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. The solution may contain a supratherapeutic concentration of agent(s) so that a therapeutic concentration of a topically administered solution accumulates in a diseased ocular structure sufficient to treat the disease. The agent(s) may be formulated with polymers or other components for extended or slow release to provide a substantially constant concentration over the course of treatment.

Description

[0001] This application is a Continuation of U.S. patent application Ser. No. 10 / 752,124 filed Jan. 6, 2004 which is a Continuation-In-Part of U.S. patent application Ser. No. 10 / 667,161 filed Sep. 19, 2003, which is expressly incorporated by reference herein in its entirety.FIELD OF THE INVENTION [0002] The invention is directed to ocular solutions containing macrolide antibiotics to provide anti-inflammatory and other beneficial effects. BACKGROUND [0003] The eye is naturally bathed internally and externally by ocular fluids. The external portion of the eye is lubricated by lacrimal fluids (tears). The internal portion of the eye has two fluid-containing chambers: the anterior chamber contains the aqueous humor or aqueous, and the posterior chamber contains the vitreous humor or vitreous. [0004] Various conditions require the need to introduce fluids into or on the surface of the eye to replace or replenish naturally occurring fluids. The loss of naturally occurring ocular fluids ...

AI Technical Summary

Benefits of technology

[0006] A substitute for an intraocular irrigating, wash, or volume replacement solution is disclosed. The solution contains a concentration in the range from about 1 ng / ml to about 200 μg / ml of a macrolide antibiotic and / or mycophenolic acid. This provides beneficial properties, such as reducing inflammation at a surgical site (anti-inflammatory effect), inhibiting cell migration and cell proliferation (anti-proliferative and anti-migratory effects), inhibiting the growth of new blood vessels at the site of an ocular tumor (anti-angiogenic effect), reducing the growth of bacteria, fungi, etc. (anti-microbial and anti-fungal effects). Its anti-inflammatory effect desirably occurs without an increase in intraocular pressure, which may occur when steroids are administered to control ocular inflammation. Such a composition may be used in patients undergoing ocular surgery such as cataract surgery, retinal repair, etc.

[0008] In one embodiment, the inventive ocular composition is administered to a patient undergoing cataract surgery. The solution, containing a concentration in the range from about 20 μg / ml to about 200 μg / ml (about 0.002%w / v to about 0.02%w / v) of a macrolide antibiotic and / or mycophenolic acid is introduced within the capsule of the lens after the diseased lens has been removed and before the replacement lens is inserted. Microspheres or microcapsules of the macrolide antibiotic and / or mycophenolic acid can be implanted within the capsule in an alternate embodiment. This can be used to reduce opacification of the posterior capsule, which is a common problem following cataract surgery.

Problems solved by technology

The composition and other properties of these solutions may affect the surgical outcome for the patient, for example, a solution may affect the clarity of the cornea and lens, which may result in decreased visual acuity.