Method For Producing Cs Particles And Microcapsules Using Porous Templates, Cs Particles And Microcapsules, And the Use Thereof

• US 20080020051A1
• Filed: 03/16/2005
• Published: 01/24/2008
• Est. Priority Date: 03/19/2004
• Status: Active Grant

• Current Assignee: Surflay Nanotec GmbH
• Original Assignee: Capsulution Pharma AG
• Inventors: Dahne, Lars, Baude, Barbara
• Granted Patent: US 7,939,103 B2
• Time in Patent Office: Days
• US Class Current: 424/490
• CPC Class Codes: A61K 9/5073 having two or more different coatings optionally including drug-containing subcoatings
• CPC Class Codes: A61K 9/5078 with drug-free core
• CPC Class Codes: B01J 13/02 Making microcapsules or microballoons for medical preparations A61K9/50
• CPC Class Codes: Y10T 428/2991 Coated

Abstract

A process for the production of CS particles (10) and microcapsules (12) is described, in which at least one active compound (4) is adsorbed in porous templates (2) (A), as a result of which templates (5) filled with active compounds are present. Subsequently, the templates (2) are provided (B) with a primer layer (6) which is intended to facilitate the subsequent construction of the capsule shell (9). The capsule shell is formed (C) by applying alternately charged polyelectrolyte layers (8). Filled CS particles (10) are obtained. By subsequent dissolution of the templates (2) the active compounds (4) are released (D) from the template into the interior of the microcapsules. The active compounds (4) remain enclosed there or are slowly released (E) from the capsule.

Claims

1-22. -22. (canceled)

23. A method for the production of core-shell (CS) particles and/or microcapsules, comprising:

preparing porous templates, the templates being porous organic and/or inorganic microparticles having a diameter of less than 100 μ

m;

adsorbing in the porous templates at least one active compound to be encapsulated;

applying at least one primer layer to the porous templates; and

forming a capsule shell around the porous templates provided with the primer layer by applying coating materials comprising at least one of alternately charged polyelectrolyte layers and nanoparticle layers to the porous templates, wherein the primer layer is formed from a material which closes pores of the porous templates and is largely impermeable to the coating materials applied in the formation of the capsule shell.

24. The method as claimed in claim 23, wherein the pores have a pore width of 0.3 nm-100 nm and preferably of 1 nm-30 nm.

25. The method as claimed in claim 23, wherein the templates comprise at least one of porous silica particles, porous zeolite particles, and porous polystyrene particles.

26. The method as claimed in claim 25, wherein the porous silica particles range in size from 100 nm to 100 μ

m and preferably from 500 nm to 30 μ

m.

27. The method as claimed in claim 25, wherein the porous zeolite particles have a pore width of 0.3 nm to 10 nm.

28. The method as claimed in claim 23, wherein the at least one active compound to be encapsulated comprises at least one of a polymer, a protein, an organic molecule having a molecular weight of over 100 g/mol, a nanoparticle, an enzyme, a catalyst, a dye, a pharmaceutical or cosmetic active compound, and a plant protection agent.

29. The method as claimed in claim 23, wherein at least one auxiliary is used for mediating the adsorption of the at least one active compound.

30. The method as claimed in claim 23, wherein poly-electrolytes and/or nanoparticles are used as the at least one active compound and wherein a surface of the pores is coated by a number of layers of alternately charged poly-electrolytes and/or nanoparticles.

31. The method as claimed in claim 29, wherein the porous templates are prepared in a solution and, additionally or alternatively to the auxiliary, the adsorption of the at least one active compound is controlled by changing the pH of the solution.

32. The method as claimed in claim 23, further comprising dissolving the porous templates after formation of the capsule shell to form the microcapsules.

33. The method as claimed in claim 25, further comprising dissolving silica and/or zeolite templates by fluoride salts in the presence of a buffer solution having a pH between 3.5 and 6.

34. A core-shell (CS) particle having:

a diameter of less than 100 μ

m;

a porous core in which at least one active compound is adsorbed;

a primer layer which surrounds the porous core; and

a capsule shell comprising a number of layers alternately charged polyelectrolyte and/or nanoparticle layers, wherein the primer layer comprises a material which closes pores of the porous core and is largely impermeable to the layers of the capsule shell.

35. The CS particle as claimed in claim 34, wherein the pores of the porous core have a pore width of 0.3 nm-100 nm and preferably of 1 nm-30 nm.

36. The CS particle as claimed in claim 34, wherein the core comprises a porous organic and/or inorganic microparticle having a diameter less than 100 μ

m.

37. The CS particle as claimed in claim 34, wherein the core comprises at least one of a porous silica particle, a porous zeolite particle, and a porous polystyrene particle.

38. The CS particle as claimed in claim 34, wherein the core comprises a porous silica particle ranging in size from 100 nm to 100 μ

m and preferably from 500 nm to 30 μ

m.

39. The CS particle as claimed in claim 34, wherein the core comprises a porous zeolite particle having a pore width of 0.3 nm to 10 nm.

40. The CS particle as claimed in claim 34, wherein the at least one active compound comprises at least one of a protein, a polymer, an enzyme, a catalyst, a dye, and a nanoparticle.

41. A microcapsule having:

a diameter of less than 100 μ

m;

a capsule shell comprising a number of layers of alternately charged polyelectrolyte and/or nanoparticle layers;

a primer layer on the inside of the capsule shell; and

an inner framework of polyelectrolyte complexes and/or polyelectrolyte/nanoparticle complexes, which is surrounded by the primer layer and the capsule shell.

42. The microcapsule as claimed in claim 41, wherein the primer layer and the capsule shell comprise different materials.

43. A method for the production of microcapsules, comprising:

preparing at least one porous template, the template being a porous organic and/or inorganic microparticle having a diameter of less than 100 μ

m;

coating the surface of pores of the porous template with a number of layers of alternately charged poly-electrolytes and nanoparticles.

applying at least one primer layer to the porous template;

forming a capsule shell around the porous template provided with the primer layer by applying coating materials comprising at least one of alternately charged polyelectrolyte and nanoparticle layers to the porous template, the primer layer being formed from a material which closes the pores of the porous template and is largely impermeable to the coating materials applied during the formation of the capsule shell; and

dissolving the porous template.