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US 2026/0090982 A1Published application
Transdermal delivery formulations
AssigneeLifeActive, Inc.
InventorsCalvin Dexter MORRIS, Burgess A. THOMASSON, JR., Scott A. JENKINS
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AssigneeLifeActive, Inc.
InventorsCalvin Dexter MORRIS, Burgess A. THOMASSON, JR., Scott A. JENKINS
Estimating the term…
Provided are transdermal delivery formulations, and methods for the manufacture thereof, for the epicutaneous administration of therapeutic agents, drugs, and nutrients to human subjects; veterinary animals; domesticated or undomesticated animals, plants or insects; or agricultural animals, plants, or insects. Transdermal delivery formulations disclosed herein comprise a homogenous mixture of (a) a transdermal accelerant comprising a weak organic acid having a pKa greater than 2.0 and (b) a microemulsion comprising a nonionic emulsifier, water, and a cis-unsaturated long-chain fatty acid. Fatty acid microemulsions are combined with the acidified transdermal accelerants having a pH greater than 1.0 (typically from 1.5 to 2.5) to yield a homogenous transdermal delivery formulation comprising fatty acid micelles and/or liposomes that encapsulate one or more compound, such as a nutrient or a drug, and incorporate one or more cis-unsaturated fatty acid having a 12 to 26 carbon chain that includes one or more double bond in a cis configuration. Transdermal delivery formulations exhibit ideal solubility and absorption properties in high humidity conditions, such as in a warm to hot shower or sauna.
A transdermal delivery formulation, comprising:
The transdermal delivery formulation of any one of claim, wherein the transdermal delivery formulation comprises about 20%, about 25%, about 30%, about 35%, about 40%, about 45%, about 50%, about 55%, about 60%, about 65%, about 70%, about 75%, or about 80% (w/w) of the at least one weak organic acid.
The transdermal delivery formulation of any one of claim, wherein the transdermal delivery formulation comprises about 60%, about 65%, about 70%, about 75%, or about 80% w/w of the total of the polysorbate 80, the one or more oils in total, and water.
The transdermal delivery formulation of any one of claim, wherein the at least one weak organic acid comprises 2 weak organic acids at a ratio by weight of about 1:1, 1:2, 1:3, 1:4, 1:5, 1:6, 1:7, 1::8, 1:9, 1:10, 1:100 or 1:1000 relative to each other.
The transdermal delivery formulation of any one of claim, wherein the at least one weak organic acid comprises about 80%, about 85%, about 90%, about 95%, about 97%, about 99% (w/w) of one or more weak organic acids.
The transdermal delivery formulation of any one of claim, wherein the at least one weak organic acid has a median pKa of from 3.0 to 5.5.
The transdermal delivery formulation of any one of claim, wherein the at least one weak organic acid has a median pKa of from 4.0 to 5.0.
The transdermal delivery formulation of any one of claim, wherein the at least one weak organic acid has a median pKa of about 4.6.
The transdermal delivery formulation of any one of claim, wherein the at least one weak organic acid comprises a mono, di or tri carbonic acid of chain length (R) between 1-16.
The transdermal delivery formulation of any one of claim, wherein the at least one weak organic acid comprises a mono or poly hydroxy moiety of 0-14.
The transdermal delivery formulation of any one of claim, wherein the at least one weak organic acid comprises lactic acid, acetic acid, formic acid, citric acid, oxalic acid, gallic acid, malic acid, maleic acid, malonic acid, succinic acid, tartaric acid, fumaric acid, or any combination thereof.
The transdermal delivery formulation of any one of claim, wherein said weak organic acid is citric acid or acetic acid.
The transdermal delivery formulation of any one of claim, wherein the at least one weak organic acid comprises citric acid and acetic acid.
The transdermal delivery formulation of any one of claim, wherein the formulation comprises two oils comprising an unsaturated long-chain fatty acid, wherein the two oils are in a ratio by weight of about 1:1, 1:2, 1:3, 1:4, 1:5, 1:6, 1:7, 1:8, 1:9, 1:10, 1:100 or 1:1000 relative to each other.
The transdermal delivery formulation of any one of claim, wherein said at least one unsaturated long-chain fatty acid comprises a chain of from 12 to 26 carbons.
The transdermal delivery formulation of any one of claim, wherein the one or more oils comprising an unsaturated long-chain fatty acid is one or more plant or animal oils.
The transdermal delivery formulation of any one of claim, wherein the transdermal delivery formulation comprises a lotion, a gel, a cream, an ointment, a liniment, a paste, a film, an encapsulation, or a liquid.
The transdermal delivery formulation of any one of claim, wherein the formulation comprises a nitrate source.
The transdermal delivery formulation of any one of claims, further comprising a viscosity enhancer, a nutrient, a plant powder or extract, an amino acid, a vitamin, or any combination thereof.
The transdermal delivery formulation of any one of claim, wherein said transdermal formulation has a pH of from 3.0 to 5.0.
The transdermal delivery formulation of any one of claim, wherein said transdermal formulation has a pH of from 3.5 to 4.5.
The transdermal delivery formulation of any one of claim, wherein said transdermal formulation has a viscosity at 20° C. of from 500 to 10,000 centipoise (cP) or from 1,000 to 5,000 cP, or from 1,500 to 4,000 cP, or from 2,000 to 3,000 cP.
The transdermal delivery formulation of any one of claim, wherein the transdermal delivery formulation forms an emulsion comprising a population of droplets from about 10 nm to about 300 nm in diameter.
The transdermal delivery formulation of any one of claims, further comprising one or more components for enhancing nutrition and optimizing health, immune support, restful sleep, exercise performance and nitric oxide metabolism, cognitive function, or any combination thereof.
The transdermal delivery formulation of any one of claims, further comprising one or more additional ingredients, wherein the additional ingredients comprise:
The transdermal delivery formulation of any one of claim, wherein the one or more active agents comprises a therapeutic agent, a nutraceutical, or a combination thereof.
Dependencies are inferred from the claim text.