Ocular solutions

Abstract

Ocular solutions containing at least one macrolide antibiotic and/or mycophenolic acid provide anti-inflammatory, anti-cell proliferation, anti-cell migration, anti-angiogenesis, antimicrobial, and antifungal effects. In one embodiment, the solution is administered intraocularly after cataract surgery before insertion of a replacement intraocular lens, resulting in reduced posterior capsular opacification which may eliminate the need for a subsequent surgery. The solution may be one that is invasively administered, for example, an irrigation or volume replacement solution containing at least one macrolide antibiotic such as tacrolimus, sirolimus, everolimus, cyclosporine, and ascomycin, or mycophenolic acid. The solution may be one that is non-invasively or topically administered in the form of drops, ointments, gels, creams, etc. and may include eye lubricants and contact lens solutions.

1 . A composition comprising a solution for intraocular administration containing a concentration in the range between about 1 ng/ml to about 200 μg/ml of at least one of a macrolide antibiotic or mycophenolic acid as a substitute for an ocular or operative fluid.  
     
     
         2 . The composition of  claim 1  wherein the macrolide antibiotic is at a concentration of about 1 μg/ml.  
     
     
         3 . The composition of  claim 1  wherein the macrolide antibiotic is at a concentration in the range of about 1 μg/ml to about 20 μg/ml.  
     
     
         4 . The composition of  claim 1  wherein the macrolide antibiotic is at a concentration in the range of about 20 μg/ml to about 200 g/ml.  
     
     
         5 . The composition of  claim 1  wherein the solution is selected from at least one of an irrigation solution, a volume replacement solution, and a wash solution.  
     
     
         6 . The composition of  claim 1  wherein the macrolide antibiotic is at least one of tacrolimus, cyclosporine, sirolimus, everolimus, ascomycin, erythromycin, azithromycin, clarithromycin, clindamycin, lincomycin, dirithromycin, josamycin, spiramycin, diacetyl-midecamycin, tylosin, roxithromycin, ABT-773, telithromycin, leucomycins, and lincosamide.  
     
     
         7 . The composition of  claim 1  wherein the macrolide antibiotic or mycophenolic acid is formulated as at least one of a microcapsule, a microsphere, a microvesicle, and a liposome.  
     
     
         8 . The composition of  claim 1  wherein the macrolide antibiotic or mycophenolic acid is provided to a prepared ocular solution.  
     
     
         9 . The composition of  claim 1  wherein the macrolide antibiotic or mycophenolic acid is provided in formulating an ocular solution.  
     
     
         10 . A therapeutic method comprising providing to an eye of a patient an ocular solution containing at least one of a macrolide antibiotic or mycophenolic acid at a concentration in the range between about 1 ng/ml to about 200 μg/ml to provide a therapeutic effect.  
     
     
         11 . The method of  claim 10  wherein the macrolide antibiotic or mycophenolic acid provides at least one of an anti-inflammatory effect, an anti-cell proliferation effect, an anti-cell migration effect, an anti-angiogenesis effect, an antimicrobial effect, and an antifungal effect.  
     
     
         12 . The method of  claim 10  wherein the macrolide antibiotic or mycophenolic acid provides an anti-inflammatory effect without increased intraocular pressure.  
     
     
         13 . The method of  claim 10  wherein the macrolide antibiotic or mycophenolic acid provides an anti-angiogenic effect in a patient with an ocular tumor, a patient with diabetes, or a patient with sickle cell anemia.  
     
     
         14 . The method of  claim 10  wherein the macrolide antibiotic or mycophenolic acid is at a concentration of about 1 μg/ml.  
     
     
         15 . The method of  claim 10  wherein the macrolide antibiotic or mycophenolic acid is at a concentration ranging from about 1 ng/ml to about 20 μg/ml.  
     
     
         16 . The method of  claim 10  wherein the macrolide antibiotic or mycophenolic acid is at a concentration ranging from about 20 μg/ml to about 200 μg/ml.  
     
     
         17 . A therapeutic method comprising intraocularly administering to a patient undergoing cataract surgery an ocular solution containing at least one of a macrolide antibiotic or mycophenolic acid at a concentration in the range from about 20 μg/ml to about 200 μg/ml within a lens capsule prior to insertion of a replacement intraocular lens.  
     
     
         18 . The method of  claim 17  wherein the solution reduces opacification of the posterior capsule.  
     
     
         19 . The method of  claim 17  wherein the macrolide antibiotic is formulated as at least one of a liposome, a macrosphere, a microsphere, a macrocapsule, a microcapsule, a macrovesicle, and a microvesicle.  
     
     
         20 . The method of  claim 17  wherein the macrolide antibiotic or mycophenolic acid is at a concentration in the range of about 20 μg/ml to about 200 μg/ml.  
     
     
         21 . The method of  claim 19  wherein the macrolide antibiotic or mycophenolic acid is implanted within the capsule.  
     
     
         22 . An article comprising an implantable ocular replacement lens in a solution containing a concentration of a macrolide antibiotic or mycophenolic acid sufficient to provide the lens with at least one effect selected from anti-cell proliferation, anti-cell migration, anti-inflammatory, anti-angiogenesis, antimicrobial, and antifungal.  
     
     
         23 . The article of  claim 22  wherein the concentration is in the range between about 20 μg/ml to about 2000 μg/ml.  
     
     
         24 . The article of  claim 22  wherein the concentration is the range between about 20 μg/ml to about 200 μg/ml.  
     
     
         25 . The article of  claim 22  wherein the macrolide antibiotic is at least one of tacrolimus, cyclosporine, sirolimus, everolimus, ascomycin, erythromycin, azithromycin, clarithromycin, clindamycin, lincomycin, dirithromycin, josamycin, spiramycin, diacetyl-midecamycin, tylosin, roxithromycin, ABT-773, telithromycin, leucomycins, and lincosamide.  
     
     
         26 . An article comprising an implantable ocular replacement lens containing at least one macrolide antibiotic or mycophenolic acid.  
     
     
         27 . The article of  claim 26  wherein the antibiotic or mycophenolic acid is in a solution in which the lens is contained.  
     
     
         28 . The article of  claim 26  wherein the lens is a porous hydrogel and the antibiotic or mycophenolic acid is within the pores of the hydrogel lens.  
     
     
         29 . The article of  claim 26  wherein the antibiotic or mycophenolic acid is in a coating on at least one lens surface.  
     
     
         30 . The article of  claim 26  wherein the lens is implanted in a lens capsule and the implanted lens releases the antibiotic or mycophenolic acid in the lens capsule.  
     
     
         31 . The article of  claim 26  wherein the macrolide antibiotic is at least one of tacrolimus, cyclosporine, sirolimus, everolimus, ascomycin, erythromycin, azithromycin, clarithromycin, clindamycin, lincomycin, dirithromycin, josamycin, spiramycin, diacetyl-midecamycin, tylosin, roxithromycin, ABT-773, telithromycin, leucomycins, and lincosamide.  
     
     
         32 . An article comprising an implantable ocular lens in an opthalmically acceptable medium, the medium further comprising an effective anti-cell proliferative or anti-cell migratory concentration of at least one macrolide antibiotic or mycophenolic acid.  
     
     
         33 . The article of  claim 32  wherein the concentration is in the range between about 20 μg/ml to about 2000 μg/ml.  
     
     
         34 . The article of  claim 32  wherein the concentration is in the range between about 200 μg/ml to about 2000 μg/ml.  
     
     
         35 . The article of  claim 32  wherein the concentration is in the range between about 20 μg/ml to about 200 μg/ml.  
     
     
         36 . The article of  claim 32  wherein the macrolide antibiotic is at least one of tacrolimus, cyclosporine, sirolimus, everolimus, ascomycin, erythromycin, azithromycin, clarithromycin, clindamycin, lincomycin, dirithromycin, josamycin, spiramycin, diacetyl-midecamycin, tylosin, roxithromycin, ABT-773, telithromycin, leucomycins, and lincosamide.