TRANSDERMAL PENETRANT FORMULATIONS
Disclosed herein is a transdermal delivery formulation for transdermal delivery of an active agent through the skin, nail or hair follicle of a subject, wherein the formulation comprises a) a transdermal delivery formulation in an amount less than about 60% w/w, comprising i. one or more phosphatides, ii. glucose, and iii. one or more fatty acids; and b) water in an amount less than about 50% w/w.
1 . A transdermal delivery formulation for transdermal delivery of an active agent through the skin, nail or hair follicle of a subject, wherein the transdermal delivery formulation comprises:
a) a transdermal delivery formulation in an amount less than about 60% w/w, comprising:
iv. one or more phosphatides,
v. glucose, and
vi. one or more fatty acids; and
b) water in an amount less than about 50% w/w.
2 . The transdermal delivery formulation of claim 1 , further comprising benzyl alcohol in an amount between about 0.5-5% w/w.
3 . The transdermal delivery formulation of claim 1 wherein the transdermal delivery formulation comprises benzyl alcohol in an amount less than 5% w/w of the formulation.
4 . The transdermal delivery formulation of claim 1 , further comprising Isopropyl Palmitate in an amount between about 5-5% w/w.
5 . The transdermal delivery formulation of claim 1 , wherein the water is deionized water and/or purified water.
6 . The transdermal delivery formulation of claim 1 , wherein the water is not deionized water and/or purified water.
7 . The transdermal delivery formulation of claim 1 , wherein the water is in an amount between about 15-40% w/w of the formulation.
8 . The formulation of claim 1 , wherein the one or more phosphatides in an amount between about 0.5-55% w/w of the transdermal delivery formulation.
9 . The transdermal delivery formulation of claim 1 , wherein the transdermal delivery formulation comprises phosphatidylcholine, hydrogenated phosphatidylcholine, phosphatidylserine, phosphatidylethanolamine, phosphatidylinositol, or a combination thereof in amount less than 30% w/w of the formulation.
10 . The transdermal delivery formulation of claim 1 , wherein the one or more phosphatides comprises phosphatidylcholine of the transdermal delivery formulation.
11 . The transdermal delivery formulation of claim 1 , wherein the one or more fatty acids in an amount between about 1-35% w/w of the transdermal delivery formulation.
12 . The transdermal delivery formulation of claim 1 , wherein the one or more fatty acids in an amount between about 5-35% w/w of the transdermal delivery formulation.
13 . The transdermal delivery formulation of claim 1 , wherein the one or more fatty acids comprises Linoleic Acid, Oleic Acid, Stearic Acid, safflower oil, or a combination thereof.
14 . The transdermal delivery formulation of claim 1 , wherein the one or more fatty acids comprises Linoleic Acid.
15 . The transdermal delivery formulation of claim 1 , wherein the one or more fatty acids comprises Oleic Acid.
16 . The transdermal delivery formulation of claim 1 , wherein the one or more fatty acids comprises Stearic Acid.
17 . The transdermal delivery formulation of claim 1 , wherein the one or more fatty acids are derived from a seed oil in an amount between about 0.5-55% w/w of the transdermal delivery formulation.
18 . The transdermal delivery formulation of claim 1 , wherein the one or more fatty acids are derived from a seed oil in an amount between about 5-35% w/w of the transdermal delivery formulation.
19 . The transdermal delivery formulation of claim 1 , wherein the one or more fatty acids are derived from a safflower oil in an amount between about 0.5-55% w/w of the transdermal delivery formulation.
20 . The transdermal delivery formulation of claim 1 , wherein the one or more fatty acids are derived from a safflower oil in an amount between about 5-35% w/w of the transdermal delivery formulation.
21 . The transdermal delivery formulation of claim 1 , wherein the one or more fatty acids are derived from an almond oil in an amount between about 0.5-55% w/w of the transdermal delivery formulation.
22 . The transdermal delivery formulation of claim 1 , wherein the one or more fatty acids are derived from an almond oil in an amount between about 5-35% w/w of the transdermal delivery formulation.
23 . The transdermal delivery formulation of claim 1 , wherein the one or more fatty acids comprises one or more fatty acids derived from soy lecithin.
24 . The transdermal delivery formulation of claim 1 , wherein the glucose in an amount between about 0.05-10% w/w of the transdermal delivery formulation.
25 . The transdermal delivery formulation of claim 1 , wherein the glucose is anhydrous dextrose in an amount between about 0.05-10% w/w of the transdermal delivery formulation.
26 . The transdermal delivery formulation of claim 1 , further comprises a nonionic surfactant in an amount between about 2-25% w/w of the transdermal delivery formulation.
27 . The transdermal delivery formulation of claim 26 , further comprises a polar solvent at least in an amount in molar excess of the nonionic surfactant.
28 . The transdermal delivery formulation of claim 27 , wherein the nonionic surfactant is a poloxamer and the polar solvent is water.
29 . The transdermal delivery formulation of claim 1 , further comprising a polar solvent in an amount less than 5% w/w of the formulation.
30 . The transdermal delivery formulation of claim 1 , wherein the transdermal delivery formulation further comprises a detergent portion in an amount between about 1-30% w/w of the transdermal delivery formulation.
31 . The transdermal delivery formulation of claim 30 , wherein the detergent portion comprises a nonionic surfactant in an amount between about 2-25% w/w of the transdermal delivery formulation; and a polar solvent in an amount less than 5% w/w of the transdermal delivery formulation.
32 . The transdermal delivery formulation of claim 1 , wherein the transdermal delivery formulation is in an amount between about 10-60% w/w of the transdermal delivery formulation.
33 . The transdermal delivery formulation of claim 1 , wherein the transdermal delivery formulation comprises an alcohol in an amount less than 10% w/w of the transdermal delivery formulation.
34 . The transdermal delivery formulation of claim 1 , wherein the transdermal delivery formulation further comprises an alcohol, a surfactant, and a polar solvent.
35 . The transdermal delivery formulation of claim 1 , wherein the transdermal delivery formulation comprises cetyl alcohol in amount less than 5% w/w of the formulation.
36 . The transdermal delivery formulation of claim 1 wherein the transdermal delivery formulation comprises ethanol in an amount less than 5% w/w of the formulation.
37 . The transdermal delivery formulation of claim 1 wherein the transdermal delivery formulation comprises glycerine in an amount less than 5% w/w of the formulation.
38 . The transdermal delivery formulation of claim 1 wherein the transdermal delivery formulation comprises propylene glycol in an amount less than 8% w/w of the formulation.
39 . The transdermal delivery formulation of claim 1 , wherein the formulation comprises a gelling agent in an amount less than 20% w/w of the formulation.
40 . The transdermal delivery formulation of claim 1 , wherein the formulation comprises menthol in an amount between about 0.05-5% w/w of the formulation.
41 . The transdermal delivery formulation of claim 1 , further comprising tranexamic acid in an amount less than 5% w/w of the formulation.
42 . The transdermal delivery formulation of claim 1 , further comprises a humectant, an emulsifier, an emollient, or a combination thereof.
43 . The transdermal delivery formulation of claim 1 , wherein the formulation has a pH of 9-11.
44 . The transdermal delivery formulation of claim 1 , wherein the formulation has a pH of 7-10.5.
45 . The transdermal delivery formulation of claim 1 , further comprising an active agent.
46 . The transdermal delivery formulation of claim 1 , further comprising an active agent component in an amount less than about 60% w/w.
47 . A transdermal delivery formulation to effect transdermal delivery of an active ingredient comprising applying to the skin, nails or hair follicles of a subject an effective amount of the formulation of claim 46 .
48 . The transdermal delivery formulation of claim 1 , wherein the formulation includes an active agent to treat a disease.
49 . The transdermal delivery formulation, wherein the disease is a cancer, a kidney disease, gout, melasma, a heart condition or a dermal disease.
50 . The transdermal delivery formulation of claim 1 , wherein the formulation has a pH of 4.5-10.5.