Ophthalmic drug sustained release formulation and uses thereof
Inventors
Utkhede, Deepank • Jones, Catherine • Wiseman, David
Assignees
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Publication Number
US-10603274-B2
Publication Date
2020-03-31
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 patent discloses solid-matrix sustained release ophthalmic drug formulations for topical delivery of a solid ophthalmic drug. The formulations include at least one hydrophobic polymer and at least one hydrophilic polymer, where the hydrophilic polymer is liquid between 20 and 25 C, together with a nonionic surfactant and nepafenac present in a specified w/w range. The release is adapted to provide therapeutically effective levels each day for about two weeks to about 12 weeks.
The solid matrix concept combines hydrophobic and hydrophilic polymers together with a nonionic surfactant to enable prolonged daily therapeutic elution. In embodiments, specific drugs and polymer/surfactant combinations are described, including nepafenac with polycaprolactone and low-molecular-weight liquid PEG, difluprednate with PEG and surfactant, and cyclosporine A with high-molecular-weight PEG plus polycaprolactone and polysorbate 80 or tyloxapol. The stated purpose is sustained release over multiple weeks for ophthalmic use.
The patent also discloses lacrimal medical-device delivery systems that incorporate the sustained-release formulation into device structures intended for ocular delivery. Device embodiments include drug inserts with an impermeable sheath for exposed proximal contact with tear fluid, and punctal plug or lacrimal implant structures with features described for retention and stabilization. The document connects these devices to ophthalmic treatment contexts described for post-cataract surgery inflammation and dry eye, with reported elution profiles indicating prolonged daily release over the stated periods.
Claims Coverage
The provided independent-claim material covers a solid matrix sustained release ophthalmic formulation for topical delivery of a solid ophthalmic drug, adapted for daily therapeutic release over about two weeks to about 12 weeks. The inventive features include polymer selection and physical state, quantitative polymer composition, inclusion of a nonionic surfactant, and the nepafenac loading range. Additional claim material extends to a punctal plug lacrimal implant with an impermeable sheath.
Liquid hydrophilic polymer in a hydrophobic-hydrophilic solid matrix
The formulation includes at least one hydrophobic polymer and at least one hydrophilic polymer, wherein the hydrophilic polymer is liquid between 20 and 25 C, and the at least one hydrophobic polymer is present at about 15 to about 25% (w/w), which is a higher percentage (w/w) than the at least one hydrophilic polymer.
Nonionic surfactant for sustained daily release
The formulation includes a nonionic surfactant.
Nepafenac-loaded solid matrix adapted for daily therapeutically effective release
Nepafenac is present from about 65% to about 75% (w/w), and the formulation is adapted to release the nepafenac at therapeutically effective levels each day for a period of about two weeks to about 12 weeks.
Punctal plug lacrimal implant with exposed proximal tear-fluid contact using an impermeable sheath
A lacrimal implant includes a punctal plug with a drug insert having a drug core formed by the formulation and an impermeable sheath partially covering the drug core, such that an exposed proximal end contacts tear fluid to release the ophthalmic drug when inserted into the lacrimal canaliculus.
The central inventive requirements are the specific hydrophobic/hydrophilic polymer arrangement with a nonionic surfactant, the nepafenac loading range adapted for sustained daily release over about two weeks to about 12 weeks, and the lacrimal implant embodiment with an impermeable sheath and exposed proximal end for tear-fluid contact.
Stated Advantages
Sustained release over multiple weeks for ophthalmic use.
Prolonged daily therapeutic elution.
Therapeutically effective levels each day for about two weeks to about 12 weeks.
Documented Applications
Post-cataract surgery inflammation treatment.
Dry eye treatment.
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