Methods and compositions for improved uptake of biological molecules

Abstract

A “one-step” process for production of peptides and other organic molecules which are both esters and also acetylated forms of the desired molecule. The ester may be a mono-ester, di-ester, or another poly-ester, complexed with a molecule for protecting the organic molecules in the digestive tract. The method allows simple adjustment of the delivery properties of the peptides produced, in particular adjustment or addition of lipiphilic tendencies. A therapeutic or nutrient made by this method comprises acetylated organic molecule esters, in particular an acetylated peptide ester or even an acetylated amino acid ester and demonstrates improved metabolic properties leading to increased efficiency for therapeutic and cosmetic purposes including oral, transdermal, sublingual, buccal, and topical administration. The present disclosure further teaches several specific examples of acetylated esters, including acetyl-glutathione-ester (mGSH), MCAR (carnosine), pyruvate and others modified from base forms by the methods of the present disclosure.

1 . A method comprising: 
 protecting one or more functional groups of a therapeutic agent to prevent degradation of the therapeutic agent in the bloodstream;    associating the therapeutic agent with a protecting agent to prevent degradation in the digestive tract;    wherein the protection of the functional groups increases the hydrophobicity of the therapeutic agent to more readily induce absorption of the therapeutic agent through the cellular membrane.    
   
   
       2 . The method of  claim 1 , wherein the protecting agent is cyclodextrin.  
   
   
       3 . The method of  claim 2 , wherein the protection of the functional groups is accomplished by acetylation or esterification.  
   
   
       4 . The method of  claim 2 , wherein the therapeutic agent is glutathione.  
   
   
       5 . The method of  claim 3 , wherein the therapeutic agent is glutathione.  
   
   
       6 . A product by the process of claims  1 .  
   
   
       7 . A product by the process of  claim 2 .  
   
   
       8 . A product by the process of  claim 3 .  
   
   
       9 . A product by the process of  claim 4 .  
   
   
       10 . A product by the process of  claim 5 .  
   
   
       11 . A method comprising: 
 acetylating and esterifying an organic molecule to prevent degradation in at least one of the digestive tract and bloodsteam; and    complexing a cyclodextrin molecule with the organic molecule to prevent degradation in the digestive tract.    
   
   
       12 . The method of  claim 11 , wherein the organic molecule is an antioxidant.  
   
   
       13 . The method of  claim 12 , wherein the organic molecule is glutathione.  
   
   
       14 . The method of  claim 13 , wherein at least three of the amino group, sulphydryl group, terminal carboxyl group, or side carboxyl groups are esterified or acetylated.  
   
   
       15 . The method of  claim 14 , wherein all of the functional groups of the glutathione are esterified or acetylated.  
   
   
       16 . The method of  claim 11 , wherein the organic molecule is one of glutathione, carnosine, and pyruvate.  
   
   
       17 . A product by the process of  claim 11 .  
   
   
       18 . A product by the process of  claim 12 .  
   
   
       19 . A product by the process of  claim 13.