Bi-functional co-polymer use for ophthalmic and other topical and local applications
The invention contemplates a copolymer which is a graft or block copolymer useful to change wettability and surface characteristics of biological surfaces. Methods for use of these formulations and coatings to change wettability and sterically stabilize, and lubricate biological surfaces in a subject, for example, in the treatment of dry eye syndrome, and to prevent adherence of unwanted proteins, for example in the treatment of contact lens intolerance, are provided.
1. A composition for contacting an ocular surface of a subject, said composition comprising a graft copolymer having a positively charged backbone and hydrophilic side chains, an active agent for treating ophthalmic disease or condition and a pharmaceutically acceptable carrier.
2. The composition of claim 1 , wherein said graft copolymer is PLL-g-PEG.
3. The composition of claim 1 , wherein said graft copolymer comprises 0.001 to 25% of said composition.
4. The composition of claim 1 , wherein the concentration of said graft copolymer ranges from 0.1 to 3 wt %.
5. The composition of claim 1 , further comprising a second polymer.
6. The composition of claim 1 , further comprising one or more of a surfactant, a preservative, and a pharmaceutical ingredient selected from the group consisting of: a demulcent, an emollient, sodium chloride and a vasoconstrictor.
7. The composition of claim 1 , wherein said active agent is selected from the group consisting of an antibiotic, acetazolamide, antazoline, aspirin, atropine, azelastine, bacitracin, betaxolol, bimatoprost, a botanical drug, lutein, lycopene brimonodine, brinzolamide, carbachol, carteolol, ciprofloxacin, ofloxacin, cromalyn, cyclosporine, a cyclosporine pro-drug, a cyclosporine derivative, an immunomodulators, dapiprazole, dexamethasone, diclofenac, dipivifren, dorzolamide, epinephrine, erythromycin, fluoromethalone, flurbiprofen, gentamycin, a glaucoma medication, gramicidin, homatropine, hydrocortisone, hyoscine, keterolac, ibuprofen, ketotifen, latanaprost, levobunolol, levocabastine, levofloxin, lotepprednol, medrysone, methazolamide, metipranolol, naphazoline, natamycin, nedocromil, neomycin, neuroprotective agents, nonsteroidal anti-inflammatory agents, nepafanec, norfloxacin, ofloxacin olopatadine, oxymetazoline, pemirolast, pheniramine, phenylephrine, pilocarpine, povidone, prednisolone, proparacaine, scopolamine, tetracaine, steroids, sulfacetamide, tetrahydrozoline, hypertonic tears, timolal, tobramycin, travaprost, trifluridine, trimethiprim, tropicamide, unoprostone and zinc.
8. The composition of claim 1 , wherein said active agent consists of an antibiotic selected from the group consisting of fluoroquinolones, vancomycin, cephalosporin, gentamycin, erythromycin, azithromycin, sulfa drugs, bacitracin, gatifloxacin, levofloxin, moxifloxacin and ofoxacin.
9. The composition of claim 1 , wherein said active agent consists of the botanical drug zeaxanthine.
10. The composition of claim 1 , wherein said active agent is selected from the group of glaucoma medications consisting of a prostaglandin, a carbonic anhydrase inhibitor, an epinephrine agonist, an alpha-agonist, and a beta-blocker.
11. The composition of claim 1 , wherein said composition further comprises a poly(ethylene oxide)-polypropylene oxide) block co-polymer surfactant.
12. A pharmaceutical formulation comprising the composition of claim 4 .
13. A kit comprising a sterile pharmaceutical formulation comprising the composition of claim 1 and packaging materials therefore which permit use as an artificial tear product introducible into the eye.
14. A kit comprising an extraocular device coated with the composition of claim 1 or claim 2 , and packaging materials therefore.
15. A kit comprising an extraocular device coated with the composition of claim 3 or claim 4 , and packaging materials therefore.
16. The kit of claim 15 , wherein the packaging materials permit contacting of the extraocular device through the nozzle of an eye care solution container.
17. A method of storing a contact lens for at least 1 hour, comprising providing a contact lens and contacting said lens with a composition comprising a graft copolymer having a positively charged backbone and hydrophilic side chains and a carrier, wherein the concentration of said graft copolymer ranges from 0.001 to 3 wt %.
18. The method of claim 17 , wherein the carrier is a pharmaceutically acceptable carrier.
19. A method of storing a contact lens for at least 1 hour, comprising providing the contact lens and said pharmaceutical formulation of claim 12 .
20. A kit comprising a contact lens and the pharmaceutical formulation of claim 12 , in a container that is unopened subsequent to manufacture.
21. A kit comprising a contact lens and the pharmaceutical formulation of claim 12 , in a container that is reusable.
22. The kit of claim 14 , wherein said extraocular device is an intracorneal inlay.
23. The kit of claim 15 , wherein said extraocular device is an intracorneal inlay.
24. The composition of claim 1 , comprising a low viscosity artificial tear with a viscosity of less than 20 cP, having prolonged tear film break up time.
25. The composition of claim 1 , wherein said positively charged moiety is sufficient as a preservative in a topical ophthalmic formulation.
26. The composition of claim 1 , in a volume sufficient for instillation in the eye.
27. A composition for contacting an ocular surface of a subject comprising a copolymer coated nanoparticle, the surface of said nanoparticle comprising a copolymer having a positively charged backbone and hydrophilic water soluble side chains.
28. The composition of claim 27 , said nanoparticle further comprising an active agent.