Topical drug delivery using phosphatidylcholine

Abstract

The present invention relates to compositions and methods for transdermal drug delivery comprising formulating a phosphatidylcholine carrier composition containing the drug and applying the composition to the skin.

1 - 18 . (canceled) 
     
     
         19 . A transdermal therapeutic composition, comprising:
 a non-liposomal multilamellar liquid crystal carrier comprising phosphatidylcholine, the non-liposomal multilamellar liquid carrier comprising a polypeptide for transdermal delivery to dermal vasculature, the phosphatidylcholine comprising a higher concentration of polyenylphosphatidylcholine than the concentration of polyenylphosphatidylcholine in food grade lecithin.   
     
     
         20 . The composition of  claim 19 , wherein the polypeptide is insulin. 
     
     
         21 . The composition of  claim 19 , wherein the polypeptide is selected from the group consisting of oxytocin, vasopressin, somatotropin, calcitonin, chorionic gonadotropin, menotropins, follitropins, somatostatins, progestins, and combinations of any of these. 
     
     
         22 . The composition of  claim 19 , wherein the carrier comprises about  85 % w/w phosphatidylcholine. 
     
     
         23 . The composition of  claim 19 , wherein the carrier further comprises one or more of ascorbyl palmitate and lipoic acid. 
     
     
         24 . The composition of  claim 19 , wherein the carrier further comprises a polyglycol. 
     
     
         25 . The composition of  claim 24 , wherein the phosphatidylcholine forms 45% w/w of the carrier and the polyglycol forms 55% w/w of the carrier. 
     
     
         26 . The composition of  claim 25 , wherein the 55% w/w polyglycol is 50% w/w polyglycol having a molecular weight of 200 and 5% w/w polyglycol having a molecular weight of 400. 
     
     
         27 . The composition of  claim 19 , wherein the phosphatidylcholine within the carrier consists essentially of polyenylphosphatidlycholine. 
     
     
         28 . The composition of  claim 19 , the carrier further comprising a surfactant. 
     
     
         29 . The composition of  claim 28 , wherein the surfactant comprises a siloxylated polyether. 
     
     
         30 . The composition of  claim 29 , wherein the siloxylated polyether comprises dimethyl, methyl(propylpolyethylene oxide propylene oxide, acetate) siloxane. 
     
     
         31 . The composition of  claim 19 , the carrier further comprising a lubricant. 
     
     
         32 . The composition of  claim 31 , wherein the lubricant comprises a silicone fluid. 
     
     
         33 . The composition of  claim 32 , wherein the silicone fluid comprises polydimethylsiloxane. 
     
     
         34 . The composition of  claim 19 , the carrier further comprising methyl paraben. 
     
     
         35 . A transdermal therapeutic composition, comprising:
 a non-liposomal multilamellar liquid crystal carrier comprising crystalline phosphatidylcholine, the phosphatidylcholine consisting essentially of polyenylphosphatidylcholine, the carrier comprising a polypeptide for transdermal delivery to dermal vasculature.   
     
     
         36 . The composition of  claim 35 , wherein the polypeptide is insulin. 
     
     
         37 . The composition of  claim 35 , wherein the polypeptide is selected from the group consisting of oxytocin, vasopressin, somatotropin, calcitonin, chorionic gonadotropin, menotropins, follitropins, somatostatins, progestins, and combinations any of these. 
     
     
         38 . The composition of  claim 35 , wherein the carrier further comprises one or more of ascorbyl palmitate and lipoic acid. 
     
     
         39 . The composition of  claim 35 , wherein the carrier further comprises polyglycol. 
     
     
         40 . The composition of  claim 39 , wherein the phosphatidylcholine forms 45% w/w of the carrier and the polyglycol forms 55% w/w of the carrier. 
     
     
         41 . The composition of  claim 40 , wherein the 55% w/w polyglycol is 50% w/w polyglycol having a molecular weight of 200 and 5% w/w polyglycol having a molecular weight of 400. 
     
     
         42 . A method, comprising:
 providing a preparation comprising phosphatidylcholine, the phosphatidylcholine comprising polyenylphosphatidylcholine at a first concentration;   enriching the preparation with an extract comprising phosphatidylcholine, the phosphatidylcholine comprising polyenylphosphatidylcholine at a second concentration, the second concentration of polyenylphosphatidylcholine being higher than the first concentration of polyenylphosphatidylcholine; and   causing the preparation to adopt a non-liposomal multilamellar liquid crystal phase.   
     
     
         43 . The method of  claim 42 , the method further comprising adding a polypeptide to the preparation. 
     
     
         44 . The method of  claim 43 , wherein the polypeptide is insulin. 
     
     
         45 . The method of  claim 44 , wherein the polypeptide is selected from the group consisting of oxytocin, vasopressin, somatotropin, calcitonin, chorionic gonadotropin, menotropins, follitropins, somatostatins, progestins, and combinations of any of these.