Delivery Systems

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Delivery Systems
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Delivery Systems

• Targeting
• Protection of Active Ingredients
• Protection of Formulas
• Easier Formulation
• Reduction of Irritation / Allergies
• Marketing Advantages

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Delivery Systems
Skin Care Patches
Glycospheres
Microspheres
Softspheres
Microns
Nanometers
Millimeters
(Matrix)
Delivery within the skin
Delivery at skin surface
Visual impact Delivery
Controlled delivery over time
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Glycospheres
Nanoparticles for Protection and Delivery
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Glycospheres
Inside
Solid Core (Cross-linked Modified
Starch) Covalently Bonded Lipid Layer (Fatty
Acid Esters) Polar Lipids Layer(s) (Hydrogenated
Lecithin)
Hydrophilic
Lipophilic
Hydrophilic
200 nanometers
Outside
Suspension in Polar Solvents (Water /
Glycols) INCI Palmitoyl Hydroxypropyl Trimonium
Amilopectin / Glycerin Crosspolymer (And)
Lecithin
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Comparison with Liposomes
Glycosphere
Liposome
Entrapment Specific Bonds
Encapsulation Non Specific Retention Possible
Leakage
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Entrapment Release Mechanism
Low Ionic Strength No Release
High Ionic Strength Controlled Release
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Lipophilic Compounds
Lipophilic Molecules are loaded within the
Lipid Layers
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Physical Characteristics
Light Scattering Nanosizer (Suspension in Buffer)
Electron Micrograph (Freeze Cracking)
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Stability Over Time
Average Size and Standard Deviation of
Glycospheres in Suspension at Room Temperature
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Protection of Formulas
Entrapment and Protection of Procyanidolic
Oligomers
Stability of PCO in Emulsion (6 months / 40C)
Polyphenolic compounds. Extracted from
plants (ex. grape seed, pine bark). Extremely
high free-radical scavenging activity Low
stability
After 6 months at 40C non protected PCOs are
polymerized (discoloration low activity). When
entrapped and protected within Glycospheres, they
remain stable and active.
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Protection of Formulas
In Vitro Tests NBT DPPH
In Vivo Activity of Formulated PCO Dithranol Test

• Much More Active than Vitamin E (Variable,
  Depending on Test Method)
• Still Active when Entrapped
• Stable under UV Light (NBT Test)

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Stabilization of Ascorbic Acid
Suspension 40C / 40 days
Gs-Vit.C
Vit.C
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Stabilization of Papain
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Protection of Active Ingredients

• Chemicaly stable submicronic particles
• Entrapment of both hydrophilic and lipophilic
  actives
• Protection of labile molecules from degradations
  (reaction with formulas, oxidation, light, ....)
• Possible coentrapment of hydrophilic and
  lipophilic compounds

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Examples of Finished Formulas
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Microspheres
Delivery of Oils at Skin Surface
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Porous Silica Microspheres

• The chemical and physical properties of the
  particles determine their ability to absorb oils

• Silica is hydrophilic but can absorb oil
• Particles with high porosity are best for oil
  absorption
• Silica Microspheres can be treated to alter their
  affinity for liquids Methicone, Methoxy
  Amodimethicone/Silsesquioxane Copolymer

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Structure

• Porous silicas are rigid particles that become an
  integral part of the cosmetic film on the skin.

• Contrary to some polymeric absorbents, silicas do
  not change size when empty or full, thus
  maintaining the integrity of the film.

• Because they are rigid, they will not release the
  oil with pressure as some polymers can.

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MSS-500/3H
Silica
Highly-Porous Spherical Silica
Particle Size 3 µm Surface Area 700
m2/g Pore Volume 2 ml/g Pore Size 250 Å Oil
Absorption 290 ml/100g
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Silica Shells
Silica
Clusters of porous silica
Particle Size 3 µm Surface Area 120
m2/g Pore Volume 0.2 ml/g Pore Size 17-3000
Å Oil Absorption 700 ml/100g
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Silica Shells-SH
Silica (And) Methoxy Amodimethicone/Silsesquioxane
Copolymer
Amino Silicone Surface Treatment

• Amino Silicone-treated Silica Shells are
  hydrophobic they are easier to formulate in oil
  phases.

Particle Size 3 µm Oil Absorption 550
ml/100g
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Summary - Added Benefits

• Absorb and deliver oils
• Microspheres are also used to reduce the look of
  fine lines (Optical Blurring)
• Microspheres enhance the feel of formulas they
  can produce special tactile effect such as
  Cream-to-Powder

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Softspheres
Visual Impact Delivery
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Large Delivery Systems
Capsules
Porous beads
Non-homogeneous Leave residues (wall) when
rubbed on the skin after breaking
Homogeneous material When soft enough, do not
leave residues
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Agar-Agar Beads
To make Particles Soft Enough
Low Agar Content
Active Ingredient
Agar Network
Large Mesh Size
Small Molecules (actives) are Washed Away from
the Agar Beads
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Use of a Restraining Copolymer
Cationic Amphiphilic Copolymer Added to the
Agar Matrix
Copolymer Too Large to be Washed Away from the
Agar Network
Copolymer
Ionic Hydrophobic Interactions with Actives
Stable Entrapment Better Feel
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Compositions

• Agar-Agar
• Restraining Polymer
• Colorants / Pigments
• Active Ingredients / Oils / Vitamins / Fragrances
  / ...

• Polyquaternium-11
• PG-Hydroxyethylcellulose Stearyldimonium Chloride
  

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Size

• Size Range 0.7 - 2.8 mm
• 3  Standard  Sizes
• Stable pH 2-10, in surfactants, at temperature
  up to 60C

• a 2.00 - 2.80
• b 1.25 - 2.00
• m 0.71 - 1.25

May vary with actual composition
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Applications (1)
Soap
Stick
Emulsions
Hydrogels, shampoos
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Applications (2)
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Visual Impact Delivery

• Large Colored Beads
• Chemically Stable (pH, Temperature, Surfactants)
• Decoration of Many Differents Types of
  Formulations
• Release Active Ingredients by Breaking under
  Pressure without Leaving Any Residues on the Skin

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Skin Care Patches
Controlled Delivery
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Skin Care Patches

• Deliver a wide range of active ingredients
• Control the release of active ingredients
• High efficacy compared to skin care formulas
• Simple application
• Available in many shapes and sizes

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Matrix Structure Composition

• Lipophilic Matrix
• Hydrogels

• Long lasting effect for long term use (overnight)
• Acrylates Copolymers
• Butyl Methacrylate
• Methyl Methacrylate Crosspolymer

• Short term use (10-30 min)
• Hydrophilic gelling agents (ie Carrageenans)

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Skin Penetration
Constant release of active ingredients
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Applications

• Lipophilic Matrix
• Hydrogels
• Customer Service

• Anti-aging eye patches Glycosphere-Vit. C,
  Vitamin A E
• Anti-Acne Salicylic Acid, plant extracts
• Whitening Arbutin, Kojic Acid, Gs-VC

• Refresh eye patches Botanical Extracts,
  Ascorbyl Phosphate, AHAs

• Custom manufacture Shape, Active Ingredients
• Pouch Printing Labelling

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Summary (1)
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Summary (2)

• Enhance efficacy of active ingredients due to a
  better skin penetration
• Enhance stability against oxidation and UV light
• Enhance solubility
• Easier to formulate

.... for Optimum Efficiency