Active agent delivery systems and methods for protecting and administering active agents

Abstract

A composition comprising a polypeptide and an active agent covalently attached to the polypeptide. Also provided is a method for delivery of an active agent to a patient comprising administering to the patient a composition comprising a polypeptide and an active agent covalently attached to the polypeptide. Also provided is a method for protecting an active agent from degradation comprising covalently attaching the active agent to a polypeptide. Also provided is a method for controlling release of an active agent from a composition comprising covalently attaching the active agent to the polypeptide.

1 . A method for controlling release of an active agent other than an amino acid in a patient comprising orally administering to said patient an amino acid/active agent complex comprising a polypeptide covalently attached to the active agent through an alcohol, an amine or a carboxylic acid functionality wherein said active agent enzymatically releases into the bloodstream following oral administration.  
     
     
         2 . The method of  claim 1 , wherein the polypeptide includes of one or more of the twenty naturally occurring amino acids.  
     
     
         3 . The method of  claim 1 , wherein said amino acid is glutamic acid, aspartic acid, arginine, asparagine, cysteine, lysine, threonine or serine.  
     
     
         4 . The method of  claim 1 , wherein said amino acid is glutamic acid.  
     
     
         5 . The method of  claim 1 , wherein said complex is in the form of an ingestible tablet, a capsule, or an oral suspension.  
     
     
         6 . The method of  claim 1 , wherein said complex further comprises a microencapsulating agent.  
     
     
         7 . The method of  claim 1 , wherein said complex further comprises an adjuvant covalently attached to said polypeptide.  
     
     
         8 . A method for preparing a composition comprising a polypeptide and an active agent covalently attached to said polypeptide comprising the steps of: 
 (a) attaching the active agent to an amino acid to form an active agent/amino acid complex;    (b) forming an N-carboxyanhydride (NCA) from said active agent/amino acid complex; and    (c) polymerizing said N-carboxyanhydride (NCA).    
     
     
         9 . The method of  claim 8 , wherein the active agent is attached to the side chain of said amino acid.  
     
     
         10 . The method of  claim 8 , wherein the active agent is attached to the N-terminus of said amino acid.  
     
     
         11 . The method of  claim 8 , wherein the active agent is attached to the C-terminus of said amino acid  
     
     
         12 . The method of  claim 8 , further comprising the step of (d) granulating said complex.  
     
     
         13 . The method of  claim 8 , wherein said amino acid is glutamic acid, aspartic acid, arginine, asparagine, cysteine, lysine, threonine or serine.  
     
     
         14 . The method of  claim 8 , wherein said amino acid is glutamic acid.  
     
     
         15 . The method of  claim 8 , wherein said amino acid is a synthetic amino acid with a pendant amine, alcohol, sulfhydryl, amide, urea, or acid functionality.