Sustained-release nanoparticle compositions and methods for using the same

Abstract

The present invention is a composition composed of a therapeutic agent encapsulated in a copolymer of an N-alkylacrylamide, a vinyl monomer, and a polyethylene glycol (PEG) conjugate and a method for using the same in the treatment or prevention of a disease or condition.

1 - 3 . (canceled) 
     
     
         4 . A sustained-release nanoparticle composition comprising a therapeutic agent and a cross-linked copolymer of an N-alkylacrylamide, a vinyl monomer selected from the group consisting of a vinyl alcohol, a vinyl ether, a vinyl ester, vinyl pyrrolidone, or a combination of said vinyl monomers, and a polyethylene glycol (PEG) conjugate in nanoparticle form, wherein the weight per weight ratio of the N-alkylacrylamide, vinyl monomer and (PEG) conjugate is 70-90:9-20:1-10, said therapeutic agent being encapsulated in said copolymer. 
     
     
         5 . The sustained-release nanoparticle composition of  claim 4 , wherein said therapeutic agent is selected from the group consisting of antibiotics, antirestenotics, anti-proliferative agents, anti-neoplastic agents, chemotherapeutic agents, cardiovascular agents, anti-inflammatory agents, immunosuppressive agents, anti-apoptotic and anti-tissue damage agents. 
     
     
         6 . The sustained-release nanoparticle composition of  claim 4 , wherein said therapeutic agent comprises an anti-proliferative agent. 
     
     
         7 . The sustained-release nanoparticle composition of  claim 4 , wherein said ratio is 80:15:5. 
     
     
         8 . The sustained-release nanoparticle composition of  claim 4 , wherein said nanoparticles have an average diameter in the range of 20 nm to 100 nm as measured by transmission electron microscopy. 
     
     
         9 . The sustained-release nanoparticle composition of  claim 4 , wherein said therapeutic agent is an anti-apoptotic agent. 
     
     
         10 . The sustained-release nanoparticle composition of  claim 9 , wherein said anti-apoptotic agent is selected from the group consisting of galectin-3, (-)deprenyl, rapamycin, quercetin or a monoamine oxidase inhibitor. 
     
     
         11 . The sustained-release nanoparticle composition of  claim 4 , wherein said therapeutic agent is rapamycin. 
     
     
         12 . A method for localized delivery of a therapeutic agent to a disease site, said method comprising administering to said disease site a sustained-release nanoparticle composition as claimed in  claim 4 . 
     
     
         13 . The method of  claim 12 , wherein said disease site is a site of hyperplasia and said therapeutic agent is an anti-proliferative agent. 
     
     
         14 . The method of  claim 13 , wherein said disease site is a site of restenosis and said anti-proliferative agent is rapamycin.