Substantially surfactant-free, submicron dispersions of hydrophobic agents containing high levels of water miscible solvent

• US 9,357,770 B2
• Filed: 03/14/2014
• Issued: 06/07/2016
• Est. Priority Date: 03/15/2013
• Status: Active Grant

• Current Assignee: Leading Edge Innovations, Llc
• Original Assignee: Leading Edge Innovations, Llc
• Inventors: Wilmott, James Michael, Ross, Michael Alan
• Primary Examiner(s): Shomer, Isaac
• Application Number:
  US14/211,562
• Publication Number:
  US 20140271877A1
• Time in Patent Office: 816 Days
• Field of Search: None
• US Class Current: 1/1
• CPC Class Codes: A01N 25/04 Dispersions, emulsions, suspoemulsions, suspension concentrates or gels foams A01N25/16
• CPC Class Codes: A01N 31/08 Oxygen or sulfur directly attached to an aromatic ring system
• CPC Class Codes: A01N 55/00 Biocides, pest repellants or attractants, or plant growth regulators, containing organic compounds containing elements other than carbon, hydrogen, halogen, oxygen, nitrogen and sulfur containing organo-phosphorus compounds A01N57/00
• CPC Class Codes: A01N 65/08 Magnoliopsida [dicotyledons]
• CPC Class Codes: A61K 2800/244 Endothermic; Cooling; Cooling sensation
• CPC Class Codes: A61K 2800/28 Rubbing or scrubbing compositions; Peeling or abrasive compositions; Containing exfoliants
• CPC Class Codes: A61K 2800/33 Free of surfactant
• CPC Class Codes: A61K 2800/413 Nanosized, i.e. having sizes below 100 nm
• CPC Class Codes: A61K 2800/48 Thickener, Thickening system
• CPC Class Codes: A61K 8/0212 Face masks
• CPC Class Codes: A61K 8/0241 Containing particulates characterized by their shape and/or structure see also A61K8/04, A61K8/11, and A61K8/14, further aspects are classified in A61K2800/40 and subcodes
• CPC Class Codes: A61K 8/04 Dispersions; Emulsions
• CPC Class Codes: A61K 8/042 Gels
• CPC Class Codes: A61K 8/25 Silicon; Compounds thereof
• CPC Class Codes: A61K 8/345 containing more than one hydroxy group
• CPC Class Codes: A61K 8/4946 Imidazoles or their condensed derivatives, e.g. benzimidazoles
• CPC Class Codes: A61K 8/73 Polysaccharides
• CPC Class Codes: A61K 8/8152 Homopolymers or copolymers of esters, e.g. (meth)acrylic acid esters; Compositions of derivatives of such polymers
• CPC Class Codes: A61K 8/891 saturated, e.g. dimethicone, phenyl trimethicone, C24-C28 methicone or stearyl dimethicone
• CPC Class Codes: A61K 8/922 of vegetable origin
• CPC Class Codes: A61Q 13/00 : Formulations or additives for perfume preparations essential oils or perfumes per se C11B9/00
• CPC Class Codes: A61Q 17/005 : Antimicrobial preparations
• CPC Class Codes: A61Q 19/00 : Preparations for care of the skin
• CPC Class Codes: A61Q 19/007 : Preparations for dry skin
• CPC Class Codes: A61Q 19/10 : Washing or bathing preparations
• CPC Class Codes: A61Q 9/02 : Shaving preparations
• CPC Class Codes: Y10S 977/773 : Nanoparticle, i.e. structure having three dimensions of 100 nm or less
• CPC Class Codes: Y10S 977/906 : Drug delivery

Abstract

A composition is provided to apply to the skin, hair, or external mucosa of a human or animal, and a method for using the composition. The composition includes for example a composition for application to skin, hair or external mucosa comprising: a) dispersed submicron particles of hydrophobic agent(s) having average particle size from 100 nm to 999 nm; b) an aqueous-solvent fluid; and c) rheological modifying agent(s); wherein the aqueous-solvent fluid is 10% to 95% wt. of one or more water miscible solvent(s), 4.99% to 89.99% wt. water, and 0.01% to 10% wt. of the rheological modifying agent(s); and wherein the hydrophobic agents comprise 0.01 to 70% wt. of the skin, hair or mucosal composition; and wherein the composition is substantially surfactant-free.

Claims

1. A composition for application to skin, hair or external mucosa comprising:

an aqueous-solvent fluid and submicron particles of hydrophobic agent(s) of average particle size from 100 nm to 999 nm dispersed and suspended in the aqueous-solvent fluid, wherein the submicron particles are 90% wt. or more non-polar, wherein 85% or more of the submicron particles have a size within 300 nm of the average particle size;

wherein the aqueous-solvent fluid comprises

30% to 95% wt. of one or more water miscible solvent(s),

4.99% to 70% wt. water, and

0.01% to 10% wt. of one or more rheological modifying agent(s);

wherein 70% wt. or more of the one or more water miscible solvents, and 30% wt. or more of the aqueous-solvent fluid, is one or more mono- or di-hydroxy compounds selected from the group consisting of C₂ or C₃ alcohols, propylene glycol, butylene glycol or pentylene glycol;

wherein the hydrophobic agent(s) comprise 0.01 to 70% wt. of the skin, hair or mucosal composition;

wherein the composition is substantially surfactant-free, wherein the amount of surfactant, if present, is not sufficient to materially lower the surface tension of the aqueous-solvent fluid; and

wherein the dispersed submicron particles are stable.

2. The composition of claim 1, wherein 80% weight or more of the water miscible solvent is one or more of said mono- or di-hydroxy compounds.

3. The composition of claim 1, wherein the composition is formulated as a moisturizing hand sanitizer, and wherein the composition comprises about 50% to 90% by weight ethanol or isopropanol.

4. The composition of claim 1, wherein the composition is formulated as a cooling cologne, and wherein the composition comprises about 50% to 90% by weight ethanol.

5. The composition of claim 1, wherein the composition is formulated as a body lotion, and wherein the composition comprises 30% to 80% wt. of said one or more water miscible solvent(s).

6. The composition of claim 1, wherein the composition is formulated as an exfoliating mask, and wherein the composition comprises 30% to 80% wt. of one or more of said one or more water miscible solvent(s).

7. The composition of claim 1, formulated as a lubricating shaving gel or cream.

8. The composition of claim 1, wherein the hydrophobic agent(s) comprises one or more therapeutic agent(s).

9. The composition of claim 1, wherein the hydrophobic agent(s) comprises at least one aesthetic modifying agent.

10. The composition of claim 1, wherein the hydrophobic agent(s) comprise one or more therapeutic agent(s) and at least one aesthetic modifying agent(s).

11. The composition of claim 1, further comprising one or more of a therapeutic agent(s), selected from the group consisting of anti-acne agents, antimicrobial agents, anti-inflammatory agents, analgesics, anti-erythemal agents, anti-pruritic agents, anti-edemal agents, anti-psoriatic agents, anti-fungal agents, skin protectants, sunscreen agents, vitamins, antioxidants, scavengers, anti-irritants, anti-bacterial agents, antiviral agents, antiaging agents, photoprotection agents, hair growth enhancers, hair growth inhibitors, hair removal agents, antidandruff agents, anti-seborrheic agents, exfoliating agents, wound healing agents, anti-ectoparasitic agents, sebum modulators, immunomodulators, hormones, botanicals, moisturizers, astringents, sensates, antibiotics, anesthetics, steroids, tissue healing substances, tissue regenerating substances, amino acids, peptides, minerals, ceramides, biohyaluronic acids, and bleaching ingredients.

12. The composition of claim 1, further comprising at least one therapeutic agent, which comprises at least one sunscreen agent selected from the group consisting of ethylhexyl methoxycinnamate, avobenzone, benzophenones, octocrylene, ethylhexyl salicylate, homomenthyl salicylate, triethanolamine salicylate, menthyl anthranilate, PABA, octyl dimethyl PABA, 2-ethoxyethyl p-methoxycinnamate, phenylbenzimidazole sulfonic acid, titanium dioxide and zinc oxide.

13. The composition of claim 9, wherein said the one or more aesthetic modifying agent comprises at least one compound selected from the group consisting of

(a) a compound having the formula C_pH_(2p+2q) wherein p is a positive integer greater than or equal to 6 and q is 0 or a positive, even integer no greater than p;

(b) a compound having the formula B or C

14. The composition of claim 9, wherein said aesthetic modifying agent comprises at least one compound selected from the group consisting of polysiloxanes, cyclic siloxanes, polyalkylsiloxanes, polyarylsiloxanes, polyalkylarylsiloxanes, polysiloxane gums and polyethersiloxane copolymers.

15. The composition of claim 1, wherein 90% or more of the one or more water miscible solvent(s) is (i) is one or more of said mono- or di-hydroxy compounds.

16. The composition of claim 1, wherein the submicron particles have an average particle size in the range between about 100 nm to about 500 nm.

17. The composition of claim 1, wherein the submicron particles have an average particle size in the range between about 150 nm to about 500 nm.

18. The composition of claim 9, wherein the one or more aesthetic modifying agents comprises one or more of C2-C26 alkyl substituted with 2-24 hydroxyls, wherein the hydroxyls of the foregoing compounds are independently acylated with a saturated, unsaturated, linear, branched or cyclic C1-C24 alkane, rendering the substituted alkyls hydrophobic agents.

19. The composition of claim 1, wherein said one or more mono- or di-hydroxy compounds are selected from the group consisting of ethanol, isopropanol, propylene glycol, butylene glycol, and pentylene glycol.

20. A method of applying one or more therapeutic agent(s) to skin, hair or external mucosa comprising applying to the skin, hair, or external mucosa of a human or animal the composition of claim 8.

21. A method of imparting a desirable tactile, olfactory, or visual property to a skin, hair, or mucosal surface of a human or animal comprising applying to the skin, hair, or mucosal surface a composition of claim 9.