Composition and methods of esterified nitroxides gated with carboxylic acids

Abstract

This invention is directed to the use of novel methods and nitroxide compositions having high redox activity to treat diseases and conditions related to free radicals. The compositions and methods described include pro-drug forms of nitroxide that enhance the therapeutic effect through their ability to penetrate readily into skin cells and remain sequestered within the cells. The formulations and methods described herein result in a significant accumulation of nitroxides in the skin cells, thus achieving a targeted delivery of a therapeutic or diagnostic dose. Applications using the novel compositions and methods described herein include use as improved imaging agents and as improved topical agents for treating conditions of the skin, including aging of the skin, wrinkles caused by sun-exposure, skin cancer, burns, psoriasis and alopecia, among others.

What is claimed is:  
     
         1 . A pharmaceutical composition comprising 
 an anti-oxidative amount of an ester of 2,2,6,6-tetramethyl-1-oxyl-piperdene-4-succinate in a pharmaceutically compatible composition.    
     
     
         2 . The composition of  claim 1  wherein the pharmaceutically compatible composition is the form for topical administration selected from the group consisting of a gel, cream, ointment, and emulsion.  
     
     
         3 . The composition of  claim 1  in a pharmaceutically compatible vehicle for administration by a method consisting of oral, intramuscular, intraperitoneal, and intravenous.  
     
     
         4 . The composition of  claim 1  wherein the ester is an assymetric diester.  
     
     
         5 . The composition of  claim 1  wherein the ester is an ethyl ester, a diethylester, or a tert-butyl ester.  
     
     
         6 . The composition of  claim 1  further comprising polynitroxide albumin.