Sustained delivery of therapeutic agents to an eye compartment

A method for treating an eye disorder in a patient in need thereof, comprising administering by intravitreal injection into the vitreous chamber of the eye an effective amount of a drug delivery system which comprises:

• (i) microparticles including a core which includes the biodegradable polymer polylactide-co-glycolide;
• (ii) a coating non-covalently associated with the microparticles, wherein the coating is a molecule that has a hydrophilic region and a hydrophobic region, and wherein the hydrophilic region is polyethylene glycol;
• and
• (iii) a therapeutically effective amount of an anti-angiogenic agent,
• wherein the drug delivery system provides sustained release of the anti-angiogenic agent into the vitreous chamber over a period of time of at least three months;
• and
• wherein the vitreous chamber of the eye exhibits at least 10% less inflammation or intraocular pressure than if the particles were uncoated, for at least about 30 days post-administration.

An injectable composition for administration to the vitreous chamber of the eye of a patient, comprising a drug delivery system that comprises:

• (i) microparticles having a diameter of 30 μm or less including a core which includes the biodegradable polymer polylactide-co-glycolide;
• (ii) a coating non-covalently associated with the microparticles, wherein the coating is formed of a molecule that has a polyethylene glycol hydrophilic region and a hydrophobic region;
• (iii) a therapeutically effective amount of an anti-angiogenic agent;
• (iv) in a sterile suspension suitable for intravitreal delivery;
• wherein the drug delivery system provides sustained release of the anti-angiogenic agent into the vitreous chamber of the eye of the patient over a period of time of at least three months and
• wherein the vitreous chamber of the eye exhibits at least 10% less inflammation or intraocular pressure than if the particles were uncoated, for at least about 30 days post-administration.

A drug delivery system for intravitreal injection into the vitreous chamber of the eye of a patient, comprising:

• (i) microparticles having a diameter of 30 μm or less including a core which includes the biodegradable polymer polylactide-co-glycolide;
• (ii) a coating non-covalently associated with the microparticles, wherein the coating is a molecule that has a hydrophilic region and a hydrophobic region, and wherein the hydrophilic region is polyethylene glycol;
• (iii) a therapeutically effective amount of a anti-angiogenic agent;
• (iv) in a sterile suspension;
• and
• (v) a means for intravitreal injection;
• wherein the drug delivery system provides sustained release of the anti-angiogenic agent into the vitreous chamber of the eye patient's over a period of time of at least three months and wherein the vitreous chamber of the eye exhibits at least 10% less inflammation or intraocular pressure than if the particles were uncoated for at least about 30 days post-administration.

A method for treating macular degeneration in a human in need thereof, comprising administering by intravitreal injection into the vitreous chamber of the eye of a patient an effective amount of a drug delivery system which comprises:

• (i) microparticles having a diameter of 30 μm or less including a core which consists essentially of the biodegradable polymer polylactide-co-glycolide;
• (ii) a coating non-covalently associated with the microparticles, wherein the coating is a molecule that has a polyethylene glycol hydrophilic region and a hydrophobic region,
• (iii) a therapeutically effective amount of an anti-VEGF agent,
• wherein the drug delivery system provides sustained release of the anti-VEGF agent into the vitreous chamber over a period of time of at least three months;
• wherein the vitreous chamber of the eye exhibits at least 10% less inflammation or intraocular pressure than if the particles were uncoated for at least about 30 days post-administration;
• and
• wherein the drug delivery system is lyophilized and then reconstituted prior to administration by intravitreal injection in a sterile suspension that includes a suspending agent.

An injectable composition for administration to the vitreous chamber of the eye of a patient, comprising a drug delivery system that comprises:

• (i) microparticles having a diameter of 30 μm or less including a core which includes the biodegradable polymer polylactide-co-glycolide;
• (ii) a coating non-covalently associated with the microparticle;
• wherein the coating is a molecule that has a polyethylene glycol hydrophilic region and a hydrophobic region;
• (iii) a therapeutically effective amount of an anti-VEGF agent;
• (iii) in a sterile suspension suitable for intravitreal delivery that includes a suspending agent;
• wherein the drug delivery system provides sustained release of the anti-VEGF agent into the vitreous chamber of the eye over a period of time of at least three months, and
• wherein the vitreous chamber of the eye exhibits at least 10% less inflammation or intraocular pressure than if the particles were uncoated for at least about 30 days post-administration.

An injectable system for intravitreal injection into the vitreous chamber of the eye of a patient, comprising a drug delivery system that comprises:

• (i) microparticles having a diameter of 30 μm or less including a core which includes the biodegradable polymer polylactide-co-glycolide;
• (ii) a coating non-covalently associated with the microparticles;
• wherein the coating is a molecule that has a polyethylene glycol hydrophilic region and a hydrophobic region;
• (iii) a therapeutically effective amount of an anti-VEGF agent;
• (iv) in a sterile suspension, wherein the sterile suspension includes a suspending agent;
• and
• (v) a means for intravitreal injection.

A method for treating an eye disorder in a patient in need thereof, comprising administering by intravitreal injection into the vitreous chamber of the eye an effective amount of a drug delivery system which comprises:

• (i) microparticles including a core which includes the biodegradable polymer polylactide-co-glycolide;
• (ii) a coating non-covalently associated with the microparticles;
• wherein the coating is a molecule that has a hydrophilic region and a hydrophobic region, and wherein the hydrophilic region is polyethylene glycol;
• (iii) a therapeutically effective amount of an anti-angiogenic agent,
• wherein the drug delivery system provides sustained release of the anti-angiogenic agent into the vitreous chamber over a period of time of at least three months;
• and
• wherein the vitreous chamber of the eye exhibits at least 10% less inflammation or intraocular pressure than if the particles were uncoated.

An injectable composition for administration to the vitreous chamber of the eye of a patient, comprising a drug delivery system that comprises:

• (i) microparticles having a diameter of 30 μm or less including a core which includes the biodegradable polymer polylactide-co-glycolide;
• (ii) a coating non-covalently associated with the microparticles;
• wherein the coating is a molecule that has a polyethylene glycol hydrophilic region and a hydrophobic region;
• (iii) a therapeutically effective amount of an anti-angiogenic agent;
• (iv) in a sterile suspension suitable for intravitreal delivery;
• wherein the drug delivery system provides sustained release of the anti-angiogenic agent into the vitreous chamber of the eye of the patient over a period of time of at least three months.

An injectable system for intravitreal injection into the vitreous chamber of the eye of a patient, comprising a drug delivery system that comprises:

• (i) microparticles having a diameter of 30 μm or less including a core which includes the biodegradable polymer polylactide-co-glycolide;
• (ii) a coating non-covalently associated with the microparticles;
• wherein the coating is a molecule that has a polyethylene glycol hydrophilic region and a hydrophobic region;
• (iii) a therapeutically effective amount of an anti-angiogenic agent;
• (iv) in a sterile suspension;
• and
• (v) a means for intravitreal injection,
• wherein the system provides sustained release of the anti-angiogenic agent into the vitreous chamber of the eye patient's over a period of time of at least three months and
• wherein the vitreous chamber of the eye exhibits at least 10% less inflammation or intraocular pressure than if the particles were uncoated.

A method for treating macular degeneration in a human in need thereof, comprising administering by intravitreal injection into the vitreous chamber of the eye of a patient an effective amount of a drug delivery system which comprises:

• (i) microparticles having a diameter of 30 μm or less including a core which consists essentially of the biodegradable polymer polylactide-co-glycolide;
• (ii) a coating non-covalently associated with the microparticles;
• wherein the coating is a molecule that has a polyethylene glycol hydrophilic region and a hydrophobic region;
• (iii) a therapeutically effective amount of an anti-VEGF agent,
• wherein the drug delivery system provides sustained release of the anti-VEGF agent into the vitreous chamber over a period of time of at least three months;
• wherein the vitreous chamber of the eye exhibits at least 10% less inflammation or intraocular pressure than if the particles were uncoated;
• and
• wherein the drug delivery system is lyophilized and then reconstituted prior to administration by intravitreal injection in a sterile suspension that includes a suspending agent.

An injectable composition for administration to the vitreous chamber of the eye of a patient, comprising a drug delivery system that comprises:

• (i) microparticles having a diameter of 30 μm or less including a core which includes the biodegradable polymer polylactide-co-glycolide;
• (ii) a coating non-covalently associated with the microparticles;
• wherein the coating is a molecule that has a polyethylene glycol hydrophilic region and a hydrophobic region;
• (iii) a therapeutically effective amount of an anti-VEGF agent;
• (iv) in a sterile suspension suitable for intravitreal delivery that includes a suspending agent;
• wherein the drug delivery system provides sustained release of the anti-VEGF agent into the vitreous chamber of the eye over a period of time of at least three months and
• wherein the vitreous chamber of the eye exhibits at least 10% less inflammation or intraocular pressure than if the particles were uncoated.

An injectable system for intravitreal injection into the vitreous chamber of the eye of a patient, comprising a drug delivery system that comprises:

• (i) microparticles having a diameter of 30 μm or less including a core which includes the biodegradable polymer polylactide-co-glycolide;
• (ii) a coating non-covalently associated with the microparticles;
• wherein the coating is a molecule that has a polyethylene glycol hydrophilic region and a hydrophobic region;
• (iii) a therapeutically effective amount of an anti-VEGF agent;
• (iv) in a sterile suspension, wherein the sterile suspension includes a suspending agent;
• and
• (x) a means for intravitreal injection.