Therapeutic polymeric nanoparticles and methods of making and using same
Described herein are polymeric nanoparticles that include a therapeutic agent which is 2-(3-((7-(3-(ethyl(2-hydroxyethyl)amino)propoxy)quinazolin-4-yl)amino)-1H-pyrazol-5-yl)-N-(3-fluorophenyl)acetamide (also known as AZD1152 hqpa) or a pharmaceutically acceptable salt thereof, and methods of making and using such therapeutic nanoparticles.
1. A therapeutic nanoparticle comprising
about 15 to about 25 weight percent of 2-(3-((7-(3-(ethyl(2-hydroxyethyl)amino)propoxy)quinazolin-4-yl)amino)-1H-pyrazol-5-yl)-N-(3-fluorophenyl)acetamide,
about 7 to about 15 weight percent of pamoic acid, and
a diblock poly(lactic) acid-poly(ethylene)glycol copolymer; wherein the diblock poly(lactic) acid-poly(ethylene)glycol copolymer has a poly(lactic acid) block having a number average molecular weight of about 16 kDa and a poly(ethylene)glycol block having a number average molecular weight of about 5 kDa; wherein the poly(ethylene)glycol block comprises about 10 to 30 weight percent of the therapeutic nanoparticle.
2. A pharmaceutically acceptable composition comprising a plurality of therapeutic nanoparticles of claim 1 and one or more pharmaceutically acceptable excipients, diluents and/or carriers.
3. A composition comprising the pharmaceutically acceptable composition as claimed in claim 2 in combination with an anti-tumour agent.
4. A kit of parts comprising:
a) a lyophilized pharmaceutical composition comprising nanoparticles as claimed in claim 1 ; and
b) instructions for use.
5. The therapeutic nanoparticle of claim 1 , which has a hydrodynamic diameter of 70-140 nm.