EP0369741A2
Expired / Lapsed
EP
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Cationic compositions for topical application
Assignee: Heron Therapeutics LLC
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Filing: 1989-11-14
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Granted: —
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Expires: 2009-11-14
Abstract
Abstract Cationic compositions comprise an active ingredient absorbed within a network of internal pores defined by a plurality of polymeric particles. The particles are preferably crosslinked polymeric beads having a diameter in the range from about 5 to 100 microns and a surface charge density from about 0.1 to 10 meq/gm hydrogen ion capacity. The active ingredients are released from the cationic polymer beads over time when applied to a keratinic material, typically human skin or hair. The cationic charge promotes adhesion of the beads to the keratinic material.
Inventors
- 👤 Sergio Nacht
- 👤 Richard Won
- 👤 Martin Katz
- 👤 Tai Cheng
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-26 08:53
CPC Classifications
A; A61; A61Q; A61Q19/00; A61K; A61K8/00; A61K8/02; A61K8/0241; A61K8/0279; A61K8/18; A61K8/72; A61K8/81; A61K8/8141; A61K8/8152; A61Q17/00; A61Q17/02; A61Q17/04; A61Q7/00; A61K2800/00; A61K2800/40; A61K2800/54; A61K2800/56
Claims Analysis
Total Claims: 26
Claim 1
Independent Claim
59 words
A topical composition comprising solid particles containing a network of pores open to the exterior of said particles and an impregnant retained inside said pore network, wherein the particles have a cationic surface charge sufficient to promote adhesion to keratinic materials, said particles being present in a carrier suitable for topical application and having a pH below about 6.
Claim 2
Dependent Claim
59 words
A topical composition comprising solid particles containing a network of pores open to the exterior of said particles and an impregnant retained inside said pore network, wherein the particles have a cationic surface charge sufficient to promote adhesion to keratinic materials, said particles being present in a carrier suitable for topical application and having a pH below about 6.
Claim 3
Dependent Claim
24 words
A topical composition as in claim 1, wherein the surface charge is in the range from about 0.1 to 10 meq/gm hydrogen ion capacity.
Claim 4
Dependent Claim
29 words
A topical composition as in claim 1, wherein the impregnant is selected from the group consisting of ultraviolet absorbing substances, steroids, insect repellants, retinoic acid, fragrances, minoxidil, and emollients.
Claim 5
Dependent Claim
15 words
A topical composition as in claim 1, wherein the impregnant is an ultraviolet absorbing substance.
Claim 6
Dependent Claim
148 words
A composition of matter comprising substantially non-collapsible polymeric beads, each defining a network of internal pores open to the exterior surface of said polymeric beads, wherein the exterior surface of said beads has a positive charge sufficient to promote adhesion of the polymeric beads to keratinic materials and said beads are substantially spherical in shape and have an average diameter of about 1 micron to about 100 microns, a total pore volume of about 0.01 cc/g to about 4.0 cc/g, an average surface area of about 1 m²/g to about 500 m²/g, an average pore diameter of about 0.001 micron to about 3.0 micron, a crosslinking density of at least about 10%, and a surface charge density in the range from about 0.1 to 10 meq/gm hydrogen ion capacity, wherein said beads are present in a carrier suitable for topical application and having a pH above about 6.
Claim 7
Dependent Claim
148 words
A composition of matter comprising substantially non-collapsible polymeric beads, each defining a network of internal pores open to the exterior surface of said polymeric beads, wherein the exterior surface of said beads has a positive charge sufficient to promote adhesion of the polymeric beads to keratinic materials and said beads are substantially spherical in shape and have an average diameter of about 1 micron to about 100 microns, a total pore volume of about 0.01 cc/g to about 4.0 cc/g, an average surface area of about 1 m²/g to about 500 m²/g, an average pore diameter of about 0.001 micron to about 3.0 micron, a crosslinking density of at least about 10%, and a surface charge density in the range from about 0.1 to 10 meq/gm hydrogen ion capacity, wherein said beads are present in a carrier suitable for topical application and having a pH above about 6.
Claim 8
Dependent Claim
21 words
A composition of matter according to claim 5, wherein said beads are a copolymer of 4-vinyl pyridine and ethylene glycol dimethacrylate.
Claim 9
Dependent Claim
19 words
A composition of matter according to claim 5, wherein said beads are a copolymer of 4-vinyl pyridine and divinylbenzene.
Claim 10
Dependent Claim
22 words
A composition of matter according to claim 5, whrein the beads are a copolymer of quartenized vinylbenzyl chloride and divinylbenzene or dimethylmethacrylate.
Claim 11
Independent Claim
115 words
A method for preparing a topical composition, said method comprising: (a) combining a monomer solution capable of forming a crosslinked polymer with a porogen in a first liquid phase, wherein at least a portion of the monomers carry a protonatable functionality; (b) dispensing the first liquid phase in a second liquid phase immiscible with the first liquid phase whereby droplets of the first liquid phase are formed; (c) polymerizing the monomers within the droplets to form polymeric beads, each bead having a network of internal pores open to the exterior surface of said polymeric beads; (d) recovering said polymeric beads from said liquid phases; and (e) protonating said beads to impart a positive surface charge.
Claim 12
Independent Claim
115 words
A method for preparing a topical composition, said method comprising: (a) combining a monomer solution capable of forming a crosslinked polymer with a porogen in a first liquid phase, wherein at least a portion of the monomers carry a protonatable functionality; (b) dispensing the first liquid phase in a second liquid phase immiscible with the first liquid phase whereby droplets of the first liquid phase are formed; (c) polymerizing the monomers within the droplets to form polymeric beads, each bead having a network of internal pores open to the exterior surface of said polymeric beads; (d) recovering said polymeric beads from said liquid phases; and (e) protonating said beads to impart a positive surface charge.
Claim 13
Dependent Claim
28 words
A method as in claim 9, wherein the monomers are organic-soluble and the first liquid phase is organic immiscible with water while the second liquid phase is water.
Claim 14
Dependent Claim
12 words
A method as in claim 10, wherein the monomers include vinyl pyridine.
Claim 15
Dependent Claim
28 words
A method as in claim 9, wherein the monomers are water-soluble and the first liquid phase is aqueous and the second liquid phase is a hydrophobic organic solvent.
Claim 16
Dependent Claim
15 words
A method as in claim 12, wherein the monomers include water quaternized acrylates and methacrylates.
Claim 17
Dependent Claim
17 words
A method as in claim 9, wherein the beads are protonated by washing in an acidic medium.
Claim 18
Dependent Claim
14 words
A method as in claim 9, wherein the porogen is an active topical ingredient.
Claim 19
Dependent Claim
30 words
A method as in claim 15, wherein the active topical ingredient is selected from the group consisting of ultraviolet absorbing substances, steroids, insect repellants, retinoic acid, fragrances, minoxidil, and emollients.
Claim 20
Dependent Claim
26 words
A method as in claim 9, further comprising: extracting the porogen from the beads; and absorbing an active topical ingredient into the pores of the beads.
Claim 21
Dependent Claim
30 words
A method as in claim 17, wherein the active topical ingredient is selected from the group consisting of ultraviolet absorbing substances, steroids, insect repellants, retinoic acid, fragrances, minoxidil, and emollients.
Claim 22
Independent Claim
46 words
A method of preparing a topical composition, said method comprising infusing an active topical ingredient into preformed porous polymeric particles, wherein said particles are characterized by a positive charge on their surface, said positive charge being sufficient to promote adhesion of the particles to keratitnic materials.
Claim 23
Independent Claim
46 words
A method of preparing a topical composition, said method comprising infusing an active topical ingredient into preformed porous polymeric particles, wherein said particles are characterized by a positive charge on their surface, said positive charge being sufficient to promote adhesion of the particles to keratitnic materials.
Claim 24
Independent Claim
68 words
A method for topically applying an active ingredient to a keratinic material, said method comprising applying to said keratinic material a topical composition comprising polymeric particles, each defining a network of internal pores open to an exterior surface, wherein the exterior surface has a positive charge sufficient to promote adhesion of the particles to the keratinic material, and an impregnant comprising said active ingredient retained in said pores.
Claim 25
Independent Claim
68 words
A method for topically applying an active ingredient to a keratinic material, said method comprising applying to said keratinic material a topical composition comprising polymeric particles, each defining a network of internal pores open to an exterior surface, wherein the exterior surface has a positive charge sufficient to promote adhesion of the particles to the keratinic material, and an impregnant comprising said active ingredient retained in said pores.
Claim 26
Dependent Claim
17 words
A method of use according to claim 20, wherein said active ingredient is an ultraviolet absorbing substance.
References Cited (Backward Citations)
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