 | Glycosphere |
Solid and stable particulate delivery systems. They are derived from the concept of Supramolecular Biovector technology patented in 1988, and have been adapted for the transport and protection of active agents in the upper layers of the epidermis.
1. Glycosphere Structure :
| Glycospheres are supramolecular configurations organized around of solid inner core. The latter, consisting of modified starch, is powerfully hydrophilic and endows the particle with its chemical and physicochemical stability, its excellent biocompatibility, | its ability to entrap or encapsulate hydrophilic active agents and, by virtue of its very small size(200 nanometers), its capacity of penetration of the uppermost layers of the stratum corneum. A single layer of fatty acids is grafted covalently at the periphery of this central core, endowing the particle with a peripheral lipophilic nature, without modifying its internal hydrophilic nature. The glycosphere can thus organize polar lipids and hence retain and vectorize liophilic active agents. |
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| ENTRAPMENT: SPECIFIC BONDS |
2. Entrapment
Both hydrophilic and lipophilic active agents can be incorporated to glycospheres. Two different types of chemical interactions play a role in their capacity to retain molecules : Ionic bonds and hydrophobic interactions.
1) Mechanism
2) Entrapment of hydrophilic actives
The central core of Glycospheres, consisting chiefly of starch, contains strongly cationic groups. Anionic hydrophilic actives are thus retained by high energy inonic bonds. Entrapment stability and performance are thus incomparably greater than with any other delivery systems.
3) Incorporation of lipophilic actives
The potent cohesion existing between the lipid layer and polar lipids arranged at the periphery of Glycospheres enables loading with amounts of lipophilic actives.
4) Entrapement of maccromolecules
Macromolecules such as enzymes can be entrapped within the inner hydrophilic core, thanks to the large mesh size of its structure. Proteins of molecular weight up to 200, 000 daltons have been successfully stabilized in Glycospheres.
5) Entrapment Stability
entrapment of ionic molecules is particularly stable thanks to ionic bonds created between the central core of Glycospheres and the active ingredient molecule. In the example below, all the entrapped active remains in the particle at low ionic strength; when ionic strength is increased by addition of salt, the ionic bond is split and the active released.
3. Stability of Glycosphere
1) Vitamin C
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2) PCO(Procyanidolic Oligomers from Grape seeds)
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3) Enzyme(Papain)
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4. Applications of Glycosphere
1)Hydrophilic : Natural anti-oxidants (Grape seed, Green tea, Oak gall), Vitamins, Amino-Acids, Plant extracts ...
2)Lipophilic : Tocopherol, Vitamin A, Ceramides & Polar Lipids...
3)Macromolecules : Enzymes(Glucose Oxidase, Papain), Proteins, Hyaluronic Acid, Natural Polymers ...
