Tagra Biotechnologies Ltd.

Yury Shapiro

Emma Kvitnitsky

Vladimir Babtsov

Valery Belakhov

Olga Privalov

Irena Oleinik

Igor Polisher

Emma Kvitnitksy

The present invention provides methods for microencapsulation of active ingredients for topical application, whereby double-layer and triple-layer microcapsules are obtained. The microcapsules protect the active ingredients, maintain their original activity throughout processing, formulation and storage, and enable controlled release of the active ingredient only upon application onto the skin.

Method of microencapsulation

Novel derivatives of ascorbic acid and compositions comprising them are provided. The novel derivatives are of the following general formula (I): where R1 is a C2&#x2013;C22 saturated or unsaturated fatty acid residues, amino acid residues, or a C1&#x2013;C17 alkyl ; R2 is a group of the following formula (II) wherein R5 or R6 are the same or different and represent hydrogen, a C1&#x2013;C4 alkyl, or R5 is C1&#x2013;C4 alkyl group and R6 is a metal cation or ammonium cation; R3 or R4 are the same or different and represent hydrogen, C2&#x2013;C22 saturated or unsaturated fatty acid residues, amino acid residues, or a C1&#x2013;C17 alkyl.

Stabilized derivatives of ascorbic acid-3-phosphate

A method for microencapsulation of substances is provided. The substance(s) is/are dissolved or dispersed in an organic solvent of the kind that is partially miscible in water media. This organic solution is then mixed with an aqueous solution, which is saturated with an organic solvent and an emulsifier to form an emulsion. The emulsion is then poured into water under continuous agitation for the extraction of residual solvent. The formation of the solid capsules takes place during this extraction process. The capsules are undergone to further purification, whereby the microcapsules can be separated from the water and dried. By conditions of incubation of microcapsules in water-containing formulations the wall-softening process takes place. The unique system for controlled releasing the ingredients from microcapsules is based on the above-mentioned process.

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Giv′at-Shmuel, Israel

Yury Shapiro