US Patent No. 9,835,572

THERAPEUTIC POLYMERIC NANOPARTICLE COMPOSITIONS WITH HIGH GLASS TRANSITION TEMPERATURE OR HIGH MOLECULAR WEIGHT COPOLYMERS


Patent No. 9,835,572
Issue Date December 05,2017
Title Therapeutic Polymeric Nanoparticle Compositions With High Glass Transition Temperature Or High Molecular Weight Copolymers
Inventorship Stephen E. Zale, Hopkinton, MA (US)
Greg Troiano, Pembroke, MA (US)
Mir M. Ali, Woburn, MA (US)
Jeff Hrkach, Lexington, MA (US)
James Wright, Lexington, MA (US)
Assignee PFIZER INC., New York, NY (US)

Claim of US Patent No. 9,835,572

1. A method for identifying therapeutic polymeric nanoparticle compositions with a desired therapeutic agent release rate
profile, comprising:
a) providing a first aqueous suspension of at least one first plurality of polymeric nanoparticles each comprising a therapeutic
agent, a block copolymer having at least one hydrophobic portion and at least one hydrophilic portion, wherein the therapeutic
agent is selected from the group consisting of taxane agents, vinca alkaloids, nitrogen mustard agents, mTOR inhibitors, boronate
esters; and peptide boronic acid compounds;

b) determining the nanoparticle glass transition temperature for the first aqueous suspension;
c) varying the amount or molecular weight of the hydrophobic portion of the block copolymer to provide a second aqueous suspension
comprising a plurality of polymeric nanoparticles each comprising the therapeutic agent, if the glass transition temperature
of step b) is below 37° C.; and

d) repeating steps b) and c) until an aqueous suspension with a glass transition temperature of between about 37° C. and about
50° C. and the desired therapeutic agent release rate profile is obtained.