US2020306201A1PendingUtilityA1

Targeted Therapeutic Nanoparticles And Methods Of Making And Using Same

Assignee: PFIZERPriority: Jul 3, 2014Filed: Feb 17, 2020Published: Oct 1, 2020
Est. expiryJul 3, 2034(~7.9 yrs left)· nominal 20-yr term from priority
Inventors:Hong Wang
A61K 31/282A61K 31/337A61K 9/5161A61K 31/427A61K 9/5123A61K 31/415A61K 9/5138A61K 9/5153A61K 31/475A61K 47/34B82Y 5/00A61K 9/141A61P 35/00A61K 47/10
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Claims

Abstract

Described herein are polymeric nanoparticles that include a therapeutic agent, and methods of making and using such therapeutic nanoparticles. In some embodiments, the contemplated nanoparticles may include an excipient.

Claims

exact text as granted — not AI-modified
1 . A therapeutic nanoparticle comprising:
 about 5 to about 25 weight percent of an excipient selected from a polyanionic polymer;   about 0.2 to about 35 weight percent of a therapeutic agent, wherein the agent is docetaxel; and   about 35 to about 99.75 weight percent of a biocompatible polymer.   
     
     
         2 . (canceled) 
     
     
         3 . The therapeutic nanoparticle of  claim 1 , wherein the polyanionic polymer is a copolymer of methacrylic acid and methyl methacrylate subunits. 
     
     
         4 . The therapeutic nanoparticle of  claim 3 , wherein the ratio of methacrylic acid to methyl methacrylate subunits is between about 1:0.9 to about 1:3. 
     
     
         5 .- 8 . (canceled) 
     
     
         9 . The therapeutic nanoparticle of  claim 1 , wherein the excipient has a molecular weight of between about 20 kDa and about 60 kDa. 
     
     
         10 . The therapeutic nanoparticle of  claim 1 , wherein the excipient has a molecular weight of between about 100 kDa and about 150 kDa. 
     
     
         11 .- 13 . (canceled) 
     
     
         14 . The therapeutic nanoparticle of  claim 1 , further comprising about 0.05 to about 35 weight percent cyclodextrin. 
     
     
         15 . The therapeutic nanoparticle of  claim 14 , comprising about 15 to about 30 weight percent cyclodextrin 
     
     
         16 . The therapeutic nanoparticle of  claim 14 , wherein the cyclodextrin is selected from the group consisting of α-cyclodextrin, β-cyclodextrin, γ-cyclodextrin, and mixtures thereof. 
     
     
         17 .- 21 . (canceled) 
     
     
         22 . The therapeutic nanoparticle of  claim 1 , wherein the hydrodynamic diameter of the therapeutic nanoparticle is about 60 to about 200 nm. 
     
     
         23 . (canceled) 
     
     
         24 . The therapeutic nanoparticle of  claim 1 , wherein the biocompatible polymer is selected from the group consisting of poly(lactic) acid-poly(ethylene)glycol copolymer and poly(lactic) acid-co-poly(glycolic) acid-poly(ethylene)glycol copolymer. 
     
     
         25 . The therapeutic nanoparticle of  claim 24 , wherein the poly(lactic) acid-poly(ethylene)glycol copolymer has a poly(lactic) acid number average molecular weight fraction of about 0.6 to about 0.95. 
     
     
         26 .- 28 . (canceled) 
     
     
         29 . The therapeutic nanoparticle of  claim 1 , wherein the therapeutic nanoparticle comprises about 10 to about 25 weight percent poly(ethylene)glycol. 
     
     
         30 .- 31 . (canceled) 
     
     
         32 . The therapeutic nanoparticle of  claim 1 , wherein the therapeutic nanoparticle comprises about 20 to about 30 weight percent poly(ethylene)glycol. 
     
     
         33 . The therapeutic nanoparticle of  claim 1 , further comprising a 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-poly(ethylene)glycol copolymer. 
     
     
         34 . The therapeutic nanoparticle of  claim 1 , wherein the nanoparticle substantially immediately releases less than about 70% of the therapeutic agent after 0.5 hours when placed in a phosphate buffer solution at 37° C. 
     
     
         35 . (canceled) 
     
     
         36 . A pharmaceutically acceptable composition comprising a plurality of therapeutic nanoparticles of  claim 1  and a pharmaceutically acceptable excipient. 
     
     
         37 . The pharmaceutically acceptable composition of  claim 36 , further comprising a saccharide and/or cyclodextrin. 
     
     
         38 . The pharmaceutically acceptable composition of  claim 37 , wherein the saccharide is a disaccharide selected from the group consisting of sucrose or trehalose, or a mixture thereof. 
     
     
         39 . The pharmaceutically acceptable composition of  claim 37 , wherein the cyclodextrin is selected from the group consisting of α-cyclodextrin, β-cyclodextrin, γ-cyclodextrin, and mixtures thereof. 
     
     
         40 .- 64 . (canceled)

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