Intraocular delivery compositions and methods
First Claim
1. A particle comprising calcium phosphate and a pharmacologically active agent at least partially coating the particle or impregnating the particle or both, wherein the particle is adapted to deliver the pharmacologically active agent to an ocular surface of a patient in need thereof for treatment of an ocular disease.
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Abstract
The present invention relates to intraocular drug delivery for treating ocular diseases. Particularly, the invention relates to particles useful for the delivery of certain pharmacologically active agents to treat ocular diseases. The particles contain calcium phosphate core particles, particularly nanoparticles, as delivery agents and adjuvants. The invention also relates to methods of making such particles and to methods of treating ocular disease by delivery of a therapeutic drug to an ocular surface using the particles of this invention. The invention further relates to methods of regulating ocular pressure using certain formulations according to the present invention.
111 Citations
18 Claims
- 1. A particle comprising calcium phosphate and a pharmacologically active agent at least partially coating the particle or impregnating the particle or both, wherein the particle is adapted to deliver the pharmacologically active agent to an ocular surface of a patient in need thereof for treatment of an ocular disease.
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15. A method for preparing particles suitable for the treatment of ocular disease, comprising:
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(a) mixing an aqueous solution of calcium chloride with an aqueous solution of sodium citrate to form a mixture;
(b) adding an aqueous solution a sodium phosphate to the mixture to form a solution;
(c) stirring the solution until particles of the desired size and comprising calcium phosphate are obtained; and
(d) dissolving a therapeutic drug used for the treatment of ocular disease in cellobiose solution and adding this solution to the calcium phosphate particles to form particles that are at least partially coated and at least partially impregnated with the therapeutic drug. - View Dependent Claims (16, 17)
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18. A particle comprising
(a) calcium phosphate, and (b) a pharmacologically active agent selected from the group: - antibiotics, antimicrobial agents, therapeutic monoclonal antibodies, such as tetracycline hydrochloride, leucomycin, penicillin, penicillin derivatives, erythromycin, sulphathiazole and nitrofurazone;
local anesthetics such as benzocaine;
a vasoconstrictor such as phenylephrine hydrochloride, tetrahydrozoline hydrochloride, naphazoline nitrate, oxymetazoline hydrochloride and tramazoline hydrochloride;
cardiotonics such as digitalis and digoxin;
a vasodilators such as nitro-glycerine and papaverine hydrochloride;
antiseptics such as chlorhexidine hydrochloride, hexylresorcinol, dequaliniumchloride and ethacridine;
enzymes such as lysozyme chloride and dextranase;
sex hormones;
hypotensives;
sedatives;
anti-tumor agents;
steroidal anti-inflammatory agents such as hydro-cortisone, prednisone, fluticasone, prednisolone, triamcinolone, triamcinolone acetonide, dexamethasone, betamethasone, beclomethasone, and beclomethasone dipropionate;
non-steroidal anti-inflammatory agents such as acetaminophen, aspirin, aminopyrine, phenylbutazone, mefanamic acid, ibuprofen, diclofenac sodium, indomethacin, colchicine, and probenocid;
enzymatic anti-inflammatory agents such as chymotrypsin and bromelain seratiopeptidase;
anti-histaminic agents such as diphenhydramine hydrochloride, chloropheniramine maleate and clemastine;
anti-allergic agents and antitussive-expectorant antiasthmatic agents such as sodium chromoglycate, codeine phosphate, and isoproterenol hydrochloride;
analgesics; and
anti-migraine compounds at least partially coating the particle or impregnating the particle or both;
wherein the particle is adapted to deliver the pharmacologically active agent to an ocular surface of a patient in need thereof.
- antibiotics, antimicrobial agents, therapeutic monoclonal antibodies, such as tetracycline hydrochloride, leucomycin, penicillin, penicillin derivatives, erythromycin, sulphathiazole and nitrofurazone;
Specification