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US 8,603,534 B2Granted
Drug loaded polymeric nanoparticles and methods of making and using same
AssigneeBIND Therapeutics, Inc.
InventorsStephen E. Zale, Greg Troiano, Mir Mukkaram Ali, Jeff Hrkach, James Wright
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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.
Claims13
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 more elements
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.
5 more elements
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.
1 more element
Dependencies are inferred from the claim text.