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Intraocular drug delivery systems

A technology of delivery system and drug, applied in the field of drug delivery system for the treatment of eye diseases, can solve the problems of increasing healing time, patient discomfort and the risk of infection or other complications, etc.

Inactive Publication Date: 2009-11-25
ALLERGAN INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since such sutures or ocular fixations have only peripheral or auxiliary value, their application can increase healing time, patient discomfort, and risk of infection or other complications

Method used

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  • Intraocular drug delivery systems
  • Intraocular drug delivery systems

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0149] 2-Methoxyestradiol Polylactic Acid Microspheres (Rabbit)

[0150] In this experiment, PLA-based microspheres containing the active agent 2-methoxyestradiol were prepared and administered by injection into various intraocular sites in rabbit eyes. Remarkably, we found that the microspheres were well tolerated and all eye redness (eye surface hyperemia) disappeared (disintegration) within one week after intraocular administration. Thus, administration of these microspheres by the methods described herein does not result in significant hyperemia of the inner surface of the eye.

[0151] The microspheres used in this experiment contained 29.7 wt% of 2-methoxyestradiol as the therapeutic agent and 70.3 wt% of poly(D,L) lactic acid polymer (Birmingham) with an intrinsic viscosity (iv) of 1.2 dL / gm. Before administration, the microspheres were suspended in isotonic phosphate buffered saline (IPBS) at pH 7.4 as the microsphere carrier. This microsphere suspension containe...

Embodiment 2

[0172] Subconjunctival brimonidine polylactic acid microspheres (rabbit)

[0173] Two experiments were performed in which lactic acid polymer, brimonidine therapeutic agent microspheres were prepared and injected into the subconjunctival space of rabbit eyes with a syringe. PLA brimonidine microspheres are injected as a suspension in an aqueous carrier such as isotonic phosphate buffered saline. The viscosity of the microsphere suspension is up to about 200,000 cps at 20°C. Brimonidine-containing microspheres are injected subconjunctivally (with a 25-30 gauge syringe needle) to deliver therapeutic levels of the therapeutic agent (brimonidine) in the anterior chamber (for example, to treat ocular hypertension) and / or the posterior chamber of the eye A therapeutic level of the therapeutic agent (brimonidine) is provided for the treatment of retinal diseases.

[0174] Notably, PLA microspheres containing brimonidine were well tolerated in both experiments (no hyperemia after ...

Embodiment 3

[0192] Intraocular Brimonidine PLA Implant (Rabbit)

[0193] I. Subfascial Implantation

[0194] A. In the first experiment, brimonidine tartrate PLA implants were implanted in the anterior subfascial space. 3 or 6 brimonidine tartrate implants (each implant containing 400 μg brimonidine tartrate) were implanted in the anterior subfascial region ( implant placement as figure 1 shown in the lower right photo). Three implants (total dose 1200 μg) were placed in 3 rabbits, 6 implants (total dose 2400 μg) were placed in 3 rabbits, and placebo implants were also placed in 3 rabbits.

[0195] figure 1 Placement of the implant was shown to result in a reduction in intraocular pressure within 50 days, with a dose response occurring. IOP was measured with a barometric tonometer.

[0196] The implant was placed in the anterior subfascial space by grasping the conjunctiva approximately 3-4 mm posterior to the limbus with toothed forceps. Wescott scissors were used to enter the c...

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Abstract

Biodegradable implants sized and suitable for implantation in an ocular region or site and methods for treating ocular conditions. The implants such as microsheres provide an extended release of an active agent at a therapeutically effective amount for a period of time between 10 days and one year or longer. The active is selected from estradiols such as 2-methoxyestradiol or alpha2-adrenergic agonists such as brimonidine and its derivates or prostagladin analogis.

Description

Background technique [0001] The present invention relates to drug delivery systems and methods for the treatment of ocular diseases. In particular, the present invention relates to systems and methods for treating eye diseases by administering a sustained release drug delivery system comprising a therapeutic agent and a bioerodible polymer to an ocular region or site. [0002] Eye disease may include a disease, aliment or condition affecting or involving the eye or one of the parts or regions of the eye. Broadly speaking, the eye includes the eyeball and the tissues and fluids that make it up, the muscles that surround the eye (such as the oblique and rectus muscles), and the portion of the optic nerve in and near the eyeball. A front of eye ocular condition is a disease, mild disease, or disease. Thus, anterior ophthalmopathy primarily affects or involves the conjunctiva, cornea, conjunctiva, anterior chamber, iris, posterior chamber (behind the iris but anterior to the po...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61F2/14A61K9/00A61K9/10A61K9/16A61K9/50A61K31/557A61K31/565A61K47/34A61K47/48
CPCA61K9/1694A61K31/565A61K9/5031A61K31/498A61K9/10A61F9/0017A61K9/0051A61K9/1635A61K31/557A61P27/00A61P27/02A61P27/06A61K47/50A61K9/16A61K9/50A61K47/30A61K9/0048A61K47/34
Inventor M·R·罗宾逊W·M·布兰达P·M·休斯G·鲁伊斯W·C·奥瑞拉S·M·惠特卡普林瓊恩D·F·韦尔蒂L·T·斯帕达
Owner ALLERGAN INC
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