Ophthalmic drug sustained release formulation and uses thereof
Inventors
Utkhede, Deepank • Jones, Catherine • Wiseman, David
Assignees
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Publication Number
US-11324693-B2
Publication Date
2022-05-10
Expiration Date
Abstract
A solid matrix sustained release ophthalmic formulation for topical delivery of a solid ophthalmic drug to the eye, medical devices, drug cores, drug inserts and drug delivery systems comprising the formulation, methods of manufacturing the formulation, medical devices and their methods thereof for delivering the ophthalmic drug for a treatment period provided herein. The formulation disclosed herein is an admixture of an ophthalmic drug, and a combination of a hydrophobic polymer, a hydrophilic polymer and a surfactant, wherein the drug is eluted daily over an extended period of time at therapeutic dose of drug.
Core Innovation
The invention provides a solid matrix sustained-release ophthalmic formulation for topical delivery of nepafenac, in which the composition includes polycaprolactone, polyethylene glycol (PEG) polymers, tyloxapol, and nepafenac in defined weight-percentage ranges. The solid matrix is configured to elute nepafenac at therapeutically effective levels each day for a treatment period described as about two weeks to about four weeks in the claim coverage, and the disclosed formulation framework supports longer topical treatment periods in the accompanying description.
The formulation concept further specifies a defined combination of a hydrophobic polymer and hydrophilic polymer together with a nonionic surfactant, yielding sustained release from a solid matrix. Polycaprolactone is used as the hydrophobic polymer, and PEG polymers are used as the hydrophilic polymer together with tyloxapol as the nonionic surfactant. The described formulation compositions include nepafenac present as a high fraction of the solid matrix, and the combination is presented as enabling sustained daily elution of the ophthalmic drug.
In addition to the nepafenac formulation, the described disclosure includes solid-matrix sustained-release ophthalmic drug insert/elution examples with other ophthalmic drugs, including difluprednate and cyclosporine. The description reports elution profiles from drug inserts configured with polymer/surfactant matrices and retention structures, and it describes ophthalmic device configurations such as lacrimal implants/punctal plugs and drug inserts. These configurations are presented as enabling sustained delivery over extended periods, including use cases such as post-cataract surgery pain and inflammation, dry eye treatment, and glaucoma.
Claims Coverage
The independent claims cover three inventive features: a defined nepafenac solid matrix sustained-release formulation, a fixed composition version of that formulation, and a drug insert with a sheath body.
Defined nepafenac solid matrix sustained-release formulation
A solid matrix sustained release ophthalmic formulation for topical delivery of nepafenac comprising about 30 to about 15% (w/w) of polycaprolactone, about 5 to about 15% (w/w) of polyethylene glycol (PEG) polymers, about 1 to about 15% w/w of tyloxapol and about 60 to about 70% (w/w) of nepafenac.
Fixed nepafenac solid matrix percentages
A solid matrix sustained release ophthalmic formulation for topical delivery of nepafenac comprising about 20% (w/w) of polycaprolactone, about 10% (w/w) of polyethylene glycol (PEG) polymers, about 4% w/w of tyloxapol and about 66% (w/w) of nepafenac.
Nepafenac drug insert with sheath body
A drug insert for topical delivery of nepafenac comprising a) a solid matrix comprising about 20% (w/w) of polycaprolactone, about 10% (w/w) of polyethylene glycol (PEG) polymers, about 4% w/w of tyloxapol and about 66% (w/w) of nepafenac; and, b) a sheath body disposed at least partially over the solid matrix.
Across the independent claims, the coverage centers on a sustained-release solid matrix using polycaprolactone, PEG polymers, tyloxapol, and nepafenac with defined weight-percentage ranges, and further includes a sheath-body drug insert configuration at least partially covering the solid matrix.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Post-cataract surgery treatment for pain and inflammation.
Dry eye treatment.
Glaucoma treatment.
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