METHODS AND FORMULATIONS FOR TRANSDERMAL ADMINISTRATION OF BUFFERING AGENTS
A formulation for transdermal delivery of one or more buffering agents through the skin of a subject, comprising: a buffering agent comprising at least one carbonate salt, lysine, tris, a phosphate buffer and/or 2-imidazole-1-yl-3-ethoxycarbonylpropionic acid (IEPA), or a combination thereof in an amount between about 10-56% w/w; and a penetrant portion in an amount between about 44 to 90% w/w, wherein the penetrant portion comprises water in an amount less than about 85% w/w, and wherein the formulation comprises less than about 12% w/w lecithin.
1 . A formulation for transdermal delivery of one or more buffering agents through the skin of a subject, comprising:
a buffering agent comprising at least one carbonate salt, lysine, tris, a phosphate buffer and/or 2-imidazole-1-yl-3-ethoxycarbonylpropionic acid (IEPA), or a combination thereof in an amount between about 10-56% w/w; and
a penetrant portion in an amount between about 44 to 90% w/w,
wherein the penetrant portion comprises water in an amount less than about 85% w/w,
and wherein the formulation comprises less than about 12% w/w lecithin.
2 . The formulation of claim 1 , wherein the penetrant portion further comprises a detergent portion in an amount between about 1 to 70% w/w.
3 . The formulation of claim 1 , wherein the buffering agent is in an amount between about 10-36% w/w of the formulation.
4 . The formulation of claim 1 , wherein the penetrant portion is in an amount between about 44-80% w/w of the formulation.
5 . The formulation of claim 1 , wherein the water is in an amount between about 15-42% w/w of the penetrant portion of the formulation.
6 . The formulation of claim 1 , wherein the penetrant portion comprises an alcohol in an amount less than 10% w/w of the formulation.
7 . The formulation of claim 7 , wherein the penetrant portion comprises lecithin organogel, an alcohol, a surfactant, and a polar solvent.
8 . The formulation of claim 1 , wherein the penetrant portion comprises a mixture of xanthan gum, lecithin, sclerotium gum, pullulan, or a combination thereof in an amount less than 5% w/w of the formulation.
9 . The formulation of claim 1 , wherein the penetrant portion comprises a mixture of caprylic triglycerides and capric triglycerides in amount less than 8% w/w of the formulation.
10 . The formulation of claim 1 , wherein the penetrant portion comprises lecithin, phosphatidylcholine, hydrogenated phosphatidylcholine, phosphatidylserine, phosphatidylethanolamine, phosphatidylinositol, one or more phosphatides, one or more Inositol phosphatides, or combinations thereof, in amount less than 12% w/w of the formulation.
11 . The formulation of claim 1 , wherein the penetrant portion comprises cetyl alcohol in amount less than 5% w/w of the formulation.
12 . The formulation of claim 1 wherein the penetrant portion comprises stearic acid in an amount less than 5% w/w of the formulation.
13 . The formulation of claim 1 , wherein the formulation comprises a gelling agent in an amount less than 5% w/w of the formulation.
14 . The formulation of claim 2 , wherein the detergent portion comprises a nonionic surfactant in an amount between about 2-25% w/w of the penetrant portion; and a polar solvent in an amount less than 5% w/w of the penetrant portion.
15 . The formulation of claim 1 , wherein the carbonate salt is sodium bicarbonate milled to a particle size less than 70 μm, wherein the sodium bicarbonate is solubilized in the formulation in an amount less than 10% w/w of the formulation.
16 . The formulation of claim 1 , further comprising tranexamic acid in an amount less than 5% w/w of the formulation.
17 . The formulation of claim 1 , further comprising a polar solvent in an amount less than 5% w/w of the formulation.
18 . The formulation of claim 1 , further comprises a humectant, an emulsifier, an emollient, or a combination thereof.
19 . The formulation of claim 1 , wherein the formulation has a pH of 7-10.5.
20 . A formulation for transdermal delivery of a buffering agent through the skin of a subject, comprising a formulation of Table 1, Table 2, Table 3, Table 4, Table 5, Table 6, Table 7, Table 8, Table 9, Table 10, Table 11, Table 12, Table 13, Table 14, Table 15, Table 16, Table 17, Table 18, Table 19, Table 20, Table 21, Table 22, Table 23, Table 24, Table 25, Table 26, Table 27, Table 28, Table 29, Table 30, Table 31, Table 32, Table 33, Table 34, Table 35, Table 36, Table 37, Table 38, Table 39, Table 40, Table 41, or Table 42.
21 . A method for transdermal delivery of the formulation of claim 1 , through the skin of a subject.