Compositions for delivery of therapeutics into the eyes and methods for making and using same

Abstract

The present invention provides for compositions for administering a therapeutically effective amount of a therapeutic component. The compositions may include an ophthalmically acceptable carrier component; a therapeutically effective amount of a therapeutic component; and a retention component which may be effective to reduce wettability, induce viscosity, increase muco-adhesion, increase meniscus height on a cornea of an eye and/or increase physical apposition to a cornea of an eye of a composition.

1 - 25 . (canceled) 
     
     
         26 . A method of administering a therapeutic component to the cornea of an eye, the method comprising:
 administering a composition comprising:   an aqueous-based ophthalmically acceptable carrier that is at least about 50% by weight water;   a therapeutic component, wherein the therapeutic component is ketorolac;   a retention component in an amount effective to provide the composition with a viscosity greater than the viscosity of saline containing 0.5% (w/v) carboxymethylcellulose having an average molecular weight of 90,000, wherein the retention component is a polyanionic component selected from the group consisting of anionic cellulosic derivatives and mixtures thereof.   
     
     
         27 .- 39 . (canceled) 
     
     
         40 . A method of administering a therapeutic component to the cornea of an eye, the method comprising:
 administering a composition comprising:   an aqueous-based ophthalmically acceptable carrier that is at least about 50% by weight water;   a therapeutic component, wherein the therapeutic component is ketorolac;   a polyanionic component including a first polyanionic component portion having a first molecular weight, and a second polyanionic component having a second molecular weight, the first and second polyanionic component portions being present in an amount effective to facilitate the administration of the therapeutic component through a cornea of an eye when the composition is administered to the eye, the first and second molecular weights being different.   
     
     
         41 . The method of  claim 26 , wherein the retention component is present in an amount in a range of about 0.1% w/v to about 10% w/v. 
     
     
         42 . The method of  claim 26 , wherein the retention component is present in an amount in a range of about 0.1% w/v to about 5% w/v. 
     
     
         43 . The method of  claim 26 , wherein the retention component is present in an amount in a range of about 0.2% w/v to about 5% w/v. 
     
     
         44 . The method of  claim 26 , wherein the retention component is present in an amount in a range of about 0.6% w/v to about 1.8% w/v. 
     
     
         45 . The method of  claim 26 , wherein the average molecular weights of the polyanionic component are about 10,000 to about 5,000,000. 
     
     
         46 . The method of  claim 26 , wherein the average molecular weights of the polyanionic component are about 20,000 to about 2,000,000. 
     
     
         47 . The method of  claim 26 , wherein the polyanionic component consists of carboxymethylcelluloses. 
     
     
         48 . The method of  claim 26 , wherein the viscosity of the composition is in the range of about 200 cps to about 2000 cps. 
     
     
         49 . The method of  claim 40 , wherein each of the polyanionic component portions is present in an amount of about 0.2% w/v to about 5% w/v. 
     
     
         50 . The method of  claim 40 , wherein each of the polyanionic component portions is present in an amount of about 0.4% w/v to about 2.5% w/v. 
     
     
         51 . The method of  claim 40 , wherein each of the polyanionic component portions is present in an amount of about 0.8% w/v to about 1.3% w/v. 
     
     
         52 . The method of  claim 40 , wherein the weight ratio of the first polyanionic component portion to the second polyanionic component portion is about 0.25 to about 4. 
     
     
         53 . The method of  claim 40 , wherein the molecular weights of the first and second polyanionic component portions differ by at least about 50,000. 
     
     
         54 . The method of  claim 40 , wherein the viscosity of the composition is in the range of about 200 cps to about 2000 cps.