APPARATUS AND METHOD FOR PREPARING COSMECEUTICAL INGREDIENTS CONTAINING EPI-DERMAL DELIVERY MECHANISMS

• US 20170181937A1
• Filed: 03/15/2017
• Published: 06/29/2017
• Est. Priority Date: 12/16/2015
• Status: Active Grant

• Current Assignee: PPP&C Inc.
• Original Assignee: PPP&C Inc.
• Inventors: Richard, David A.
• Granted Patent: US 10,322,073 B2
• Time in Patent Office: Days
• CPC Class Codes: A61K 2800/70 Biological properties of the composition as a whole
• CPC Class Codes: A61K 2800/805 Corresponding aspects not provided for by any of codes A61K2800/81 - A61K2800/95
• CPC Class Codes: A61K 8/06 Emulsions
• CPC Class Codes: A61K 8/14 Liposomes; Vesicles
• CPC Class Codes: A61K 8/416 Quaternary ammonium compounds A61K8/35 takes precedence
• CPC Class Codes: A61K 8/553 Phospholipids, e.g. lecithin
• CPC Class Codes: A61K 8/63 Steroids; Derivatives thereof
• CPC Class Codes: A61K 8/735 Mucopolysaccharides, e.g. hyaluronic acid; Derivatives thereof
• CPC Class Codes: A61K 8/9789 Magnoliopsida [dicotyledons]
• CPC Class Codes: A61Q 19/00 Preparations for care of the skin
• CPC Class Codes: A61Q 19/08 Anti-ageing preparations

Abstract

The skin serves as a barrier that protects the body from the external environment and prevents water loss. This barrier function also prevents most hydrophilic or hydrophobic and large molecular weight ingredients (>500 kDa) from penetrating intact skin. Until recently, methods to increase stratum corneum permeability were generally not effective enough to make the stratum corneum so permeable that the barrier posed by the viable epidermis mattered. However, that has now changed with the development of the present embodiment'"'"'s physical methods and highly optimized chemical formulations, such that we revisited the permeability of the full epidermis with the example embodiment'"'"'s constructs and not focus only on the stratum corneum. This example embodiment therefore tests the hypothesis that the viable epidermis offers a significant permeability barrier to both small molecules and macromolecules that becomes the rate limiting step.

Claims

1. A method for the construction of cosmeceutically bioactive compositions including liposome or elastic niosome vesicle epi-dermal delivery vehicles, the method comprising:

forming a solution or mixture of cosmeceutically benevolent phospholipids, the solution being a hydrophobic or hydrophilic, natural or synthetic ingredient, with an aqueous phase;

removing any constituent attributes of water-insolubility from the solution, while operating under mild conditions to preserve the activity of the labile biomolecules, the constituents of the solution that are either lipids or polymers all having in common that a final arrangement is governed by the nature of the initial components and a methodology used in their preparation;

loading the solution of the membrane lipid or niosome components and desired hydrophobic bio-actives into an organic solvent residing in a pressure reactor, the pressure reactor having been previously driven to a proper working temperature;

pressurizing the reactor with a large amount of compressed CO2 until reaching the proper low working pressure; and

depressurizing the resulting CO2-expanded solution over an aqueous phase to form vesicular conjugates, the resulting solution containing water soluble cationic or non-ionic surfactants and hydrophilic or hydrophobic bio-actives.

2. The method of claim 1 wherein the vesicle content is one of natural or synthetic cosmetic ingredients used for treating or correcting a therapeutic effect of the skin surface and epi-dermal layers to be beneficial including hydration, skin lightening, anti-wrinkle, skin smoothing, antioxidant activity/free radical scavenger, anti-inflammatory/anti-irritant, collagen stimulation, cell regeneration/stimulation, sebum regulation, anti-cellulite, antimicrobial, acne(s) and antibacterial results.

3. The method of claim 1 wherein the vesicle contains naturally derived cosmetic beneficial ingredients that originate from plants, herbs, roots, flowers, fruits, leaves or seeds, such as:

aloe vera, almond oil, avocado oil, coconut oil, hazelnut oil, jojoba oil, olive oil, palm oil, pumpkin seed oil, sesame oil, sunflower oil, tamanu oil, candeia oil, arnica, chamomile, oat extract, hibiscus flower, boswellia serratta, cocoa powder, green and white tea, gotu kola, chamomile extract, L-arginine, glutamine, pantothenic acid, white willow bark extract, tetrahydrocurcuminoids, alpha-arbutin, aloesin, alpha glucosyl hesperidin, niacinimide, fucoidan, magnesium asorbyl phosphate, azelaic acid, N-acetyl-D-glucosamine, glutathione, mulberry, pomegranate seed oil, cyprus rotund root extract, licorice, licorice-glabrin root extract, kojic acid, panax ginseng root extract, ginko bilbao, salicylic acid, Lauric acid, glycerin, caffeine, tocopheryl acetate, copper peptide, retinyl palmitate, asorbyl palmitate, wakame, dimethylethanolamine, beta glucan, triglyceride as well as hyaluronic acid (Hyaluronic acid is a natural and sugar-like biopolymer in the human body that alternately consists of D-glucuronic acid and N-acetyl-D-glucosamine-units).

4. The method of claim 1 wherein the elastic vesicles contain a cosmetically and topically effective active agent, and a cosmetically acceptable carrier or diluent.

5. The method of claim 1 wherein the elastic vesicles contain a pharmaceutically and topically effective active agent, and a pharmaceutically acceptable carrier or diluent.

6. The method of claim 4 wherein the active agent is lipid soluble and is present in the elastic vesicle wall or membrane.

7. The method of claim 4 wherein the active agent is water or oil soluble and is encapsulated within the elastic vesicle walls.

8. The method of claim 1 wherein a vesicle-forming lipid is solubilized in a hydrophilic pharmaceutically acceptable solvent other than water.

9. The method of claim 1 wherein a penetration enhancer is added to a solubilized vesicle forming lipid.

10. The method of claim 1 wherein said elastic vesicles further comprise a biologically active agent in entrapped form.

11. The method of claim 1 wherein a therapeutic agent is lipophilic and is added to the lipophilic phase of said emulsion.

12. The method of claim 1 further including preparing liposomes having a central core compartment containing an oil-in-water emulsion, preparing an oil-in-water emulsion which is stabilized by a surfactant, solubilizing an elastic vesicle-forming lipid in a pharmaceutically acceptable solvent other than water, adding the oil-in-water emulsion to the solubilized vesicle-forming lipid, and mixing to form liposomes having a lipid-bilayer membrane composed of a vesicle-forming lipid and containing the oil-in-water emulsion in the central core compartment.

13. The method of claim 1 wherein a sterol is selected from the group consisting of cholesterol, cholesterol derivatives, and mixtures thereof.

14. The method of claim 1 wherein a lipid vesicle comprises an oil.

15. The method of claim 14 wherein the oil is selected from the group consisting of castor oil, soybean oil, squalene oil, squalane oil, sesame oil, olive oil, canola oil, corn oil, rapeseed oil, safflower oil, sunflower oil, fish oils, avocado oil, water insoluble vitamins, and mixtures thereof.

16. The method of claim 1 wherein the elastic vesicles are paucilamellar lipid vesicles having nonionic amphiphiles as their major structural component consisting of 2-8 lipid bilayers.

17. The method of claim 1 including making unilamellar lipid vesicles comprised of short-chain phospholipids and long-chain phospholipids.

18. The method of claim 17 wherein the short-chain phospholipids are comprised of fatty acids with fewer than 9 carbons atoms and the long-chain phospholipids are comprised of fatty acids with at least 12 carbon atoms.