Formulations for transdermal administration of active agents

A formulation for transdermal delivery of a medicament through the skin of a subject, the formulation comprising a therapeutically effective amount of a medicament and a penetrant portion,

• wherein the penetrant portion comprises:
• a phospholipid, a fatty acid ester formed from a low molecular weight alcohol, and a long-chain fatty acid,
• wherein phosphatidylcholine, hydrogenated phosphatidylcholine, phosphatidylserine, phosphatidylethanolamine, phosphatidylinositol, inositol phosphatide, or sphingomyelin is the phospholipid;
• isopropyl palmitate, isopropyl myristate, isopropyl linoleate, isopropyl oleate, ethyl laurate, or ethyl myristate is the fatty acid ester;
• and a linoleic, oleic, stearic acid, linolenic, palmitic, arachidonic, palmitoleic, myristic, eicosenoic, benehic, euricic, or lignoceric acid is the long-chain fatty acid or the long-chain fatty acid is obtained from safflower oil or almond oil.

A formulation for transdermal delivery of a medicament through the skin of a subject, the formulation comprising a therapeutically effective amount of a medicament and a penetrant portion,

• wherein the penetrant portion comprises:
• a phospholipid, a fatty acid ester formed from a low molecular weight alcohol, and a long-chain fatty acids, and one or more of a viscosity-improving agent, a penetration enhancer, and an emulsifier,
• wherein phosphatidylcholine, hydrogenated phosphatidylcholine, phosphatidylserine, phosphatidylethanolamine, phosphatidylinositol, inositol phosphatide, or sphingomyelin is the phospholipid;
• isopropyl palmitate, isopropyl myristate, isopropyl linoleate, isopropyl oleate, ethyl laurate, or ethyl myristate is the fatty acid ester;
• and a linoleic, oleic, stearic acid, linolenic, palmitic, arachidonic, palmitoleic, myristic, eicosenoic, benehic, euricic, or lignoceric acid is the long-chain fatty acid or the long-chain fatty acid is obtained from safflower oil or almond oil;
• polyglyceryl-4-laurate, polyglyceryl-4-oleate, span 60, cetyl alcohol, or polyglyceryl-3-oleate is the penetration enhancer;
• a poloxamer (e.g., poloxamer 407, poloxamer 188, poloxamer 184, and poloxamer 124) or sodium lauryl sulfate is the viscosity-improving agent;
• benzyl alcohol, ethanol, propylene glycol, polyethylene glycol, limonene, menthol, borneol, or camphor is the penetration enhancer.

A formulation for transdermal delivery of a medicament through the skin of a subject, the formulation comprising a phospholipid in an amount from about 5% to about 15% w/w of the formulation;

• an emollient/moisturizer in an amount from about 10% to about 20% w/w of the formulation;
• a fatty acid in an amount from about 0.5% to about 2% w/w of the formulation;
• an alcohol in an amount from about 0.5% to about 2% w/w of the formulation;
• an oil in an amount from about 1% to about 5% w/w of the formulation;
• a surfactant in an amount from about 0.5% to about 2% w/w of the formulation;
• water in an amount from about 30% to about 80% w/w of the formulation;
• and a therapeutically effective amount of a medicament in an amount from about 0.00001% to about 30% w/w of the formulation.

A formulation for transdermal delivery of a medicament through the skin of a subject, the formulation comprising phosphatidylcholine in an amount of about 7.64% w/w of the formulation;

• isopropyl palmitate in an amount of about 13.30% w/w of the formulation;
• stearic acid in an amount of about 0.62% w/w of the formulation;
• benzyl alcohol in an amount of about 1.39% w/w of the formulation;
• safflower oil in an amount of about 2.93% w/w of the formulation;
• oleic acid in an amount of about 0.97% w/w of the formulation;
• polyglyceryl-4 laurate in an amount of about 1.06% w/w of the formulation;
• deionized water in an amount of about 60.84% w/w of the formulation;
• poloxamer 407 in an amount of about 9.25% w/w of the formulation;
• and a therapeutically effective amount of a medicament in an amount of about 2% w/w of the formulation.

A formulation for transdermal delivery of a medicament through the skin of a subject, the formulation comprising phosphatidylcholine in an amount of about 7.66% w/w of the formulation;

• isopropyl palmitate in an amount of about 13.34% w/w of the formulation;
• benzyl alcohol in an amount of about 1.39% w/w of the formulation;
• stearic acid in an amount of about 0.68% w/w of the formulation;
• carthamus tinctorius (safflower) oil in an amount of about 2.79% w/w of the formulation;
• polyglyceryl-4 laurate in an amount of about 1.07% w/w of the formulation;
• oleic acid in an amount of about 1.06% w/w of the formulation;
• deionized water in an amount of about 61.73% w/w of the formulation;
• poloxamer 407 in an amount of about 9.28% w/w of the formulation;
• and a therapeutically effective amount of a medicament in an amount of about 1.00% w/w of the formulation.

A formulation for transdermal delivery of a medicament through the skin of a subject, the formulation comprising a therapeutically effective amount of a medicament and a penetrant portion, wherein the penetrant portion comprises:

• phosphatidylcholine in an amount from about 3% to about 15% w/w of the formulation;
• isopropyl palmitate in an amount from about 5% to about 20% w/w of the formulation;
• stearic acid in an amount from about 0.1% to about 10% w/w of the formulation;
• benzyl alcohol in an amount from about 0.5% to about 5% w/w of the formulation;
• polyglyceryl-4 laurate in an amount from about 0.5% to about 10% w/w of the formulation;
• and poloxamer 407 in an amount from about 5% to about 20% w/w of the formulation.