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.
Claims28
A therapeutic nanoparticle having a hydrodynamic diameter of the therapeutic nanoparticle of about 70 to about 130 nm;
- comprising:
- about 5 to about 30 weight percent of a therapeutic agent;
- about 10 to about 99 weight percent of a diblock poly(lactic) acid-poly(ethylene)glycol copolymer, wherein said diblock poly(lactic) acid-poly(ethylene)glycol copolymer comprises 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 about 0.2 to about 10 weight percent of a polymer conjugate represented by:
- PLA-PEG-ligand;
- wherein the ligand is covalently bound to the PEG, and wherein PLA is poly(lactic)acid and PEG is poly(ethylene)glycol;
- and wherein the particle releases less than about 5% of the therapeutic agent over 1 hour when placed in a phosphate buffer solution at room temperature.
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 a chemotherapeutic agent;
- 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, about 0.2 to about 10 weight percent of a polymer conjugate represented by:
- PLA-PEG-ligand;
- wherein the ligand is covalently bound to the PEG or covalently bound to the PEG through an alkylene linker, and wherein PLA is poly(lactic)acid and PEG is poly(ethylene)glycol and
- a saccharide;
- wherein said nanoparticles are stable for at least 3 days when held at 25° C. in said composition.
A therapeutic nanoparticle having a hydrodynamic diameter of the therapeutic nanoparticle of about 70 to about 130 nm;
- comprising:
- about 5 to about 30 weight percent of a therapeutic agent;
- about 10 to about 99 weight percent of a diblock poly(lactic) acid-poly(ethylene)glycol copolymer, wherein said diblock poly(lactic) acid-poly(ethylene)glycol copolymer comprises 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 about 0.2 to about 10 weight percent of a polymer conjugate represented by:
- PLA-PEG-ligand;
- wherein the ligand is covalently bound to the PEG, and wherein PLA is poly(lactic)acid and PEG is poly(ethylene)glycol;
- and wherein the therapeutic nanoparticle substantially retains the therapeutic agent for at least 5 days at 25° C.
A therapeutic nanoparticle having a hydrodynamic diameter of the therapeutic nanoparticle of about 70 to about 130 nm;
- comprising:
- about 5 to about 30 weight percent of a therapeutic agent;
- about 10 to about 99 weight percent of a diblock poly(lactic) acid-poly(ethylene)glycol copolymer, wherein said diblock poly(lactic) acid-poly(ethylene)glycol copolymer comprises 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 about 0.2 to about 10 weight percent of a polymer conjugate represented by:
- PLA-PEG-ligand;
- wherein the ligand is covalently bound to the PEG, and wherein PLA is poly(lactic)acid and PEG is poly(ethylene)glycol;
- and wherein the therapeutic nanoparticle releases less than 10% of the therapeutic agent over about one minute when placed in a phosphate buffer solution at 37° C.
Dependencies are inferred from the claim text.