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Delivery Systems

Delivery Systems. Delivery Systems. Targeting Protection of Active Ingredients Protection of Formulas Easier Formulation Reduction of Irritation / Allergies Marketing Advantages. Delivery Systems. Glycospheres. Microspheres. Softspheres. Millimeters. Nanometers. Microns. Delivery

yoshio-zamora
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Delivery Systems

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  1. Delivery Systems

  2. Delivery Systems • Targeting • Protection of Active Ingredients • Protection of Formulas • Easier Formulation • Reduction of Irritation / Allergies • Marketing Advantages

  3. Delivery Systems Glycospheres Microspheres Softspheres Millimeters Nanometers Microns Delivery within the skin Delivery at skin surface Visual impact & Delivery

  4. Glycospheres Nanoparticles for Protection and Delivery

  5. 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 / Glycerin Crosspolymer (And) Lecithin

  6. Comparison with Liposomes Glycosphere Liposome Entrapment : Specific Bonds Encapsulation : Non Specific Retention Possible Leakage

  7. Entrapment : Release Mechanism Low Ionic Strength : No Release High Ionic Strength : Controled Release

  8. Measurement of Retention Capacity • Solution • (non entrapment) • Released • Entrapment

  9. Lipophilic Compounds Lipophilic Molecules are loaded within the Lipid Layers

  10. Physical Characteristics Light Scattering Nanosizer (Suspension in Buffer) Electron Micrograph (Freeze Cracking)

  11. Stability Over Time Average Size and Standard Deviation of Glycospheres in Suspension at Room Temperature

  12. Protection of Formulas Entrapment and Protection of Procyanidolic Oligomers Stability of PCO in Emulsion (6 months / 40°C) Polyphenolic compounds. Extracted from plants (ex. grape seed, pine bark). Extremely high free-radical scavenging activity Low stability 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.

  13. 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)

  14. Stabilization of Ascorbic Acid Suspension : 40°C / 40 days Gs-Vit.C Vit.C

  15. Stabilization of Papain

  16. 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

  17. Examples of Finished Formulas

  18. Microspheres Delivery of Oils at Skin Surface

  19. 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

  20. 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.

  21. 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

  22. 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

  23. 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

  24. 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”

  25. Softspheres Visual Impact & Delivery

  26. Structure (1) : Capsules Inner (liquid) material (+ active) Solid wall (+ pigments) • Wall has to be solid to avoid inner material(s) to leak out of the capsule • Empty capsules are still visible after breaking on the skin

  27. Structure (2) : Homogeneous gel “beads” No walls : same material “inside” & “outside” • Gel is weak enough to break and “disappear” when beads are rubbed onto the skin

  28. 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 (1)

  29. Small molecules will diffuse out of the matrix (equilibrium) • Large molecules (polymers) will not diffuse through the gel matrix Entrapment in gel beads (2) • For the bead to be soft enough, the matrix has to be large

  30. 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 (1)

  31. + + + + Entrapment in Softspheres (2) • Softspheres can entrap within the gel matrix : • - Ionic small molecules • - Lipophilic products • (different polymer) • - Macromolecules • - Pigments • - ...

  32. Compositions • Agar-Agar • Restraining Polymer : • Colorants / Pigments • Active Ingredients / Oils / Vitamins / Fragrances / ... • Polyquaternium-11 • PG-Hydroxyethylcellulose Stearyldimonium Chloride

  33. Size • Size Range : 0.7 - 2.8 mm • 3 « Standard » Sizes : • Stable pH 2-10, in surfactants, at temperature up to 60°C * • a = 2.00 - 2.80 • b = 1.25 - 2.00 • c = 0.71 - 1.25 * May vary with actual composition

  34. Applications (1) Soap Stick Emulsions Hydrogels, shampoos

  35. Applications (2)

  36. 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

  37. Summary (1)

  38. 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 Updated 4/26/13

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