Efficient Ophthalmic Drug Delivery for Relief

Introduction

This innovative topical drug delivery system provides an efficient and precise way to administer ophthalmic treatments, offering patients improved comfort and accurate dosing for a variety of eye conditions. Designed to optimize drug delivery to the eye, this system minimizes waste and ensures that therapeutic compounds reach their intended target within the eye, enhancing treatment efficacy. For pharmaceutical companies, eye care providers, and healthcare innovators, this technology represents a powerful tool for advancing ocular therapies and providing high-quality care for patients with eye health needs.

The Challenge: Effective and Comfortable Drug Delivery

Administering drugs to the eye presents unique challenges, as traditional drops or ointments can lead to discomfort, overuse, or imprecise dosing. Patients often struggle with self-administration, resulting in either too much or too little of the medication reaching the affected area. Furthermore, eye conditions such as glaucoma, dry eye, or post-surgical inflammation require regular and precise medication applications for optimal results. Healthcare providers and patients need a drug delivery system that addresses these issues, providing comfort, accuracy, and convenience.

Enhanced Delivery for Targeted Ophthalmic Care

This advanced ophthalmic drug delivery system addresses these challenges by offering a precise, easy-to-use method for administering medications directly to the eye. The system’s design allows for controlled release and targeted delivery, ensuring that each dose reaches the intended area without overflow or irritation. By optimizing the delivery process, this system reduces the risk of wastage and enhances the efficacy of medications, making it ideal for both prescription and over-the-counter ophthalmic treatments. This solution supports patient adherence to treatment regimens, providing consistent relief and promoting faster recovery.

Key Benefits for Pharmaceutical and Eye Care Sectors

For pharmaceutical manufacturers, this ophthalmic drug delivery system provides an opportunity to develop high-quality products that enhance patient outcomes and compliance. Eye care providers can offer this delivery system to improve comfort and effectiveness in treating chronic and acute eye conditions. The technology’s precision also supports healthcare providers in managing patient needs with a system that ensures consistent dosing, reduces treatment time, and improves overall satisfaction. Its adaptability across various ophthalmic applications makes it a versatile solution for advancing eye care.

Invest in Precision Ophthalmic Solutions

Licensing this ophthalmic drug delivery system positions your company as a leader in eye care innovation. By offering a solution that optimizes drug delivery for eye health, your business can meet the growing demand for effective, patient-friendly therapies in ophthalmology. This technology is a valuable investment for companies focused on improving eye health, enhancing drug delivery systems, and advancing patient comfort and satisfaction in ophthalmic care.

Please see terms and conditions

Abstract
Claims

Topical drug delivery systems for ophthalmic use including mixed nanomicellar formulations of water-insoluble drugs and methods of treating diseases affecting the posterior ocular segments are disclosed. In an embodiment, an aqueous ophthalmic solution includes nanomicelles in a physiologically acceptable buffer, having a pH of 5.0 to 8.0, wherein a corticosteroid at a concentration from about 0.01% w/v to about 1.00% w/v is solubilized through entrapment in a mixed micellar hydrophobic core with a corona composed of hydrophilic chains extending from the hydrophobic core, wherein the nanomicelles comprise vitamin E TPGS at a concentration ranging from about 3.0% w/v to about 5.0% w/v stabilized with octoxynol-40 at a concentration ranging from about 1.0% w/v to about 3.0% w/v.

What is claimed is:

1. An aqueous ophthalmic solution comprising nanomicelles in a physiologically acceptable buffer, having a pH of 5.0 to 8.0, wherein the nanomicelles consist essentially of dexamethasone, vitamin E TPGS and octoxynol-40, wherein the dexamethasone at a concentration ranging from about 0.01% w/v to about 1.00% w/v is solubilized through entrapment in a mixed micellar hydrophobic core with a corona composed of hydrophilic chains extending from the hydrophobic core, wherein the vitamin E TPGS at a concentration ranging from about 2.0% w/v to about 5.0% w/v is stabilized with the octoxynol-40 at a concentration ranging from about 1.0% w/v to about 3.0% w/v, wherein the aqueous ophthalmic solution is stable after about 40 days at about 4° C.

2. The aqueous ophthalmic solution of claim 1 wherein the concentration of the dexamethasone is from about 0.05% w/v to about 0.25% w/v.

3. The aqueous ophthalmic solution of claim 1 wherein the pH is in a range from about 6.6 to about 7.0.

4. The aqueous ophthalmic solution of claim 1 wherein the concentration of the vitamin E TPGS is from about 4.0% w/v to about 5.0% w/v.

5. The aqueous ophthalmic solution of claim 1 wherein the concentration of the octoxynol-40 is from about 1.5% w/v to about 2.5% w/v.

6. An eye drop formulation comprising nanomicelles in a physiologically acceptable buffer, wherein the nanomicelles consist essentially of:

dexamethasone at a concentration ranging from about 0.01% w/v to about 1.00% w/v;

vitamin E TPGS at a concentration ranging from about 2.0% w/v to about 5.0% w/v; and

octoxynol-40 at a concentration ranging from about 1.0% w/v to about 3.0% w/v,

wherein the dexamethasone is solubilized through entrapment in a mixed micellar hydrophobic core of the vitamin E TPGS and the octoxynol-40, wherein the aqueous ophthalmic solution is stable after about 40 days at about 4° C.

7. The eye drop formulation of claim 6 wherein the concentration of the dexamethasone is from about 0.05% w/v to about 0.25% w/v.

8. The eye drop formulation of claim 6 wherein the concentration of the vitamin E TPGS is from about 4.0% w/v to about 5.0% w/v.

9. The eye drop formulation of claim 6 wherein the concentration of the octoxynol-40 is from about 1.5% w/v to about 2.5% w/v.

10. The eye drop formulation of claim 6 wherein the dexamethasone is present in the formulation at a concentration of about 0.1 wt % w/v, the vitamin E TPGS is present in the formulation at a concentration of about 4.5% w/v, and the octoxynol-40 is present in the formulation at a concentration of about 2.0% w/v.

11. A kit comprising:

a unit dose of an aqueous ophthalmic solution comprising nanomicelles in a physiologically acceptable buffer, having a pH of 5.0 to 8.0, wherein the nanomicelles consist essentially of dexamethasone, vitamin E TPGS and octoxynol-40, wherein the dexamethasone at a concentration ranging from about 0.01% w/v to about 1.00% w/v is solubilized through entrapment in a mixed micellar hydrophobic core with a corona composed of hydrophilic chains extending from the hydrophobic core, wherein the vitamin E TPGS at a concentration ranging from about 2.0% w/v to about 5.0% w/v is stabilized with the octoxynol-40 at a concentration ranging from about 1.0% w/v to about 3.0% w/v, wherein the unit dose in contained within a vial prepared from a pharmaceutically acceptable packaging material, wherein the aqueous ophthalmic solution is stable after about 40 days at about 4° C.

12. The kit of claim 11 wherein the unit dose is about 50 μL.

13. The kit of claim 11 wherein the dexamethasone is present in the formulation at a concentration of about 0.1 wt % w/v, the vitamin E TPGS is present in the formulation at a concentration of about 4.5% w/v, and the octoxynol-40 is present in the formulation at a concentration of about 2.0% w/v.

14. The kit of claim 11 wherein the pharmaceutically acceptable packaging material is low density polyethylene or high density polyethylene.

15. A method of treating a back-of-the-eye ocular condition with dexamethasone in a patient in need thereof comprising:

administering to an eye of a patient an effective amount of an aqueous ophthalmic solution comprising nanomicelles in a physiologically acceptable buffer, having a pH of 5.0 to 8.0, wherein the nanomicelles consist essentially of dexamethasone, vitamin E TPGS and octoxynol-40, wherein the dexamethasone at a concentration ranging from about 0.01% w/v to about 1.00% w/v is solubilized through entrapment in a mixed micellar hydrophobic core with a corona composed of hydrophilic chains extending from the hydrophobic core, wherein the vitamin E TPGS at a concentration ranging from about 2.0% w/v to about 5.0% w/v is stabilized with the octoxynol-40 at a concentration ranging from about 1.0% w/v to about 3.0% w/v, wherein the aqueous ophthalmic solution is stable after about 40 days at about 4° C.

16. The method of claim 15 wherein the dexamethasone is present in the solution at a concentration of about 0.1 wt % w/v, the vitamin E TPGS is present in the solution at a concentration of about 4.5% w/v, and the octoxynol-40 is present in the solution at a concentration of about 2.0% w/v.

Title

Topical drug delivery systems for ophthalmic use

Inventor(s)

Ashim K. Mitra, Poonam R. Velagaleti, Ulrich M. Grau

Assignee(s)

Aurinia Pharmaceuticals Inc

Patent #

9017725

Patent Date

April 28, 2015