Formulation of dual eicosanoid system and cytokine system inhibitors for use in the prevention and treatment of oral diseases and conditions
The present invention provides a novel composition of matter comprised of a mixture of two specific classes of compounds—Free-B-Ring flavonoids and flavans—for use in the prevention and treatment of diseases and conditions associated with mouth, gums and teeth. This composition of matter simultaneously inhibits cyclooxygenase (COX) and lipoxygenase (LOX) enzymatic activity and reduces cytokine production at the mRNA level in normal, aged and damaged periodontal cells and tissues. This invention further provides a method for the prevention and treatment of diseases and conditions of the mouth, gums and teeth. The method for preventing and treating diseases and conditions of the mouth, teeth and gums is comprised of administering to a host in need thereof a therapeutically effective amount of a composition comprising a mixture of Free-B-Ring flavonoids and flavans synthesized and/or isolated from a single plant or multiple plants, preferably in the Scutellaria, Oroxylum, Acacia or Uncaria genus of plants and pharmaceutically and/or cosmetically acceptable carriers. Finally the present invention provides a method for the prevention and treatment of diseases and conditions of the mouth, teeth or gums, including but not limited to periodontal diseases, such as gingivitis, periodontitis, pulpitis, periodontal conditions caused by the physical implantation of oral dentures, trauma, injuries, bruxism, neoplastic and other degenerative processes; material alba, pellicles, dental plagues, calculus, and stains. Use of the composition described herein also affords the benefit of maintaining optimum saliva production and pH, minimizing bacterial growth, reducing the formation of pellicles and plague, inhibiting tooth decalcification and tooth caries (decay), promoting remineralization, which yields healthy gums, whitening teeth, maintaining healthy oral hygiene and reducing oral malodor (halitosis).
1. An oral care composition, comprising:
a mixture of a Scutellaria extract enriched for baicalin and an Acacia or Uncaria extract enriched for catechin or epicatechin or both; and a polymeric polycarboxylate;
wherein the composition is in the form of a toothpaste, gel, cream, mouthwash, chewing gum, tincture or drink.
2. The composition according to claim 1 wherein the composition further comprises a solubilizing agent and an efficacy-enhancing agent.
3. The composition according to claim 2 , wherein the efficacy-enhancing agent is selected from an anionic polymer or co-polymer comprising a delivery-enhancing group and a retention-enhancing group, wherein the delivery-enhancing group enhances delivery of a flavonoid and a flavan to oral tissue and the retention-enhancing group enhances retention of the flavonoid and the flavan by oral tissue.
4. The composition according to claim 2 , wherein the solubilizing agent is selected from an ether, a glycol, a fat, an oil, a lipid, a surfactant, an alcohol, a humectant, and mixtures thereof.
5. The composition according to claim 1 , further comprising an oral care active agent that is selected from the group consisting of: an antibacterial agent, an antimicrobial agent, an anti-caries agent, an anti-tartar agent, an anti-attachment agent, a biofilm disruption agent, an anti-inflammatory agent, an antibiotic, and mixtures thereof.
6. The composition according to claim 1 , further comprising an oral care active agent that comprises a non-ionic compound.
7. The composition according to claim 1 , further comprising an oral care active agent that comprises an active compound selected from the group consisting of: benzethonium chloride, octenidine, hexetidine, hexamidine, cetyl pyridinium chloride, chlorhexidine, alexidine, N α -cocoyl-L-arginine methyl ester, N α -cocoyl-L-arginine ethyl ester, N α -cocoyl-L-arginine propyl ester, N α -stearoyl-L-arginine methyl ester, N α -stearoyl-L-arginine ethyl ester, N α -Lauroyl arginine ethyl ester, 2′,4,4′-trichloro-2-hydroxy-diphenyl ether (triclosan), stannous ion source, fluoride ion source, zinc ion source, salts and mixtures thereof.
8. An oral care composition, comprising:
a mixture of a Scutellaria extract enriched for free-B-ring flavonoids containing primarily baicalin and an Acacia or Uncaria extract enriched for flavans containing primarily catechin or epicatechin or both; and a polymeric polycarboxylate;
wherein the composition is in the form of a toothpaste, gel, cream, mouthwash, chewing gum, tincture or drink, and wherein the free-B-ring flavonoids and the flavans are present in an amount of about 0.05% to about 25% by weight of the composition.
9. The composition according to claim 8 , wherein said mixture of free-B-ring flavonoids and flavans is formulated as a toothpaste in an amount of 0.1% to 5% by weight of the composition.
10. The composition according to claim 8 , wherein said mixture of free-B-ring flavonoids and flavans is formulated as a mouthwash in an amount of 0.2% to 1% by weight of the composition.
11. The composition according to claim 8 , wherein said mixture of free-B-ring flavonoids and flavans is formulated as an emulsion gel or cream in an amount of 0.5 to 5% by weight of the composition.