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Details for Patent: 6,265,389

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Details for Patent: 6,265,389

Title: Microencapsulation and sustained release of oligonucleotides
Abstract:This invention relates to a composition, and method of forming and using said composition, for the sustained release of oligonucleotides, in particular antisense ODNs. The sustained release composition of this invention comprises a polymer matrix of a biocompatible polymer and stabilized oligonucleotide, wherein the stabilized oligonucleotide is dispersed within the biocompatible polymer. The method of the invention, for forming a composition for the sustained release of oligonucleotide, in particular an antisense ODN, includes dissolving a polymer in a polymer solvent to form a polymer solution, dispersing stabilized oligonucleotide in the polymer solution, and then solidifying the polymer to form a polymeric matrix containing a dispersion of the stabilized oligonucleotide. The method of using the sustained release composition of the present invention comprises providing a therapeutically effective blood level of oligonucleotide in a subject for a sustained period by administering to the subject a dose of the sustained release composition described herein.
Inventor(s): Burke; Paul A. (Oxnard, CA)
Assignee: Alkermes Controlled Therapeutics, Inc. (Cambridge, MA)
Filing Date:Jun 25, 1998
Application Number:09/104,549
Claims:1. A composition for the sustained release of an antisense oligonucleotide from a polymer matrix, comprising:

a) a biocompatible polymer; and

b) a therapeutically effective amount of antisense oligonucleotide which is complexed with a metal cation, wherein said antisense oligonucleotide is dispersed within the biocompatible polymer.

2. The sustained release composition of claim 1 wherein the metal cation-complexed antisense oligonuclcotide is in the form of particles.

3. The sustained release composition of claim 1 wherein the biocompatible polymer is selected from the group consisting of poly(lactides), poly(glycolides), poly(lactide-co-glycolides), poly(lactic acid)s, poly(glycolic acid)s, poly(lactic acid-co-glycolic acid)s, polycaprolactone, polycarbonates, polyesteramides, polyanhydrides, poly(amino acids), polyorthoesters, polycyanoacrylates, poly(p-dioxanone), poly(alkylene oxalate)s, biodegradable polyurethanes, blends and copolymers thereof.

4. The sustained release composition of claim 3 wherein said polymer comprises poly(lactide-co-glycolide).

5. The sustained release composition of claim 1 wherein the metal cation of the metal cation-complexed antisense oligonucleotide is multivalent.

6. The sustained release composition of claim 5 wherein the multivalent metal cation comprises a cation selected from the group consisting of: Zn.sup.+2, Ca.sup.+2, Cu.sup.+2, Mg.sup.+2 and any combination thereof.

7. The sustained release composition of claim 6 wherein the metal cation is Zn.sup.+2.

8. The sustained release composition of claim 1 wherein the antisense oligonucleotide which is complexed to the metal cation has SEQ ID NO. 1.

9. The sustained release composition of claim 1 wherein the antisense oligonucleotide which is complexed to the metal cation has SEQ ID NO. 2.

10. The sustained release composition of claim 1 wherein the antisense oligonucleotide which is complexed to the metal cation is present from about 0.01% (w/w) to about 50% (w/w) based on the dry weight of the composition and the weight of the antisense oligonucleotide prior to stabilization.

11. A method for providing a therapeutically effective amount of an antisense oligonucleotide in a subject for a sustained period comprising administering to the subject a dose of the sustained release composition of claim 1.

12. A method for forming a composition for the sustained release of an antisense oligonucleotide, comprising the steps of:

a) dissolving a biocompatible polymer in a polymer solvent to form a polymer solution;

b) adding a therapeutically effective amount of antisense oligonucleotide which is complexed with a metal cation, to the polymer solution; and

c) solidifying the polymer to form a polymer matrix containing a dispersion of said antisense oligonucleotide.

13. The method of claim 12 wherein the biocompatible polymer is selected from the group consisting of poly(lactides), poly(glycolides), poly(lactide-co-glycolides), poly(lactic acid)s, poly(glycolic acid)s, poly(lactic acid-co-glycolic acid)s, polycaprolactone, polycarbonates, polyesteramides, polyanhydrides, poly(amino acids), polyorthoesters, polycyanoacrylates, poly(p-dioxanone), poly(alkylene oxalate)s, biodegradable polyurethanes, blends, and copolymers thereof.

14. The method of claim 13 wherein said polymer comprises poly(lactide-co-glycolide).

15. The method of claim 12 wherein the metal cation which is complexed to the antisense oligonucleotide is a multivalent metal cation.

16. The method of claim 15 wherein the multivalent metal cation is selected from the group consisting of: Zn.sup.+2, Ca.sup.+2, Cu.sup.+2, Mg.sup.+2, and any combination thereof.

17. The method of claim 16 wherein the metal cation is Zn.sup.+2.
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