Timed release of substances to treat ocular disorders

Patent metadata

Field	Value
Publication number	US-9962333-B2
Application number	US-201414907745-A
Country	US
Kind code	B2
Filing date	Aug 14, 2014
Priority date	Aug 16, 2013
Publication date	May 8, 2018
Grant date	May 8, 2018

Abstract

A system is disclosed for simple, non-invasive, sustained delivery of ophthalmic substances to the interior of the eye, for the prevention and treatment of eye diseases and conditions. Liposomes and inverted micelles are disclosed as suitable vehicles, and timed release of the substances is effected. Delivery methods include coating of a lens or injection into the eye.

First claim

We claim:

1. A liposomal formulation for ocular drug delivery, the formulation defined as:
(a) comprising liposomes with particle sizes selected from the group consisting of 100 to 200 nm hydrodynamic diameters;
(b) exhibiting increased percent encapsulation of drugs into the liposomes compared to encapsulation using a standard, not modified, liposomal formulation; and
(c) comprising a cocktail of at least three different liposomal formulations with hydrophobic anti-oxidants encapsulated within the lipid bilayers, wherein the hydrophobic antioxidants are selected from the group consisting of beta carotene and canthaxanthin, and comprising PC:PE:PG:Cholesterol in varying ratios to customize releasing drugs in timed release from 40 to 200 days the ratios selected from the group consisting of 60:10:0:30; 65:5:5:25 and 60:5:5:30.

2. The drug of claim 1 selected from the group consisting of anti-VEGF antibodies, Bevacizumab (Avastin), Ranibizumab (Lucentis), Pegaptanib (Macugen), Aflibercept (Eylea), Atropine, Flurbiprofen, Physostimine, Azopt, Gentamicin, Pilocarpine, Bacitracin, Goniosol, Polymyxin B, Betadine, Gramicidin, Prednisolone, Betaxolol, Humorsol, Proparacaine, Betoptic, Hylartin, Propine, Brinzolamide, Hypertonic NaCl, Puralube, BSS, Indocycanine Green, Rose Bengal, Carbachol, Itraconazole, Sodium Hyaluronate, Cefazolin, Latanoprost, Suprofen, Celluvisc, Mannitol, Terramycin, Chloramphenicol, Methazolamide, Timolol, Ciloxan, Miconazole, Tobramycin, Ciprofloxacin, Miostat, Triamcinolone, Cosopt, Muro 128, Trifluridine, Demecarium, Neomycin, Tropicamide, Dexamethasone, Neptazane, Trusopt, Dipivefrin, Ocuflo, Vidarabine, Dorzolamide, Ofloxacin, Vira-A, Epinephrine, Oxytetracycline, Viroptic, Fluorescein, Phenylephrine and Xalatan, and combinations thereof.

3. The formulation of claim 1 further comprising a coating wherein the surface of the liposomes are modified by PEGylation to improve stability.

Assignees

• Univ Northern Illinois Board Of Trustees

Inventors

• Gaillard Elizabeth
• Dillon James
• Friedrichs Jason
• Xu Tao
• Hagen Timothy J
• Karumanchi Devi Kalyan

Classifications

• A61K9/0051 Primary

  Ocular inserts or implants · CPC title

• A61K9/0048

  Eye, e.g. artificial tears · CPC title

• A61K9/127

  Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant · CPC title

• A61K47/34

  Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence) · CPC title

• A61K9/1271

  Non-conventional liposomes, e.g. PEGylated liposomes or liposomes coated or grafted with polymers (liposomes as conjugates {A61K47/6911}) · CPC title