The Procter Gamble Company

Summit Innovation Labs LLC

The Procter & Gamble

Ghebre Egziabher Tzeghai

David Frederick Swaile

Christine Marie Putman

Eric John Bretzler, Deceased

Satyanarayana Majeti

Curtis Bobby Motley

Gerald John Guskey

Paul D Leis, Jr

The invention encompasses compositions and methods for effectively treating and/or preventing diabetes and/or obesity. This is accomplished by totally addressing the multiple mechanisms that lead to such conditions. The invention includes compositions comprising a combination of agents that effectively suppress, regulate or interfere with the various biochemical processes and mechanisms that lead to diabetes and obesity. The inventive compositions used for administration to human and other mammalian subjects comprise (1) at least one agent capable of modulating expression and/or activity of one or more of peroxisome activated protein receptor gamma (PPAR-&#x3b3;), CAAT/enhancer binding protein-&#x3b1; (C/EBP&#x3b1;) and Sterol Regulatory Element-Binding Protein (SREBP-1); (2) at least one agent capable of activating Wnt/&#x3b2;-catenin pathway; (3) at least one agent capable of activating the adenosine monophosphate-activated protein kinase (AMPK) signaling pathway; (4) at least one agent that inhibits the activity of pro-oxidants including reactive nitrogen species and reactive oxygen species (ROS); (5) at least one agent that suppresses one or more of inflammatory mediators including interleukins IL-1&#x3b1;, IL-1&#x3b2;, IL-6, NF-&#x3ba;B, TNF-&#x3b1;, matrix metalloproteinases (MMPs) and prostaglandin E2 (PGE2); (6) at least one agent capable of enhancing glucose transporter (GLUT4) and/or inhibiting glucose transporter GLUT2; (7) at least one agent that induces the expression of and/or activates adiponectin and (8) at least one agent that induces the expression of and/or activates sirtuin (SIRT1). The active agents for use herein are natural materials such as phytonutrients, vitamins and minerals. Compositions with combinations of such natural agents have the ability to prevent, reduce or treat diabetes and obesity by (a) clearing glucose and fatty acids from blood, (b) reducing the number of adipose cells and fat storage, (c) interfering with fat, glucose, and cholesterol biosynthesis, and (d) promoting fat and glucose oxidation. Since the present compositions are aimed toward normalizing metabolism and energy expenditure and managing oxidative stress and inflammation, they are also beneficial in relation to physical activity, in particular performance, endurance, fatigue and recovery during intensive and continuous exercise/exertion.

Treatment and prevention of diabetes and obesity

The invention encompasses compositions and methods for effectively interfering, reducing and preventing conversion of vascular smooth muscle cells (VSMCs) and circulating stem cells to osteoblastic bone-like cells, thereby reducing and/or preventing vascular calcification (VC) or calcium mineral (hydroxyapatite) deposition in the vasculature. The severity and extent of calcification in the major arteries reflect atherosclerotic plaque burden and strongly predict cardiovascular morbidity and mortality. The present inventive compositions used for administration to human and other mammalian subjects comprise select actives that inhibit, interfere or regulate the biochemical processes leading to such calcification and include (1) at least one agent that modulates expression and/or activity of peroxisome activated protein receptor gamma (PPAR-&#x3b3;); (2) at least one agent that inhibits expression and/or suppresses activity of one or more of the osteogenic transcription factors (Cbf&#x3b1;1/Runx2, Osterix, Msx2) and &#x3b2;-catenin signaling; (3) at least one agent that inhibits expression and/or suppresses activity of one or more of bone morphogenetic proteins (BMPs: BMP 2 and 4), alkaline phosphatase (ALP), and osteocalcin; (4) at least one agent that inhibits the activity of Reactive Oxygen Species (ROS); and (5) at least one agent that suppresses one or more of inflammatory mediators including interleukins IL-1&#x3b1;, IL-1&#x3b2;, IL-6, NF-&#x3ba;B, TNF-&#x3b1;, matrix metalloproteinases (MMPs) and prostaglandin E2 (PGE2). The compositions may further comprise at least one agent that promotes expression and/or carboxylation of matrix Gla protein (MGP). Advantageously, these select actives include materials such as phytonutrients, vitamins and minerals that have been broadly used in food and drink products and are safe for human and pet/animal consumption. Compositions with such combinations have the ability to prevent, treat and reverse VC not only in coronary arteries but also in other tissues capable of undergoing undesirable calcification. In addition the present compositions are effective against associated conditions or contributory factors/inducers to VC, including diabetes, obesity, hypertension, inflammation, oxidative stress, osteoporosis and arthritis.

Vascular calcification prevention and treatment

The invention encompasses compositions and methods for effectively treating and/or preventing the development and/or progression of osteoporosis and related disorders such as osteoarthritis and rheumatoid arthritis, and for promoting overall bone and joint health. This is accomplished by addressing multiple key mechanisms that lead to such disorders. The invention includes compositions comprising a combination of agents having biological activities that effectively suppress, regulate or interfere with the various key biochemical processes and mechanisms that increase the risk for development and/or progression of osteoporosis. The present compositions and methods simultaneously promote bone formation and reduce bone resorption by (a) stimulating osteoblast formation and osteogenesis; (b) suppressing adipocyte differentiation; (c) inhibiting osteoclast formation; and (d) increasing apoptosis of osteoclasts. The inventive compositions used for administration to human and other mammalian subjects having or at risk for development of osteoporosis comprise (1) at least one agent capable of modulating expression and/or activity of one or more of peroxisome activated protein receptor gamma (PPAR-&#x3b3;), CAAT/enhancer binding protein-&#x3b1; (C/EBP&#x3b1;) and Sterol Regulatory Element-Binding Protein (SREBP-1); (2) at least one agent that activates expression and/or activity of one or more of the osteogenic transcription factors (Runx2/Cbf&#x3b1;1, Dlx5, Osterix, Msx2); (3) at least one agent that activates expression and/or activity of one or more of bone morphogenetic proteins (BMPs: BMP 2 and 4), alkaline phosphatase (ALP), and osteocalcin; (4) at least one agent capable of activating Wnt/&#x3b2;-catenin signaling pathway; (5) at least one agent that inhibits the activity of pro-oxidants including reactive nitrogen species and reactive oxygen species (ROS); (6) at least one agent that suppresses one or more of inflammatory mediators including interleukins IL-1&#x3b1;, IL-1&#x3b2;, IL-6, NF-&#x3ba;B, TNF-&#x3b1;, matrix metalloproteinases (MMPs) and prostaglandin E2 (PGE2); and (7) at least one agent that induces the expression of and/or activates one or more of adenosine monophosphate-activated protein kinase (AMPK), sirtuin (SIRT1) and adiponectin (AP).

Treatment and prevention of bone and joint disorders

The invention encompasses compositions and methods for effectively treating and/or preventing the development and/or progression of osteoarthritis and rheumatoid arthritis and for promoting overall joint health. This is accomplished by totally addressing the key multiple biochemical processes and mechanisms that lead to such disorders. The invention includes compositions comprising a combination of natural agents that safely and effectively suppress, regulate or interfere with the various biochemical processes and mechanisms that increase the risk for or lead to the development and/or progression of OA and RA. The present compositions are holistically formulated to be effective in preventing/arresting loss of and/or damage to the articular cartilage (AC) by suppressing (a) extracellular matrix (ECM) degradation, (b) chondrocyte apoptosis, and (c) inflammation of synovium through modulation of mechanisms that involve transcription factors, growth factors, kinases, antiapoptotic/apoptotic factors and deacetylases. The active agents used herein are natural materials, in particular phytonutrients (or phytochemicals), minerals and/or vitamins.

Treatment and prevention of joint disorders

Disclosed are anhydrous antiperspirant cream compositions that are substantially free of polymeric or inorganic thickening, and have improved product stability and spreading performance. These compositions have a rheology profile characterized by select product hardness (from about 75 gram force to about 500 gram force), delta stress (from about 300 dyne/cm.sup.2 to about 8,000 dyne/cm.sup.2) and static yield stress (at least about 1,000 dyne/cm.sup.2 ) values. The new rheology profile is preferably applied to antiperspirant cream compositions comprising from about 0.1% to about 20 % by weight of a crystalline gellant, from about 10% to about 80% by weight of an anhydrous liquid carrier for the crystalline gellant having a solubility parameter of from about 3 to about 13 and, from about 5 % to about 35% by weight of a particulate antiperspirant active. Also disclosed are methods of using and making the compositions, and packaged compositions having a shear force delivery means for applying the composition to the axilla or other area of the skin. The disclosed compositions are especially effective at minimizing or eliminating solvent syneresis during packaging, storage, transport or during extrusion through a perforated mesh cap or other shear force delivery means.

Antiperspirant cream compositions having improved rheology

Disclosed are anhydrous antiperspirant cream compositions that are substantially free of polymeric or inorganic thickening, and have improved product stability and spreading performance. These compositions have a rheology profile characterized by select product hardness (from about 75 gram force to about 500 gram force), delta stress (from about 300 dyne/cm.sup.2 to about 8,000 dyne/cm.sup.2) and static yield stress (at least about 1,000 dyne/cm.sup.2) values. The new rheology profile is preferably applied to antiperspirant cream compositions comprising from about 0.1% to about 20% by weight of a crystalline gellant, from about 10% to about 80% by weight of an anhydrous liquid carrier for the crystalline gellant having a solubility parameter of from about 3 to about 13 and, from about 5% to about 35% by weight of a particulate antiperspirant active. Also disclosed are methods of using and making the compositions, and packaged compositions having a shear force delivery means for applying the composition to the axlla or other area of the skin. The disclosed compositions are especially effective at minimizing or eliminating solvent syneresis during packaging, storage, transport or during extrusion through a perforated mesh cap or other shear force delivery means.

Antiperspirant cream composition having improved rheology

Disclosed are anhydrous antiperspirant cream compositions that are substantially free of polymeric or inorganic thickening, and have improved product stability and spreading performance. These compositions have a rheology profile characterized by select product hardness (from about 75 gram force to about 500 gram force), delta stress (from about 300 dyne/cm.sup.2 to about 8,000 dyne/cm.sup.2) and static yield stress (at least about 1,000 dyne/cm.sup.2) values. The new rheology profile is preferably applied to antiperspirant cream compositions comprising from about 0.1% to about 20% by weight of a crystalline gellant, from about 10% to about 80% by weight of an anhydrous liquid carrier for the crystalline gellant having a solubility parameter of from about 3 to about 13 and, from about 5% to about 35% by weight of a particulate antiperspirant active. Also disclosed are methods of using and making the compositions, and packaged compositions having a shear force delivery means for applying the composition to the axilla or other area of the skin. The disclosed compositions are especially effective at minimizing or eliminating solvent syneresis during packaging, storage, transport or during extrusion through a perforated mesh cap or other shear force delivery means.

Disclosed are anhydrous antiperspirant cream compositions that are substantially free of polymeric or inorganic thickening, and have improved product stability and spreading performance. These compositions have a rheology profile characterized by select product hardness (from about 75 gram force to about 500 gram force), delta stress (from about 300 dyne/cm.sup.2 to 8,000 dyne/cm.sup.2) and static yield stress (at least about 1,000 dyne/cm.sup.2) values. The new rheology profile is preferably applied to antiperspirant cream compositions comprising from about 0.1% to about 20% by weight of a crystalline gellant, from about 10% to about 80% by weight of an anhydrous liquid carrier for the crystalline gellant having a solubility parameter of from about 3 to about 13 and, from about 5% to about 35% by weight of a particulate antiperspirant active. Also disclosed are methods of using and making the compositions, and packaged compositions having a shear force delivery means for applying the composition to the axilla or other area of the skin. The disclosed compositions are especially effective at minimizing or eliminating solvent syneresis during packaging, storage, transport or during extrusion through a perforated mesh cap or other shear force delivery means.

Disclosed are anhydrous antiperspirant compositions comprising from about 0.5% to about 60% by weight of particulate antiperspirant active; from about 1% to about 15% by weight of a solid non-polymeric gellant; from about 10% to about 80% by weight of an anhydrous liquid carrier having an average solubility parameter of from about 3 to about 13 (cal/cm.sup.3).sup.0.5 ; and from about 0.0001% to about 5.0% by weight of a solid nucleating agent wherein the molar ratio of the solid non-polymeric gellant to the nucleating agent is from about 10:1 to about 1000:1. These antiperspirant compositions provide improved low residue performance and improved antiperspirant efficacy.

Antiperspirant gel-solid stick compositions containing select nucleating

Therapeutic particles are disclosed which have a coating of a combination of lipids over the therapeutic agent. The lipid coating provides good stomach protection while providing good release of the therapeutic agent in the intestines.

Growing community of inventors

Wyoming, OH, United States of America

Ghebre Egziabher Tzeghai