Topical formulations for the treatment of depression with S adenosyl methionine

A transdermal composition comprising

• an emulsion that includes a 15%-45% wt/wt of a lipophilic component and 55%-85% wt/wt of an aqueous component;
• S-adenosyl methionine at least partially dissolved in the emulsion, wherein the amount of S-adenosyl methionine is at least 35% wt/wt of the composition;
• a buffering agent;
• a vasodilating agent which can be pyridoxal-5-phosphate, niacinamide, dimethyl sulfoxide, pentoxifylline, ibuprofen, horse chestnut extract (Aesculus hippocastanum) or pyridoxine;
• and
• the composition being formulated to be stable against separation of the emulsion for a period of at least 30 days when stored at room temperature.

A transdermal composition comprising an emulsion that includes a lipophilic component and an aqueous component;

• S-adenosyl methionine, in an amount effective for treating depression, partially dissolved in a first portion of the lipophilic component, partly dissolved in a first portion of the aqueous component, partly encapsulated in micelles comprising a second portion of the lipid component surrounding a second portion of the aqueous component;
• a pH adjusting component to bring the pH of the composition between 6.5 and 7.5;
• a vasodilating agent which can be pyridoxal-5-phosphate, niacinamide, dimethyl sulfoxide, pentoxifylline, ibuprofen, horse chestnut extract (Aesculus hippocastanum) or pyridoxine;
• and
• the composition being formulated to be stable against separation of the emulsion for a period of at least 30 days when stored at room temperature.

A method of making a composition for treatment of depression by topical administration of S-adenosyl methionine comprising:

• preparing the composition in a humidity controlled environment of about less than 40% humidity and at temperatures from between about 65° F. to about 75° F., in the following order:
• mixing at least 35% wt/wt S-adenosyl methionine of the composition into an emulsion comprising 15%-45% wt/wt of a lipophilic component and 55%-85% wt/wt of an aqueous component, to form a paste comprising partially dissolved and partially suspended S-adenosyl methionine;
• milling the paste until the partially suspended S-adenosyl methionine is not detectable in the paste by unaided visual inspection;
• mixing into the paste a vasodilating agent which can be pyridoxal-5-phosphate, niacinamide, dimethyl sulfoxide, pentoxifylline, ibuprofen, horse chestnut extract (Aesculus hippocastanum) or pyridoxine;
• and
• diluting the milled paste with a diluent, wherein the paste and diluent are selected to provide an emulsion that is stable from separation when stored for at least 30 days at room temperature, such that the composition is suitable for transdermal delivery of S-adenosyl methionine into the subject's bloodstream for a systemic effect for the treatment of depression.

A transdermal composition comprising:

• an emulsion comprising, a lipophilic component and an aqueous component;
• S-adenosyl methionine at least partially dissolved in the emulsion, wherein the amount of S-adenosyl methionine is at least 35% wt/wt of the composition;
• a vasodilating agent which can be pyridoxal-5-phosphate, niacinamide, dimethyl sulfoxide, pentoxifylline, ibuprofen, horse chestnut extract (Aesculus hippocastanum) or pyridoxine;
• and
• the composition being formulated to be stable against separation of the emulsion for a period of at least 30 days when stored at room temperature.

A transdermal composition comprising:

• an emulsion comprising 15%-45% wt/wt of a lipophilic component and 55%-85% wt/wt of an aqueous component;
• S-adenosyl methionine, in an amount effective for treating depression;
• a vasodilating agent which can be pyridoxal-5-phosphate, niacinamide, dimethyl sulfoxide, pentoxifylline, ibuprofen, horse chestnut extract (Aesculus hippocastanum) or pyridoxine;
• and
• the composition being formulated to be stable against separation of the emulsion for a period of at least 30 days when stored at room temperature.

A transdermal composition comprising:

• an emulsion comprising a lipophilic component and an aqueous component;
• S-adenosyl methionine, in an amount effective for treating depression, partially dissolved in a first portion of the lipophilic component, partly dissolved in a first portion of the aqueous component, partly encapsulated in micelles comprising a second portion of the lipid component surrounding a second portion of the aqueous component;
• a vasodilating agent which can be pyridoxal-5-phosphate, niacinamide, dimethyl sulfoxide, pentoxifylline, ibuprofen, horse chestnut extract (Aesculus hippocastanum) or pyridoxine;
• and
• the composition being formulated to be stable against separation of the emulsion for a period of at least 30 days when stored at room temperature.

A method of making a composition for topical administration of S-adenosyl methionine comprising:

• preparing the composition in a humidity controlled environment of about less than 40% humidity and at temperatures from between about 65° F. to about 75° F., in the following order:
• mixing a weight of S-adenosyl methionine in an amount effective for treating depression into an emulsion comprising 15%-45% wt/wt of a lipophilic component and 55%-85% wt/wt of an aqueous component, to form a paste comprising partially dissolved and partially suspended S-adenosyl methionine;
• milling the paste until the partially suspended S-adenosyl methionine is not detectable in the paste by unaided visual inspection;
• mixing into the paste a vasodilating agent which can be pyridoxal-5-phosphate, niacinamide, dimethyl sulfoxide, pentoxifylline, ibuprofen, horse chestnut extract (Aesculus hippocastanum) or pyridoxine;
• diluting the milled paste with a diluent;
• and
• adding a buffering agent to the composition, wherein the emulsion and diluent are selected to provide the composition that is stable from separation when stored for at least 30 days at room temperature, such that the composition is suitable for transdermal delivery of S-adenosyl methionine into the subject's bloodstream for a systemic effect for the treatment of depression.

A transdermal composition comprising:

• an emulsion comprising a lipophilic component and an aqueous component;
• S-adenosyl methionine partially dissolved in a first portion of the lipophilic component, partly dissolved in a first portion of the aqueous component, partly encapsulated in micelles comprising a second portion of the lipid component surrounding a second portion of the aqueous component, wherein the amount of S-adenosyl methionine is at least 35% wt/wt of the composition;
• a buffering agent;
• and
• the composition being formulated to be stable against separation of the emulsion for a period of at least 30 days when stored at room temperature.

A transdermal composition comprising:

• an emulsion comprising a lipophilic component and an aqueous component;
• S-adenosyl methionine, wherein the amount of S-adenosyl methionine is at least 35% wt/wt of the composition;
• a buffering agent;
• and
• the composition being formulated to be stable against separation of the emulsion for a period of at least 30 days when stored at room temperature.

A method for treating depression in a subject, comprising:

• administering to a subject having depression, an effective amount of a transdermal composition to deliver S-adenosyl methionine directly into the subject's bloodstream for a systemic effect, the composition comprising:
• an emulsion comprising, a lipophilic component and an aqueous component;
• and
• S-adenosyl methionine at least partially dissolved in the emulsion, wherein the amount of S-adenosyl methionine is at least 35% wt/wt of the composition;
• and
• the composition being formulated to be stable against separation of the emulsion for a period of at least 30 days when stored at room temperature, thereby treating depression in the subject.