MULTIPHASIC BIOFUNCTIONAL NANO-COMPONENTS AND METHODS FOR USE THEREOF

• US 20070237800A1
• Filed: 06/15/2007
• Published: 10/11/2007
• Est. Priority Date: 11/10/2004
• Status: Active Grant

• Current Assignee: Board of Regents of the University of Michigan (University of Michigan)
• Original Assignee: Board of Regents of the University of Michigan (University of Michigan)
• Inventors: Lahann, Joerg
• Granted Patent: US 8,241,651 B2
• Time in Patent Office: Days
• US Class Current: 424/422
• CPC Class Codes: A61K 49/1854 the organic macromolecular compound being obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly(meth)acrylate, polyacrylamide, polyvinylpyrrolidone, polyvinylalcohol
• CPC Class Codes: A61K 49/1887 Agglomerates, clusters, i.e. more than one (super)(para)magnetic microparticle or nanoparticle are aggregated or entrapped in the same maxtrix
• CPC Class Codes: A61K 9/1694 resulting in granules or microspheres of the matrix type containing more than 5% of excipient
• CPC Class Codes: A61K 9/5089 Processes
• CPC Class Codes: A61K 9/5153 Polyesters, e.g. poly(lactide-co-glycolide)
• CPC Class Codes: A61K 9/70 Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug hollow drug-filled fibres A61K9/0092
• CPC Class Codes: B82Y 5/00 Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery

Abstract

Multiphasic nano-components (MPNs) having at least two phases and at least one active ingredient are provided. The MPNs can be used in various methods for medical diagnostics or with pharmaceutical, personal care, oral care, and/or nutritional compositions, for example, in oral care, hair, or skin products. The MPNs can be designed to have targeted delivery within an organism, while providing controlled release systems or combining incompatible active ingredients. Further, the MPNs can be used as biomedical coatings (such as anti-microbial coatings), or anti-corrosive coatings, bioimaging probes with combined diagnostic and therapeutic use, and fragrance release systems, among others. The MPNs can be formed by electrified jetting of polymers.

Claims

1. A multiphasic nano-component comprising a first phase and at least one additional phase distinct from said first phase, wherein said first phase and said at least one additional phase each have an exposed surface, wherein at least one of said first phase and said additional phase comprises a pharmaceutically and/or cosmetically acceptable polymer, and wherein at least one of said first phase and said additional phase comprises an active ingredient.

2. The composition according to claim 1, wherein said first phase comprises a first active ingredient and said at least one additional phase comprises a second active ingredient.

3. The composition according to claim 1, wherein said first phase comprises a first component that is incompatible with a second component present in said at least one additional phase.

4. The composition according to claim 1, wherein at least one of said exposed surfaces comprises a moiety for binding to a target associated with an animal.

5. The composition according to claim 4, wherein said moiety is selected from the group:

proteins, peptides, polysaccharides, sugars, toxins, antibodies, aptamers, and combinations thereof.

6. The composition according to claim 1, wherein at least one of said exposed surfaces is treated after formation of the nano-component to modify the chemical or physical characteristics of said surface.

7. The composition according to claim 1, wherein said first active ingredient has a first charge and a second component present in said at least one additional phase has a second charge opposite to said first charge.

8. The composition according to claim 1, wherein said first phase is hydrophobic and said at least one additional phase is hydrophilic.

9. The composition according to claim 1, wherein said active ingredient is selected from the group consisting of:

a therapeutic active ingredient, a systemic active ingredient, a chemotherapy active ingredient, a localized active ingredient, an oral care active ingredient, a nutritional active ingredient, a personal care active ingredient, a cosmetic active ingredient, a diagnostic imaging indicator agent, and combinations thereof.

10. The composition according to claim 1, wherein said nano-component is formed by an electrified jetting process and has a shape selected from the group consisting of:

spheres, rectangles, polygons, disks, toroids, cones, pyramids, rods, cylinders, and fibers.

11. The composition according to claim 1, wherein the pharmaceutically and/or cosmetically acceptable polymer comprises a polymer selected from the group consisting of:

biodegradable polymers, water soluble polymers, water dispersible polymers, water insoluble polymers, and combinations and co-polymers thereof.

12. The composition according to claim 1, wherein an amount of active ingredient present in said first phase is about 0.01% to about 90% by weight of the first phase.

14. A composition according to claim 1, wherein the pharmaceutically and/or cosmetically acceptable polymer is selected from the group consisting of:

sodium polystyrene sulfonate (PSS), polyethers, polyethylene oxide (PEO), polyethylene imine (PEI), polylactic acid, polycaprolactone, polyglycolic acid, poly(lactide-co-glycolide polymer (PLGA), polyvinylpyrrolidone, hydroxyl alkyl cellulose, hydroxypropyl methyl cellulose (HPMC), hydroxypropyl cellulose (HPC), hydroxyethyl cellulose (HEC), methyl cellulose (MC), carboxymethyl cellulose (CMC), vinyl acetate, polyvinylpyrrolidone-vinyl acetate copolymers, polyvinyl alcohol (PVA), polyacrylates, polyacrylic acid (PAA), vinylcaprolactam/sodium acrylate polymers, methacrylates, poly(acryl amide-co-acrylic acid) (PAAm-co-AA), vinyl acetate, crotonic acid copolymers, polyacrylamide, polyethylene phosphonate, polybutene phosphonate, polystyrenes, polyvinylphosphonates, polyalkylenes, carboxy vinyl polymer, cellulose acetate, cellulose nitrate, ethylene-vinyl acetate copolymers, vinyl acetate homopolymers, ethyl cellulose, butyl cellulose, isopropyl cellulose, shellac, siloxanes, polydimethylsiloxane, polymethyl methacrylate (PMMA), cellulose acetate phthalate, natural or synthetic rubber;

cellulose, polyethylene, polypropylene, polyesters, polyurethane, nylon, and copolymers, derivatives, and mixtures thereof.

15. The composition according to claim 1, wherein the active ingredient is selected from the group consisting of:

low-molecular weight molecules, quantum dots, natural and artificial macromolecules, proteins, sugars, peptides, polypeptides, proteins, amino acids, enzymes, DNA, RNA, polymers, nanoparticles, nanocrystals, growth hormones, growth factors, anti-rejection drugs, anti-inflammatory agents, analgesics, stem cell therapy agents, gene therapy agents, anti-oxidants, free radical scavengers, nutrients, co-enzymes, systemic drugs, therapeutic drugs, localized drugs, tooth whitening agents, skin whitening agents, antimicrobial agents, antibacterial agents, antibiotics, antifungal agents, anti-caries agents, anti-tartar agents, anti-plaque agents, anti-adhesion agents, desensitizing agents, anti-inflammatory agents, malodor control agents, flavoring agents, anti-aging agents, salivary stimulants, periodontal actives, depigmentation agents, skin lightening agents, reflectants, humectants, allergy inhibitors, anti-acne agents, anti-aging agents, anti-wrinkling agents, antiseptics, keratolytic agents, fresheners, healing agents, inflammation inhibitors, wound healing promoters, deodorants, antiperspirants, skin emollients, tanning agents, antifungals, depilating agents, counterirritants, non-steroidal soothing agents, anti-itch agents, poison ivy agents, poison oak agents, burn products, vitamins, cooling agents, heating agents, chelating agents, anti-psoriasis agents, anti-dandruff agents, skin conditioners, moisturizing agents, emollients, humectants, occlusive agents, skin lipid fluidizers, deodorant active agents, antiperspirant active agents, skin and/or scalp sensates, skin and/or scalp soothing and/or healing agents, astringents, opacifying agents, biocides, natural and synthetic extracts and essential oils, nutrients, enzymes, proteins, amino acids, vitamins, analgesics, sunscreen agents, UV absorbers, antioxidants, antibiotics, exfoliants, cell turnover enhancers, coloring agents, sunscreens, nourishing agents, moisture absorbers, sebum absorbers, skin penetration enhancers, colorants, pigments, dyes, flavors, fragrances, and combinations thereof.

13. The composition according to claim 13, wherein said at least one additional phase further comprises a second active ingredient present at about 0.01% to about 90% by weight of said additional phase.

16. A method of delivering an active ingredient to an animal comprising:

providing a pharmaceutically and/or cosmetically acceptable multiphasic nano-component comprising the active ingredient to an animal, wherein said multiphasic nano-component comprises a moiety that binds to a target to promote release of an active ingredient near a target region associated the animal, wherein said multiphasic nano-component comprises at least two distinct phases and comprises a pharmaceutically and/or cosmetically acceptable polymer and an active ingredient, wherein each said phase has an exposed surface and said active ingredient is released to said target region at an effective amount.

17. The method according to claim 16, wherein said at least two distinct phases of said multiphasic nano-component include a first phase and a distinct second phase, wherein said first phase has a first rate of release of said active ingredient and said second phase has a second rate of release of said active ingredient to said target region.

18. The method according to claim 16, wherein said active ingredient comprises a chemotherapy active ingredient, said target comprises an immune system cell, and said target region is malignant or cancerous tissue.

19. The method according to claim 16, wherein at least one of said exposed surfaces comprises a cloaking agent to avoid detection by the animal'"'"'s immune system.

20. A method for treating and/or preventing a physiological and/or psychological condition in an animal, the method comprising:

providing a pharmaceutically and/or cosmetically acceptable multiphasic nano-component to an animal, wherein said multiphasic nano-component comprises at least two distinct phases, including a first phase comprising a first active ingredient and a distinct second phase comprising a second active ingredient, wherein said first phase releases said first active ingredient at a first rate and said second phase releases said second active ingredient at a second rate differing from said first rate, wherein said nano-component delivers an effective amount of each of said first and said second active ingredients to a target region of the animal.