Methods and compositions for sustained delivery of drugs

Abstract

The present disclosure relates to methods and compositions for the topical sustained delivery of therapeutic agents. Topical application of compositions containing a muscle fasciculating agent result in the sustained release of any therapeutic agent contained within the composition. More particularly, topical application of such compositions to the outer surface of the eyelid of a patient results in increased absorption and sustained release of the therapeutic agent into the eyes or systemically.

1 - 47 . (canceled) 
     
     
         48 . A method for systemic delivery of a therapeutically effective amount of at least one therapeutic agent in a human patient in need thereof comprising topically applying a composition comprising said at least one therapeutic agent and a muscle fasciculating agent selected from the group consisting of caffeine, theophylline, pentoxifyline and theobromide to the outer surface of at least one upper eyelid of the patient. 
     
     
         49 . The method of  claim 48  wherein the muscle fasciculating agent is caffeine. 
     
     
         50 . The method of  claim 48  wherein the muscle fasciculating agent is present in an amount of from about 0.001 wt % to about 50 wt % of the composition. 
     
     
         51 . The method of  claim 48  further comprising the step of administering the composition to at least one lower eyelid of the patient. 
     
     
         52 . The method of  claim 48  wherein the patient suffers from a pathologic condition selected from diabetes, systemic infection, kidney disease, hypertension, heart disease, nicotine withdrawal, or a hormone deficiency. 
     
     
         53 . The method of  claim 48  wherein the therapeutic agent is a hypertensive medication. 
     
     
         54 . The method of  claim 48  wherein the therapeutic agent is insulin or recombinant insulin. 
     
     
         55 . The method of  claim 48  wherein the composition further comprises an ionotropic agent. 
     
     
         56 . The method of  claim 55  wherein topical application of the at least one therapeutic agent to the outer surface of at least one eyelid results in sustained systemic delivery of said therapeutic agent or combination of therapeutic agents. 
     
     
         57 . The method of  claim 48  wherein topical application of the at least one therapeutic agent to the outer surface of at least one eyelid results in systemic delivery of the therapeutic agent or combination of therapeutic agents to a target site remote from the eye. 
     
     
         58 . The method of  claim 48  wherein the at least one therapeutic agent is selected from the group consisting of insulin, recombinant insulin, antihypertensive agents, nicotine, antibiotics, hormones, recombinant hormones, and antiarrhythmia agents or combinations thereof.