METHOD AND PROCESS FOR THE PRODUCTION OF MULTI-COATED RECOGNITIVE AND RELEASING SYSTEMS

• US 20080226684A1
• Filed: 03/12/2008
• Published: 09/18/2008
• Est. Priority Date: 03/12/2007
• Status: Active Grant

• Current Assignee: Board of Regents of the University of Texas System (University of Texas System)
• Original Assignee: Board of Regents of the University of Texas System (University of Texas System)
• Inventors: Peppas, Nicholas A.
• Granted Patent: US 9,155,703 B2
• Time in Patent Office: Days
• US Class Current: 424/401
• CPC Class Codes: A61K 2800/10 General cosmetic use
• CPC Class Codes: A61K 2800/413 Nanosized, i.e. having sizes below 100 nm
• CPC Class Codes: A61K 2800/546 Swellable particulate polymers
• CPC Class Codes: A61K 2800/56 Compounds, absorbed onto or entrapped into a solid carrier, e.g. encapsulated perfumes, inclusion compounds, sustained release forms
• CPC Class Codes: A61K 2800/592 Mixtures of compounds complementing their respective functions
• CPC Class Codes: A61K 2800/77 Perfumes having both deodorant and antibacterial properties
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 38/28 Insulins
• CPC Class Codes: A61K 38/43 Enzymes; Proenzymes; Derivatives thereof
• CPC Class Codes: A61K 8/0245 Specific shapes or structures not provided for by any of the groups of A61K8/0241
• CPC Class Codes: A61K 8/042 Gels
• CPC Class Codes: A61K 8/11 Encapsulated compositions
• CPC Class Codes: A61K 8/73 Polysaccharides
• CPC Class Codes: A61K 8/733 Alginic acid; Salts thereof
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
• CPC Class Codes: A61K 9/1676 having a drug-free core with discrete complete coating layer containing drug adsorbates of liquid drug formulations on inert powders without simultaneous granulation step A61K9/141; with further drug-free outer coating A61K9/5078; drug conjugated to non-active particles A61K47/6921
• CPC Class Codes: A61K 9/209 containing drug in at least two layers or in the core and in at least one outer layer
• CPC Class Codes: A61K 9/5073 having two or more different coatings optionally including drug-containing subcoatings
• CPC Class Codes: A61K 9/5084 Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs tablets containing such a mixture A61K9/2077
• CPC Class Codes: A61K 9/5123 Organic compounds, e.g. fats, sugars
• CPC Class Codes: A61K 9/5138 : obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/5161 : Polysaccharides, e.g. alginate, chitosan, cellulose derivatives; Cyclodextrin
• CPC Class Codes: A61K 9/7084 : Transdermal patches having a drug layer or reservoir, and one or more separate drug-free skin-adhesive layers, e.g. between drug reservoir and skin, or surrounding the drug reservoir; Liquid-filled reservoir patches
• CPC Class Codes: A61Q 1/02 : Preparations containing skin colorants, e.g. pigments preparations in powder form A61Q1/12
• CPC Class Codes: A61Q 1/06 : Lipsticks
• CPC Class Codes: A61Q 1/08 : for cheeks, e.g. rouge
• CPC Class Codes: A61Q 1/10 : for eyes, e.g. eyeliner, mascara
• CPC Class Codes: A61Q 13/00 : Formulations or additives for perfume preparations essential oils or perfumes per se C11B9/00
• CPC Class Codes: A61Q 15/00 : Anti-perspirants or body deodorants deodorisation of air A61L9/00
• CPC Class Codes: A61Q 19/00 : Preparations for care of the skin
• CPC Class Codes: A61Q 19/10 : Washing or bathing preparations
• CPC Class Codes: A61Q 5/02 : Preparations for cleaning the hair

Abstract

The present invention includes compositions, methods, systems and kits for the controlled delivery of an active agent within a polymeric network upon the binding of a molecule that decreases the structural integrity of the polymeric network at one or more micro- or nanovacuoles.

Claims

1. A molecule-imprinted reversible polymeric network composition comprising:

a polymer comprising one or more micro- or nanovacuoles or pores, wherein the nanovacuoles recognize a specific molecule and wherein the subsequent presence and binding with the molecule creates reversible internal stresses that rupture the polymeric network at the micro- or nanovacuoles, wherein the polymer swells less than 20% of the volume of the dried polymer in a solvent alone.

2. The composition of claim 1, wherein the polymer comprises a micromolecular system, a hydrogel, a gel or a composite.

3. The composition of claim 1, wherein the polymer swells between 2-18%, 4-16%, 5-15% and 7-12% of the volume of the dried polymer in a solvent alone.

4. The composition of claim 1, wherein the polymer swells between 5 and 15% of the volume of the dried polymer in a solvent alone.

5. The composition of claim 1, wherein rupture of the polymeric network is due to:

osmosis upon the presence and binding of the molecule leading to rupture due to swelling;

change of the solubility of the polymeric network leading to polymer dissolution;

local temperature changes leading to expansion of the polymeric network and combinations thereof.

6. The composition of claim 1, wherein the composition is loaded with one or more active agents to form an active agent-loaded, molecule-imprinted network.

7. The composition of claim 6, wherein the active agent-loaded, molecule-imprinted network is adapted for pharmaceuticals, medical agents, food components, detergents, bleaches, fabric softeners, fragrances, cosmetic products, air fresheners, room deodorant devices, perfumed substrates, perfumed plastics and pet collars.

8. The composition of claim 6, wherein the active agent-loaded, molecule-imprinted network is adapted for food and cosmetic applications that use hydrocolloids as imprinting carriers for polymers of high molecular weight, wherein the hydrocolloids are extracted from plants, seaweeds or animal collagen, produced by microbial synthesis, and comprise polysaccharides, proteins and combinations thereof.

9. The composition of claim 6, wherein the molecule-imprinted network is imprinted in a carbohydrate polymer of glycosidic type mono-sugar repeative units, galactomannans, pectins, alginates, carrageenans and xanthan gum that are linear or branched, neutral or anionic and combinations thereof.

10. The composition of claim 6, wherein the active agent-loaded, molecule-imprinted network is adapted for household products selected from laundry care;

paper products;

specialty cleaners (chlorinated cleaners, scouring pads, effervescent toilet bowl cleaner powders);

air fresheners and combinations thereof.

11. The composition of claim 6, wherein the active agent-loaded, molecule-imprinted network is adapted for personal care selected from hair care (shampoos, hair mousses, styling agents);

skin care (body lotions, vitamin, aloe vera);

bath products (moisture-triggered release products);

body powders;

toilet soap (milled or poured, ionic strength-triggered release) and combinations thereof.

12. The composition of claim 6, wherein the active agent-loaded, molecule-imprinted network is adapted for cosmetics and treatment products selected from lipstick;

eye-liner;

foundation;

base;

blush;

mascara;

eye shadow;

lip liner;

facial powder;

consealer;

facial cream;

make-up remover;

mascara remover;

make-up;

skin treatments and combinations thereof.

13. The composition of claim 6, wherein the active agent-loaded, molecule-imprinted network is adapted for compositions that deliver a fragrance selected from cologne;

perfume;

sampling;

antiperspirant;

deodorant;

anti-dandruff shampoos;

athlete foot products and combinations thereof.

14. The composition of claim 6, wherein the active agent-loaded, molecule-imprinted network is further encapsulated.

15. The composition of claim 6, wherein the active agent-loaded, molecule-imprinted network is encapsulated and comprises a surfactant, a bleaching agent, a corrosion inhibitor, a sudsing modifier, a fluorescent whitening agent, one or more enzymes, an anti redeposition agent, a color, a fragrance, one or more additives and combinations thereof.

16. The composition of claim 6, wherein the active agent is released upon a change in solubility, pressure, a pH shift, a change in temperature, a temperature increase, enzymatic breakdown, diffusion and combinations thereof.

17. The composition of claim 6, wherein the polymeric recognitive network is formed into one or more layers.

18. The composition of claim 6, wherein the polymeric recognitive network is formed into one or more layers, each of which recognizes one or more different molecules and each of which provides a barrier to the release of one or more different active or inert agents or both.

19. The composition of claim 6, wherein the polymeric recognitive network is formed into a sphere, film, planar, semi-spherical, cylinder, rod, hemispheres, conical, hemi-cylinders and combination thereof.

20. The composition of claim 6, wherein the polymeric recognitive network is at least partially porous.

21. An active agent-loaded, molecule-imprinted polymeric network comprising:

two or more active agent loaded, aggregated polymeric or gel nanoparticles or microparticles comprising micro- or nanovacuoles or micro- or nanopores previously imprinted with one or more pre-determined molecules and wherein the micro or nanoparticles are coated with one or more layers, wherein the pre-determined molecules can recognized and bind specifically to the micro- or nanovacuoles or micro- or nanopores and contact with the pre-determined molecule creates internal stresses that rupture the network at the micro- or nanovacuoles or micro- or nanopores thereby releasing one or more active agents loaded into the active agent-loaded, molecule-imprinted polymeric network, wherein the polymer swells less than 20% of the volume of the dried polymer in a solvent alone.

22. The network of claim 21, wherein the polymeric recognitive network is formed into one or more layers, each of which recognizes a different molecule, releases a different active agent or both.

23. The network of claim 21, wherein the polymer swells between 2-18%, 4-16%, 5-15% and 7-15% of the volume of the dried polymer in a solvent alone.

24. The network of claim 21, wherein the polymer swells between 5 and 15% of the volume of the dried polymer in a solvent alone.

25. A method of making a recognitive release system with limited swelling upon exposure to solvent alone comprising:

selecting one or more molecules for imprinting;

forming micro- or nano-vacuoles in a polymeric recognitive network about the one or more molecules, wherein a monomer is selected to form a polymer that swells less than 20% of the volume of a dried polymer upon exposure to solvent alone;

removing the molecule from the micro- or nano-vacuoles in the polymeric recognitive network; and

drying the polymeric recognitive network, wherein the polymer swells less than 20% of the volume of the dried polymer in the presence of solvent alone.

26. The method of claim 25, further comprising the step of coating one or more active agents with a polymeric recognitive network, wherein the one or more active agents release upon contact by the polymeric recognitive network with its cognate molecule.

27. The method of claim 25, wherein the polymeric recognitive network is formed about a core.

28. The method of claim 25, wherein the polymeric recognitive network is coated into multiple layers.

29. The method of claim 25, wherein the polymeric recognitive network is coated by a Wurster coating method.

30. The method of claim 25, wherein the polymeric recognitive network is further encapsulated in a capsule, caplet, softgel, gelcap, suppository, film, granule, gum, insert, pastille, pellet, troche, lozenge, disk, poultice or wafer.

31. The method of claim 25, wherein the polymeric recognitive network is formed into one or more layers, each of which recognizes one or more different molecules and each of which provides a barrier to the release of one or more different active or inert agents or both.

32. The method of claim 25, wherein the polymeric recognitive network is formed into a sphere, film, planar, semi-spherical, cylinder, rod, hemispheres, conical, hemi-cylinders and combination thereof.

33. The method of claim 25, wherein the polymeric recognitive network is at least partially porous.

34. A method of making a polymeric recognitive network comprising:

selecting one or more targets for recognition;

forming micro- or nano-vacuoles in the polymeric recognitive network about the one or more targets;

embedding within the polymeric recognitive network one or more active agents for release upon dissociation of the polymeric recognitive network; and

removing the targets from the micro- or nano-vacuoles,

wherein subsequent binding of the target to the micro- or nano-vacuoles causes disruption of the polymeric recognitive network and release of the one or more active agents, and wherein the polymer is selected such that it swells less than 20% of the volume of the dried polymer in the presence of solvent alone.

35. A method of loading an active agent in a molecule-imprinted network comprising:

mixing the active agent to the molecule-imprinted network at or about room temperature;

heating the mixture to about 40°

C. to swell the molecule-imprinted network, wherein the active agent diffuses into the molecule-imprinted network; and

cooling the mixture to about room temperature, wherein the molecule-imprinted network collapses and traps the active agent within the molecule-imprinted network.

36. The method of claim 35, wherein the active agent-loaded, molecule-imprinted network is adapted for pharmaceuticals, medical agents, food components, detergents, bleaches, fabric softeners, fragrances, cosmetic products, air fresheners, room deodorant devices, perfumed substrates, perfumed plastics and pet collars.

37. The method of claim 35, wherein the active agent-loaded, molecule-imprinted network is adapted for food and cosmetic applications that use hydrocolloids as imprinting carriers for polymers of high molecular weight, wherein the hydrocolloids are extracted from plants, seaweeds or animal collagen, produced by microbial synthesis, and comprise polysaccharides, proteins and combinations thereof.

38. The method of claim 35, wherein the molecule-imprinted network comprises a carbohydrate polymer of glycosidic type mono-sugar repeative units, galactomannans, pectins, alginates, carrageenans and xanthan gum that are linear or branched, neutral or anionic and combinations thereof.

39. The method of claim 35, wherein the active agent-loaded, molecule-imprinted network is further coated or encapsulated.

40. The method of claim 35, wherein the active agent-loaded, molecule-imprinted network is encapsulated and comprises a surfactant, a bleaching agent, a corrosion inhibitor, a sudsing modifier, a fluorescent whitening agent, one or more enzymes, an anti redeposition agent, a color, a fragrance, one or more additives and combinations thereof.

41. The method of claim 35, wherein the active agent is released upon a change in solubility, pressure, a pH shift, a change in temperature, a temperature increase, enzymatic breakdown, diffusion and combinations thereof.

42. The method of claim 35, wherein the polymeric recognitive network is formed into one or more layers.

43. The method of claim 35, wherein the polymeric recognitive network is formed into one or more layers, each of which recognizes one or more different molecules and each of which provides a barrier to the release of one or more different active or inert agents or both.

44. The method of claim 35, wherein the polymeric recognitive network is formed into a sphere, film, planar, semi-spherical, cylinder, rod, hemispheres, conical, hemi-cylinders and combination thereof.

45. The method of claim 35, wherein the polymeric recognitive network is at least partially porous.

46. A kit for making a polymeric recognitive network comprising:

one or more targets for recognition by the polymeric recognitive network;

monomers for forming a polymeric recognitive network comprising micro- or nano-vacuoles about the one or more targets;

a polymeric catalyst for forming the polymeric recognitive network about the targets; and

instructions for polymerizing the polymeric recognitive network and removing the targets from the micro- or nano-vacuoles and loading of the polymeric recognitive network with one or more active agents.