# US 9,750,697 B2 · Delivery of an active material

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- Number: US 9,750,697 B2
- Document ID: US9750697B2
- Status: Granted
- Kind: B2
- Application number: 14/234,944
- Filed: 2012-07-27
- Published: 2014-10-16
- Granted: 2017-09-05
- Earliest claimed: 2011-07-27
- Assignees: Sisaf Limited
- Applicants: Roghieh Saffie-Siebert; Nasrollah Torabi-Pour
- Inventors: Roghieh Saffie-Siebert; Nasrollah Torabi-Pour
- Web page: https://patentgrep.com/patent/US9750697B2

## CPC

- A61K 9/1611: {Inorganic compounds}
- A61K 8/0279: {Porous; Hollow}
- A61K 8/25: Silicon; Compounds thereof
- A61K 8/671: {Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal}
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 31/07: Retinol compounds, e.g. vitamin A (retinoic acids A61K31/203)
- A61Q 19/00: Preparations for care of the skin
- A61K 2800/56: Compounds, absorbed onto or entrapped into a solid carrier, e.g. encapsulated perfumes, inclusion compounds, sustained release forms
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS

## Abstract

A composition for use as a topical delivery system for an active material is provided, the composition comprising a plurality of skin cell removal particles and a plurality of active material molecules, at least some of the skin cell removal particles each carrying at least one active material molecule, wherein carrying of an active material molecule by a skin cell removal particle maintains activity of the active material molecule. A topical delivery system for an active material, and a method of topical delivery of an active material are also provided.

## Claims

### Claim 1

A composition comprising a plurality of skin cell removal particles and a plurality of active material molecules,
wherein the skin removal particles comprise at least one elemental silicon particle,
wherein the elemental silicon particle has a jagged outer surface,
wherein at least some of the skin cell removal particles each carry at least one active material molecule, and
wherein carrying of at least one active material molecule by a skin cell removal particle stabilizes an activity of the at least one active material molecule.

### Claim 2 (depends on 1)

The composition of claim 1, wherein at least some of the skin cell removal particles comprise one or more pores, wherein at least one active material molecule is disposed in at least some of the pores.

### Claim 3 (depends on 1)

The composition of claim 1, wherein at least some of the skin cell removal particles comprise a hollow shell, wherein at least one active material molecule is disposed in at least some of the hollow shells.

### Claim 4 (depends on 1)

The composition of claim 1, wherein the at least one active material molecule is detachably fixed onto an external surface of a skin cell removal particle.

### Claim 5 (depends on 1)

The composition of claim 1, wherein the at least one active material molecule is detachably linked to a skin cell removal particle.

### Claim 6 (depends on 1)

The composition of claim 1, wherein the at least one active material molecule is carried by a delivery vehicle molecule, and wherein at least one delivery vehicle molecule is carried by a skin cell removal particle.

### Claim 7 (depends on 6)

The composition of claim 6, wherein the delivery vehicle is one or more delivery vehicles selected from the group consisting of lipid-based materials, polymer-based materials, liposomes, niosomes, polymers, dendrimers, emulsions, collagen, ceramides, cholesterol and cyclodextrin.

### Claim 8 (depends on 1)

The composition of claim 1, wherein the carrying of at least one active material molecule by a skin cell removal particle maintains one or more activities of the active material molecule selected from the group consisting of maintaining stability of the active material molecule, maintaining solubility of the active material molecule, improving solubility of the active material molecule, and increasing partitioning of the active material molecules.

### Claim 9 (depends on 1)

The composition of claim 1, wherein the active material molecule is one or more molecules selected from the group consisting of vitamins, moisturizing agents, anti-UV agents, anti-inflammatory agents, anti-oxidants, free radical scavengers, anti-seborrhoeic agents, keratolytic agents, refreshing agents, melanoregulators, liporegulators, anti-ageing agents, anti-bacterial agents, vascular protectors, anti-fungal agents, skin conditioners, immunomodulators, nutrients, essential oils, retinoids, anaesthetics, vaccines, antigens and anti-bodies.

### Claim 10 (depends on 1)

A topical delivery system for an active material comprising a composition according to claim 1.

### Claim 11

A method for topical delivery of an active material comprising
applying a composition to a portion of skin, wherein the composition comprises a plurality of skin cell removal particles and a plurality of active material molecules,
wherein at least some of the skin cell removal particles each carry at least one active material molecule,
wherein carrying of at least one active material molecule by a skin cell removal particle maintains activity of the at least one active material molecule;
working the composition against the portion of skin to remove stratum corneum cells;
dissociating the active material molecules from the skin cell removal particles; and
delivering the active material molecules to sub-corneum skin layers.

### Claim 12 (depends on 11)

The method of claim 11, wherein working the composition against the skin removes substantially all stratum corneum cells of the skin portion providing a gap which allows the active material molecules to reach sub-corneum skin layers.

### Claim 13 (depends on 11)

The method of claim 11, wherein working the composition against the skin removes some layers of stratum corneum cells of the skin portion which allows the active material molecules to penetrate through remaining layers of stratum corneum cells of skin portion to sub-corneum skin layers.

### Claim 14 (depends on 11)

The method of claim 11, wherein working the composition against the skin to remove some layers of stratum corneum cells of the skin portion decreases the packing density of the remaining layers of stratum corneum cells enabling pores of the skin to increase in diameter and allowing the active material molecules to penetrate through the remaining layers of stratum corneum cells by transport thereof through the pores.

### Claim 15 (depends on 11)

The method of claim 11, wherein working the composition against the skin to remove some layers of stratum corneum cells of the skin portion decreases the packing density of the remaining layers of stratum corneum cells causing spacing of the cells and allowing the active material molecules to penetrate through the remaining layers of stratum corneum cells by penetration between the cells.

### Claim 16 (depends on 1)

The composition of claim 1, wherein the skin cell removal particles further comprises one or more particles selected from the group consisting of porous silicon, porous crystal, porous germanium, porous diamond, porous gold, porous ceramic, and porous boron.

### Claim 17 (depends on 1)

The composition of claim 1, wherein the skin cell removal particles comprise about 0.01 to 50 wt % of the composition.
