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 . A composition comprising crystallized phosphatidylcholine and polypeptide drug molecules entrapped within the phosphatidylcholine for transdermal delivery of the polypeptide drug molecules into dermal vasculature.  
     
     
         2 . The composition of  claim 1 , wherein the polypeptide drug molecules are selected from the group consisting of oxytocin, vasopressin, insulin, somatotropin, calcitonin, chorionic gonadotropin, menotropins, follitropins, somatostatins, progestins, and combinations of any of these.  
     
     
         3 . The composition of  claim 1 , wherein the phosphatidylcholine is enriched with polyenylphosphatidylcholine.  
     
     
         4 . The composition of  claim 3 , wherein the phosphatidylcholine is pure polyenylphosphatidylcholine.  
     
     
         5 . The composition of  claim 1 , wherein the composition contains about 85% phosphatidylcholine.  
     
     
         6 . The composition of  claim 1 , wherein the phosphatidylcholine is soybean lecithin.  
     
     
         7 . The composition of claims  1 , further comprising one or more adjunct ingredients to preserve integrity of the polypeptide drug molecules, selected from the group consisting of ascorbyl palmitate, lipoic acid, and combinations of these.  
     
     
         8 . The composition of  claim 2 , wherein the phosphatidylcholine is enriched with polyenylphosphatidylcholine.  
     
     
         9 . The composition of  claim 8 , wherein the phosphatidylcholine is pure polyenylphosphatidylcholine.  
     
     
         10 . The composition of  claim 2 , wherein the composition contains about 85% phosphatidylcholine.  
     
     
         11 . The composition of  claim 2 , wherein the phosphatidylcholine is soybean lecithin.  
     
     
         12 . The composition of claims  2 , further comprising one or more adjunct ingredients to preserve integrity of the polypeptide drug molecules, selected from the group consisting of ascorbyl palmitate, lipoic acid, and combinations of these.  
     
     
         13 . A topical composition for transdermal delivery of macromolecular drugs, comprising: 
 a carrier containing crystallized phosphatidylcholine enriched with polyenylphosphatidylcholine; and    at least one macromolecular drug entrapped within the crystallized phosphatidylcholine carrier for transdermal delivery into dermal vasculature.    
     
     
         14 . The composition of  claim 13 , wherein the polypeptide drug molecules are selected from the group consisting of oxytocin, vasopressin, insulin, somatotropin, calcitonin, chorionic gonadotropin, menotropins, follitropins, somatostatins, progestins, and combinations of any of these.  
     
     
         15 . The composition of  claim 13 , further comprising at least one adjunct ingredient selected from the group consisting of ascorbyl palmitate, lipoic acid, and combinations of these, to preserve integrity of the macromolecular drug during delivery.  
     
     
         16 . The composition of  claim 13 , wherein the phosphatidylcholine carrier is pure polyenylphosphatidylcholine.  
     
     
         17 . The composition of  claim 13 , wherein the composition contains about 85% phosphatidylcholine.  
     
     
         18 . The composition of  claim 13 , wherein the phosphatidylcholine carrier is soybean lecithin.