IP Library Granted Patent US 8,603,534
Granted Patent B2
US 8,603,534 · App. 13/903,249 · Granted Dec 10, 2013

Drug loaded polymeric nanoparticles and methods of making and using same

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Quick Facts
Patent No.
US 8,603,534
App. No.
13/903,249
Granted
Dec 10, 2013
Kind
B2
Abstract

The present disclosure generally relates to nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic)acid-poly(ethylene)glycol. Other aspects of the invention include methods of making such nanoparticles.

Claims (22)

1. A therapeutic nanoparticle comprising:

about 4 to about 25 weight percent of an anti-cancer agent, wherein the anti-cancer agent is a kinase inhibitor;

about 10 to about 99 weight percent of a diblock poly(lactic) acid-poly(ethylene)glycol copolymer, wherein said poly(lactic) acid-poly(ethylene)glycol copolymer comprises poly(lactic acid) having a number average molecular weight of about 15 to 20 kDa and poly(ethylene)glycol having a number average molecular weight of about 4 to about 6 kDa; and

wherein the hydrodynamic diameter of the therapeutic nanoparticle is about 60 to about 140 nm; and wherein the therapeutic nanoparticle releases less than 10% of the anti-cancer agent over about one minute when placed in a phosphate buffer solution at 37° C.

2. The therapeutic nanoparticle of claim 1 , wherein the hydrodynamic diameter is about 70 to about 120 nm.

3. The therapeutic nanoparticle of claim 1 , wherein the therapeutic nanoparticle substantially retains the anti-cancer agent for at least 5 days at 25° C.

4. The therapeutic nanoparticle of claim 1 , comprising about 40 to about 90 weight percent diblock poly(lactic) acid-poly(ethylene)glycol copolymer.

5. The therapeutic nanoparticle of claim 1 , wherein the particle releases less than about 5% of the anti-cancer agent over 1 hour when placed in a phosphate buffer solution at room temperature.

6. The therapeutic nanoparticle of claim 1 , wherein the particle releases less than about 10% of the anti-cancer agent over 24 hours when placed in a phosphate buffer solution at room temperature.

7. The therapeutic nanoparticle of claim 4 , wherein said poly(ethylene)glycol has a number average molecular weight of about 5 kDa.

8. A method of treating prostate, breast or hematological tissue cancer comprising administering to a patient in need thereof an effective amount of the therapeutic nanoparticle of claim 1 .

9. A pharmaceutical composition comprising:

a plurality of polymeric nanoparticles each comprising about 5 to about 30 weight percent of an anti-cancer agent; about 70 to about 99 weight percent of a biocompatible polymer, wherein the biocompatible polymer is selected from the group consisting of: a) poly(lactic) acid-poly(ethylene)glycol copolymer, wherein said poly(lactic) acid-poly(ethylene)glycol copolymer comprises poly(lactic acid) having a number average molecular weight of about 16 kDa and poly(ethylene)glycol having a number average molecular weight of about 5 kDa; and b) a combination of a) and poly(lactic) acid; and

a pharmaceutically acceptable excipient;

wherein the hydrodynamic diameter of the polymeric nanoparticle is about 70 to about 130 nm; and wherein the polymeric nanoparticle releases less than 10% of the anti-cancer agent over about one minute when placed in a phosphate buffer solution at 37° C.

10. The pharmaceutical composition of claim 9 , wherein the anti-cancer agent is a kinase inhibitor.

11. The pharmaceutical composition of claim 9 , wherein the pharmaceutically acceptable excipient is sucrose.

12. A pharmaceutical composition comprising:

a plurality of polymeric nanoparticles each having a hydrodynamic diameter of about 60 nm to about 140 nm and comprising about 3 to about 40 weight percent of an anti-cancer agent, wherein said anti-cancer agent is a kinase inhibitor; about 10 to about 99 weight percent of a diblock poly(lactic)acid-poly(ethylene)glycol copolymer comprising poly(lactic)acid having a number average molecular weight of about 15 to about 20 kDa and poly(ethylene)glycol having a number average molecular weight of about 4 to about 6 kDa, and

a saccharide;

wherein said nanoparticles are stable for at least 3 days when held at 25° C. in said composition.

13. The pharmaceutical composition of claim 12 , wherein the saccharide is sucrose.

Assignments (4)
ASSIGNEE ADDRESS CORRECTION Recorded Mar 20, 2023
From: PFIZER INC.
To: PFIZER INC.
Reel/Frame 063119/0087 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 10, 2017
From: BIND THERAPEUTICS, INC.
To: PFIZER INC.
Reel/Frame 041227/0161 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 25, 2014
From: ZALE, STEPHEN E.; TROIANO, GREG; ALI, MIR M.; HRKACH, JEFF; WRIGHT, JAMES
To: BIND BIOSCIENCES, INC.
Reel/Frame 033601/0662 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 25, 2014
From: BIND BIOSCIENCES, INC.
To: BIND THERAPEUTICS, INC.
Reel/Frame 033606/0711 →