US2013129830A1PendingUtilityA1
Polymer Protein Microparticles
Est. expiryNov 18, 2031(~5.3 yrs left)· nominal 20-yr term from priority
A61K 9/1647A61P 27/02A61K 9/1641A61K 9/1623A61K 9/5031A61K 9/1617A61K 9/1611A61K 9/5047A61K 38/179A61K 9/14A61K 9/1652A61K 9/5089A61K 38/00A61K 47/36A61K 2039/505A61K 47/34
66
PatentIndex Score
0
Cited by
0
References
0
Claims
Abstract
Microparticles containing a core of therapeutic protein and a cortex of a biocompatible and biodegradable polymer, and methods of making and using the microparticles are provided. The extended release of a therapeutic protein from the microparticles in a physiological solution is demonstrated over an extended period of time.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A composition comprising a protein coated with a polymer, wherein the composition is a particle with a diameter of from about 5 μm to about 40 μm.
2 . The composition of claim 1 , wherein the protein is an antigen-binding protein.
3 . The composition of claim 2 , wherein the protein comprises an Fc domain.
4 . The composition of claim 3 , wherein the protein is an antibody.
5 . The composition of claim 3 , wherein the protein is a receptor-Fc-fusion protein.
6 . The composition of claim 2 , wherein the protein is an antibody fragment.
7 . The composition of claim 5 , wherein the protein is a VEGF-Trap.
8 . The composition of claim 4 , wherein the antibody is a human monoclonal antibody.
9 . The composition of claim 1 , wherein the polymer is a biodegradable polymer.
10 . The composition of claim 9 , wherein the polymer is selected from the group consisting of poly (lactic acid) (PLA), polyanhydride poly[1,6-bis(p-carboxyphenoxy)hexane] (pCPH), poly(hydroxbutyric acid-cohydroxyvaleric acid) (PHB-PVA), polyethylene glycol-poly (lactic acid) copolymer (PEG-PLA), poly- D,L -lactide-co-glycolide (PLGA), polyorthoester (POE), ethyl cellulose (EC), and poly-ε-caprolactone (PCL).
11 . The composition of claim 1 , wherein the protein is either a trap or an antibody, and the polymer is a POE.
12 . The composition of claim 11 , wherein the average diameter of the particle is about 15 μm.
13 . The composition of claim 1 , wherein the protein is either a trap or an antibody, and the polymer is a PLGA.
14 . A microparticle having a diameter of about 2 μm to about 70 μm comprising a protein particle core of about 2 μm to about 12 μm in diameter and a biodegradable polymer cortex.
15 . The microparticle of claim 14 , wherein the biodegradable polymer is selected from the group consisting of poly (lactic acid) (PLA), polyanhydride poly[1,6-bis(p-carboxyphenoxy)hexane] (pCPH), poly(hydroxbutyric acid-cohydroxyvaleric acid) (PHB-PVA), polyethylene glycol-poly (lactic acid) copolymer (PEG-PLA), poly- D,L -lactide-co-glycolide (PLGA), polyorthoester (POE), ethyl cellulose (EC), and poly-ε-caprolactone (PCL).
16 . The microparticle of claim 15 , wherein the protein particle core comprises an antigen-binding protein.
17 . The microparticle of claim 16 , wherein the antigen binding protein is a receptor-Fc-fusion protein.
18 . The microparticle of claim 17 , wherein the protein particle core comprises a VEGF-Trap and the polymer cortex comprises POE, PLA, or PLGA.
19 . The microparticle of claim 16 , wherein the antigen binding protein is an antibody.
20 . The microparticle of claim 19 , wherein the antibody is a human IgG molecule, and the polymer cortex comprises POE, PLA, or PLGA.
21 . A plurality of microparticles having diameters ranging from about 2 μm to about 70 μm comprising a protein particle core of about 2 μm to about 12 μm in diameter and a biodegradable polymer cortex.
22 . The plurality of microparticles of claim 21 , wherein the microparticles degrade at different rates and the protein is released in an aqueous environment over an extended period of time.
23 . The plurality of microparticles of claim 22 , wherein the period of time is at least 3 days.
24 . The plurality of microparticles of claim 23 , wherein the period of time is at least 60 days.
25 . The plurality of microparticles of claim 24 , wherein the protein is an antigen-binding protein.
26 . The plurality of microparticles of claim 25 , wherein the antigen-binding protein is a receptor-Fc-fusion protein.
27 . The plurality of microparticles of claim 26 , wherein the receptor-Fc-fusion protein is a VEGF Trap and the polymer cortex comprises POE, PLA, or PLGA.
28 . The plurality of microparticles of claim 25 , wherein the antigen-binding protein is an antibody.
29 . The plurality of microparticles of claim 28 , wherein the antibody is a human IgG molecule and the polymer cortex comprises POE, PLA, or PLGA.
30 . A method of treating a disease, comprising administering to a patient a therapeutically effective amount of a plurality of microparticles of claim 21 , wherein a therapeutic protein is released from the microparticles over an extended period of time.
31 . The method of claim 30 , wherein the protein is a VEGF-Trap and the polymer is POE, PLA, or PLGA.
32 . The method of claim 31 , wherein the disease is an ocular disease and the microparticles are delivered to the vitreous of the patient at no less than 60 day intervals.
33 . A method of manufacturing a composition comprising a protein and a biodegradable polymer, the method comprising the steps of:
a. obtaining a protein particle; b. suspending the protein particle in a solution comprising the polymer and a solvent; and c. removing the solvent,
wherein a particle is formed comprising the protein coated with the polymer.
34 . The method of claim 33 , wherein the protein particle is obtained by spray drying a solution comprising the protein.
35 . The method of claim 34 , wherein the spray drying is performed by dual-nozzle sonication, single-nozzle sonication, or electrospray.
36 . The method of claim 35 , wherein the solvent is evaporated by creating a dispersion of the protein suspension of step (b) by spray drying.
37 . The method of claim 36 , wherein the solvent is removed by heat evaporation, air evaporation, or extraction.
38 . The method of claim 37 , wherein the polymer is selected from the group consisting of poly (lactic acid) (PLA), polyanhydride poly[1,6-bis(p-carboxyphenoxy)hexane] (pCPH), poly(hydroxbutyric acid-cohydroxyvaleric acid) (PHB-PVA), polyethylene glycol-poly (lactic acid) copolymer (PEG-PLA), poly- D,L -lactide-co-glycolide (PLGA), polyorthoester (POE), ethyl cellulose (EC), and poly-ε-caprolactone (PCL).
39 . The method of claim 38 , wherein the protein is a receptor-Fc-fusion protein or an antibody.
40 . The method of claim 39 , wherein the protein is a VEGF-Trap or an IgG molecule, and the polymer is POE, PLA, or PLGA.
41 . The method of claim 40 , wherein the particle has an average diameter of about 15 μm.
42 . A method for modulating the release of a protein, comprising the step of (a) combining a protein with a biodegradable polymer to form a protein-polymer complex; followed by the step of (b) contacting the protein-polymer complex with a solvent, wherein the polymer degrades over time and the protein is gradually released into the solvent.
43 . The method of claim 42 , wherein step (a) is performed according to claim 39 .
44 . The method of claim 43 , wherein the protein is a VEGF-Trap or an IgG molecule, and the polymer is POE, PLA, or PLGA.
45 . The method of claim 44 , wherein the particle has an average diameter of about 15 μm.
46 . The method of claim 45 , wherein the protein is released from the protein-polymer complex over at least three days.
47 . The method of claim 45 , wherein the protein is released from the protein-polymer complex over at least 60 days.
48 . The method of claim 47 , wherein the solvent is buffered saline.
49 . The method of claim 47 , wherein the solvent is in vivo.
50 . The method of claim 49 , wherein the solvent is vitreous humour.Join the waitlist — get patent alerts
Track US2013129830A1 — get alerts on status changes and closely related new filings.
We store only your email — no account needed. See our privacy policy.