Efficient lipid delivery to human tear film using a salt-sensitive emulsion system

Abstract

Provided herein are low salt ophthalmic pharmaceutical composition and methods of use thereof, for example, in the treatment of dry eye syndrome.

What is claimed is: 
     
         1 . A low salt ophthalmic pharmaceutical composition comprising a sub-micron emulsion, a polymer lubricant, and a salt-sensitive viscosity modulating polymer, wherein said sub-micron emulsion comprises a surfactant and castor oil. 
     
     
         2 . The low salt ophthalmic pharmaceutical composition according to  claim 1 , wherein said castor oil present at a concentration of about 0.25% (w/w). 
     
     
         3 . The low salt ophthalmic pharmaceutical composition according to  claim 1 , wherein said surfactant is a sorbitan ester, wherein said sorbitan ester is polysorbate 80 present at a concentration of about 0.5% (w/w). 
     
     
         4 . The low salt ophthalmic pharmaceutical composition according to  claim 1 , wherein said salt-sensitive viscosity modulating polymer is an acrylate/C 10 -C 30  acrylate crosspolymer having a standard emulsion viscosity between 1,700 and 4,500 cPs. 
     
     
         5 . The low salt ophthalmic pharmaceutical composition according to  claim 1 , wherein said polymer lubricant is carboxymethylcellulose sodium present at a concentration of about 0.5% (w/w). 
     
     
         6 . The low salt ophthalmic pharmaceutical composition according to  claim 1 , further comprising a compatible solute. 
     
     
         7 . The low salt ophthalmic pharmaceutical composition according to  claim 6 , wherein said compatible solute is erythritol or levocarnitine. 
     
     
         8 . The low salt ophthalmic pharmaceutical composition according to  claim 7  comprising erythritol at a concentration of about 0.25% (w/w) and levocarnitine at a concentration of about 0.25% (w/w). 
     
     
         9 . The low salt ophthalmic pharmaceutical composition according to  claim 1 , further comprising a tonicity agent, wherein said tonicity agent is glycerin present at a concentration of about 1.0% (w/w). 
     
     
         10 . The low salt ophthalmic pharmaceutical composition according to  claim 1 , further comprising a preservative. 
     
     
         11 . The low salt ophthalmic pharmaceutical composition according to  claim 10 , wherein said preservative is a stabilized oxychloro complex present at a concentration of about 0.01% (w/w). 
     
     
         12 . The low salt ophthalmic pharmaceutical composition according to  claim 11  further comprising a buffer. 
     
     
         13 . The low salt ophthalmic pharmaceutical composition according to  claim 12 , wherein said buffer is boric acid present at a concentration of about 0.6% (w/w). 
     
     
         14 . The low salt ophthalmic pharmaceutical composition according to  claim 13  further comprising a pH adjustment agent. 
     
     
         15 . The low salt ophthalmic pharmaceutical composition according to  claim 14 , wherein said pH adjustment agent is NaOH. 
     
     
         16 . The low salt ophthalmic pharmaceutical composition according to  claim 14  having pH of about 7.3. 
     
     
         17 . A low salt ophthalmic pharmaceutical composition comprising:
 castor oil at a concentration of about 0.25% (w/w);   polysorbate 80 at a concentration of about 0.5% (w/w);   acrylate/C 10 -C 30  acrylate crosspolymer at a concentration of about 0.1% (w/w), wherein said acrylate/C 10 -C 30  acrylate crosspolymer has a standard emulsion viscosity between 1,700 and 4,500 cPs;   carboxymethylcellulose sodium at a concentration of about 0.5% (w/w);   glycerin at a concentration of about 1.0% (w/w);   a stabilized oxychloro complex preservative at a concentration of about 0.01% (w/w);   boric acid at a concentration of about 0.6% (w/w);   erythritol at a concentration of about 0.25% (w/w);   levocarnitine at a concentration of about 0.25% (w/w);   NaOH; and   
       water. 
     
     
         18 . A method for treating dry eye syndrome comprising:
 administering to a subject in need of treatment of dry eye syndrome a low salt ophthalmic pharmaceutical composition according to  claim 17 ;   thereby treating said dry eye syndrome.   
     
     
         19 . The method of  claim 18  wherein the ophthalmic composition is applied at least once a day to treat dry eye. 
     
     
         20 . The method of  claim 19  wherein the ophthalmic composition reduces pain and inflammation associated with dry eye.