Tyrosine kinase microsphers
First Claim
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1. A biodegradable intravitreal implant comprising:
- a plurality of biodegradable polymer microspheres encapsulating a tyrosine kinase inhibitor (TKI), the microspheres releasing the TKI at a rate effective to sustain release of the TKI from the microspheres for at least about one week after the implant is placed in the vitreous of an eye.
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Abstract
Biocompatible intraocular microspheres include a tyrosine kinase inhibitor and a biodegradable polymer that is effective to facilitate release of the tyrosine kinase inhibitor into the vitreous of an eye for an extended period of time. The therapeutic agents of the microspheres can be associated with a biodegradable polymer matrix, such as a matrix that is substantially free of a polyvinyl alcohol. The microspheres can be placed into an eye to treat or reduce the occurrence of one or more ocular conditions.
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Citations
17 Claims
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1. A biodegradable intravitreal implant comprising:
a plurality of biodegradable polymer microspheres encapsulating a tyrosine kinase inhibitor (TKI), the microspheres releasing the TKI at a rate effective to sustain release of the TKI from the microspheres for at least about one week after the implant is placed in the vitreous of an eye. - View Dependent Claims (2, 3, 4)
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5. A process for making biodegradable active agent microspheres, the process comprising the steps of:
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(a) preparing an organic phase, which comprises, an active agent, a biodegradable polymer, and a solvent for the active agent and the polymer;
(b) preparing a first aqueous phase;
(c) combining the organic and the aqueous phase to form an emulsion;
(d) preparing a second aqueous phase;
(e) adding the second aqueous phase to the emulsion to form a solution (f) stirring the solution, and;
(g) evaporating the solvent, thereby making biodegradable active agent microspheres. - View Dependent Claims (6, 7, 8, 9, 10, 12)
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11. A process for making biodegradable active agent microspheres, the process comprising the steps of:
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(a) preparing a viscous organic phase, which comprises, a TKI, a biodegradable PLGA polymer, and a solvent for the active agent and the PLGA polymer;
(b) crystallizing active agent in the viscous organic phase (c) preparing a first aqueous phase with a pH between about pH 6 and about pH 8;
(d) combining the organic and the aqueous phase to form an emulsion;
(e) crystallizing active agent in the emulsion;
(f) preparing a second aqueous phase with a pH between about pH 4 and about pH 9;
(g) adding the second aqueous phase to the emulsion to form a solution (h) stirring the solution, and;
(i) evaporating the solvent, thereby making biodegradable active agent microspheres. - View Dependent Claims (13)
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- 14. A method of treating an ocular condition of an eye of a patient, comprising the step of placing biodegradable intraocular microspheres into the vitreous of an eye of the patient, the microspheres comprising a TKI and a biodegradable polymer, wherein the microspheres degrades at a rate effective to sustain release of an amount of the TKI from the microspheres effective to treat the ocular condition.
Specification