Topical drug delivery systems for ophthalmic use
First Claim
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°
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Abstract
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.
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Citations
16 Claims
- 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°
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6. An eye drop formulation comprising nanomicelles in a physiologically acceptable buffer, wherein the nanomicelles consist essentially of:
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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.- View Dependent Claims (7, 8, 9, 10)
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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.- View Dependent Claims (12, 13, 14)
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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.- View Dependent Claims (16)
Specification