 1,2-Hexanediol (And) Caprylyl Glycol
KFL-079A: Anti-Aging Mask
KFL-106B-BR: Beauty Booster Serum
KFL-107-EU – Hydra Mist
Softspheres™
Visual Impact & Delivery
Structure – Capsules (1)
Inner (liquid) material
(+ active)
Solid wall (+ pigments)
• Wall has to be solid to avoid inner material(s)

from leaking out of the capsule
• Empty capsules are still visible after breaking
on the skin
Structure – Capsules (2)
Structure - Homogeneous Gel Beads (1)
No walls : same material “inside” & “outside”
• Gel is weak enough to break and “disappear” when

beads are rubbed onto the skin
Structure - Homogeneous Gel Beads (2)
Entrapment in Gel Beads (1)
• Gel forms a matrix
• There is no wall between

“outside” and “inside”
compartments when the
bead is in water (solvent)
• Water (solvent) can flow

in/out of the bead
(although at a lower
diffusion rate)
Entrapment in Gel Beads (2)
• For the bead to be soft

enough, the matrix has
to be large
• Small molecules will

diffuse out of the matrix
(equilibrium)
• Large molecules
(polymers) will not
diffuse through the gel
matrix
Entrapment in Softspheres™ (1)
• Cationic polymer is added to

+ the composition (cannot
move)
+
• Anionic molecules form
ionic bonds with the
polymer
+
• Anionic molecules cannot

diffuse out of the beads
+
Entrapment in Softspheres™ (2)
• Softspheres™ can entrap

+ within the gel matrix
> Ionic small molecules
+ > Lipophilic products
(different polymer)
> Macromolecules
+
> Pigments
Size
• Size Range: 1.0 - 2.8 mm

• 3 « Standard » Sizes:
> a = 2.20 - 2.80 mm
> b = 1.60 - 2.20 mm
> m = 1.00 - 1.60 mm
• Stable pH 2-10, in
surfactants, at temperatures
up to 60°C*
* May vary with actual composition
Composition
• Agar-Agar
• Restraining Polymer: Polyquaternium-11
• Colorants/Pigments
• Active Ingredients/Oils/Vitamins/Fragrances/...
• Preservative systems:
1. Propylene Glycol, Imidazolidinyl Urea, Phenoxyethanol,
Parabens
2. Propylene Glycol, Pentylene Glycol, Caprylyl Glycol,
1,2-Hexanediol
Applications
Examples of active ingredients successfully entrapped in

Softspheres™
• Anionic: colorants, hyaluronic acid
• Lipophilic: tocopherol, vitamin A, natural oils, ceramides
• Macromolecules: enzymes
• Pigments: iron, titanium & zinc oxides
• Miscellaneous: emulsions, fragrances
Recommended use levels range from 2.5 to 10% depending on

the Softspheres™ diameter.
Softspheres™ - Summary
• Large Colored Beads

• Chemically Stable (pH, Temperature, Surfactants)
• Decoration of Many Different Types of Formulations
• Release Active Ingredients by Breaking under Pressure
without Leaving Residues on the Skin
Examples
Trade Names Trade Names Active Ingredient Color
with Preserv. #1 with Preserv. #2
● SpS-5coral56 Tocopheryl acetate Pearlescent Tan
● SpS-BkFeO41 - Black
Sp-AOPL41 ● Sweet Almond oil + Tocopheryl ac. Pearlescent Pink
Sp-BkFEB41 ● - Metallic Grey
Sp-JbOTiO41 ● Jojoba Oil White
Sp-SfOVEaUMDC41 ● Sunflower Seed Oil + Tocopheryl ac. Pearlescent Blue
Sp-UM41 ● - Deep Blue
Sp-VApGP41 ● Retinyl Palmitate Gold
Sp-VCTiOGH ● Magnesium Ascorbyl Palmitate Light Green
Sp-VCYOTR56 ● Tocopheryl ac. + Mg Ascorbyl Palmitate Orange
Tocopheryl Ac. + Aloe Barbadensis Leaf
Sp-VEaVAGrP41 ● Pearlescent Green
Juice
Sp-VEaDC56 ● Tocopheryl Acetate Pearlescent White
Sp-VEaTR41 ● Tocopheryl Acetate Red
All products are available in 3 sizes (suffixes a = 2.2-2.8 mm - b = 1.6-2.2 mm - m = 1.0-1.6 mm)
Preservatives: 1- Propylene Glycol, Imidazolidinyl Urea, Phenoxyethanol, Parabens

2- Propylene Glycol, Pentylene Glycol, Caprylyl Glycol, 1,2-Hexanediol
● Available as special order

KCL-019-EU – Grapefruit Shower Gel
KCL-004B:
Vitamin Rich Body Wash with Softspheres™
KFL-135C
Revitalizing Clear Serum with Softspheres™

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Delivery Systems

• Target certain areas of the skin

Low Ionic Strength: High Ionic Strength:

Low Water Content / High Ionic Strength

SEM Picture (Freeze Cracking) Stability Over Time

Glycospheres are extremely stable (> 3 years at RT);

Glycospheres only penetrate into the top layers

Extracted from plants

Extremely high free-radical

Low stability (discolor over time)

After 6 months at 40°C

When entrapped and

Non-Entrapped PCO 100 467

Entrapped PCO 147 513

Non-Entrapped Vit E -27 154

Entrapped Vit E -17 149

• More active than Vitamin E (variable, depending on test method)

Entrapped vs. non-entrapped

• Papain is an enzyme present in the

Papain Gs-PPY Papain Gs-PPY

Papain in solution rapidly loses its activity, but papain

To evaluate the effect of papain on hair cuticles, tresses were soaked in

• Chemically stable sub-micron particles

● Cn-HAHWS Sodium Hyaluronate Water

Solid wall (+ pigments)

• Wall has to be solid to avoid inner material(s)

No walls : same material “inside” & “outside”

• Gel is weak enough to break and “disappear” when

• Gel forms a matrix

• There is no wall between

• Water (solvent) can flow

• For the bead to be soft

• Small molecules will

• Cationic polymer is added to

• Anionic molecules cannot

• Softspheres™ can entrap

• Size Range: 1.0 - 2.8 mm

* May vary with actual composition

Examples of active ingredients successfully entrapped in

Recommended use levels range from 2.5 to 10% depending on

• Large Colored Beads

Preservatives: 1- Propylene Glycol, Imidazolidinyl Urea, Phenoxyethanol, Parabens

● Available as special order

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