Methods and formulations for transdermal administration

Abstract

Improved formulations for topical treatment that ensure at least localized transdermal or systemic delivery of an active agent through skin, nails or hair follicles are disclosed.

1 . A formulation for transdermal delivery of an active agent through the skin, nail or hair follicle of a subject, which formulation comprises at least one active agent in an amount effective for treatment of a condition in said subject and
 benzyl alcohol—0.5-20% w/w of said formulation; and   lecithin organogel—25-70% w/w of said formulation.   
     
     
         2 . The formulation of  claim 1  wherein the lecithin organogel is present at 30%-60% w/w. 
     
     
         3 . The formulation of  claim 1  wherein the lecithin organogel is a combination of soy lecithin with isopropyl palmitate. 
     
     
         4 . The formulation of  claim 1  which further comprises
 nonionic surfactant—2-25% w/w of said formulation; and 
 polar solvent at least in an amount in molar excess of the nonionic surfactant. 
 
     
     
         5 . The formulation of  claim 4  wherein the polar solvent completes the formulation. 
     
     
         6 . The formulation of  claim 4  wherein the nonionic surfactant is a poloxamer and the polar solvent is water. 
     
     
         7 . The formulation of  claim 1  which is essentially anhydrous and further comprises nonionic surfactant and bile salt wherein the bile salt is present at 1-15% w/w and the surfactant is provided in powdered form at 20-60% w/w. 
     
     
         8 . The formulation of  claim 1  which further contains an antioxidant. 
     
     
         9 . The formulation of  claim 1  wherein at least two active agents are included in said formulation. 
     
     
         10 . The formulation of  claim 1  wherein the formulation comprises micelles. 
     
     
         11 . The formulation of  claim 1  wherein the formulation has a pH of 9-11. 
     
     
         12 . The formulation of  claim 1  wherein an active ingredient is an anesthetic, a fat-dissolving agent, a nutrient or nutrient combination, a tissue volume enhancer, a vaccine component, a hair growth modulator, an antifungal agent, an agent to promote smoking cessation, and/or a cannabinoid. 
     
     
         13 . The formulation of  claim 1 , which comprises an active agent in an amount effective for treatment of a condition in said subject; and
 benzyl alcohol—0.5-20% w/w of said formulation;   lecithin organogel—30-60% w/w of said formulation; and   the remainder of the formulation a 20%-40% w/w nonionic detergent in a polar solvent.   
     
     
         14 . The formulation of  claim 1 , which comprises an active agent in an amount effective for treatment of a condition in said subject; and
 benzyl alcohol—0.5-20% w/w of said formulation;   lecithin organogel—30-60% w/w of said formulation;   bile salt—5-15% w/w of said formulation; and   the remainder of the formulation a nonionic detergent.   
     
     
         15 . A method to effect transdermal delivery of an active ingredient, which method comprises applying to the skin, nails or hair follicles of a subject an effective amount of the formulation of  claim 1 . 
     
     
         16 . A method to dissolve localized fat in a subject which comprises treating the skin proximal to the localized fat with a formulation comprising benzyl alcohol in the range of 0.5% w/w-20% w/w, lecithin organogel in the range of 0.5% w/w-70% w/w, and bile salt in the range of 5-15% w/w. 
     
     
         17 . The method of  claim 16  wherein said formulation further comprises an effective amount of anesthetic. 
     
     
         18 . A method to alleviate pain associated with dissolving localized fat in a subject which method comprises, along with said dissolving, applying to the area wherein said dissolving is performed a formulation comprising benzyl alcohol in the range of 0.5% w/w-20% w/w, lecithin organogel in the range of 0.5% w/w-70% w/w and an effective amount of anesthetic. 
     
     
         19 . The method of  claim 15  wherein said treating is of skin and which further includes, following said treating, applying a composition comprising linoleic acid to the area of treatment. 
     
     
         20 . The method of  claim 16  which further includes, following said treating, applying a composition comprising linoleic acid to the area of treatment. 
     
     
         21 . A penetrant composition which comprises sufficient lecithin organogel, benzyl alcohol, surfactant, polar solvent and/or bile salt to result, when mixed with active agent, the formulation of  claim 1 . 
     
     
         22 . A formulation for transdermal delivery of an active agent through the skin, nail or hair follicle of a subject, which formulation comprises at least one active agent in an amount effective for treatment of a condition in said subject and
 benzyl alcohol—0.5-20% w/w of said formulation;   lecithin organogel—0.5-70% w/w of said formulation;   bile salt—1-15% w/w of said formulation; and   surfactant—20-60% w/w of said formulation.