Polymeric nanoparticles and a process of preparation thereof

Abstract

The present invention relates to the field of nanotechnology, in particular, to the production of biodegradable polymeric nanoparticles. The present invention provides a biodegradable polymeric nanoparticle made up of a block copolymer and a process for producing the same. The nanoparticles are produced without the use of any emulsifiers and have a size ranging from 30-120 nm. The methods of controlling the drug loading capacity are disclosed along with the process of producing entity-loaded nanoparticles. Compositions comprising the nanoparticles and their use in therapeutics, diagnostics and theranostics are also disclosed.

1 - 66 . (canceled) 
     
     
         67 . Biodegradable polymeric nanoparticles comprising a poly(lactic acid-polyethylene glycol-polypropylene glycol-polyethylene glycol (PLA-PEG-PPG-PEG) tetra block copolymer or a PLA-PEG-PPG-PEG-PLA penta block copolymer. 
     
     
         68 . The biodegradable polymeric nanoparticles of  claim 67 , wherein the biodegradable polymeric nanoparticle comprises the PLA-PEG-PPG-PEG tetra block copolymer. 
     
     
         69 . The biodegradable polymeric nanoparticles of  claim 67 , wherein the biodegradable polymeric nanoparticle comprises the PLA-PEG-PPG-PEG-PLA penta block copolymer. 
     
     
         70 . The biodegradable polymeric nanoparticles of  claim 67 , wherein the biodegradable polymeric nanoparticle is suitable for delivery in a subject by either intravenous injection, intramuscular injection, or oral routes. 
     
     
         71 . The biodegradable polymeric nanoparticles of  claim 70 , wherein the biodegradable polymeric nanoparticles are suitable for delivery in a subject by intravenous injection. 
     
     
         72 . The biodegradable polymeric nanoparticles of  claim 70 , further comprising a therapeutic agent. 
     
     
         73 . The biodegradable polymeric nanoparticles of  claim 72 , wherein the therapeutic agent is encapsulated, surface conjugated, or adsorbed on the biodegradable polymeric nanoparticles. 
     
     
         74 . The biodegradable polymeric nanoparticles of  claim 73 , wherein the therapeutic agent is selected from a group comprising small organic molecules, polynucleotides, polynucleosides, DNA, RNA, amino acids, peptides, proteins, antibiotics, low molecular weight molecules, chemotherapeutics, drugs, metal ions, dyes, radioisotopes, contrast agents and imaging agents. 
     
     
         75 . The biodegradable polymeric nanoparticles of  claim 74 , wherein the peptide is an anti-cancer peptide or insulin. 
     
     
         76 . The biodegradable polymeric nanoparticles of  claim 67 , further comprising a targeting moiety selected from the group consisting of vitamins, small molecule drugs, ligands, amines, peptide fragments, antibodies, and aptamers. 
     
     
         77 . The biodegradable polymeric nanoparticles of any one of  claim 67 , wherein the PLA has an average molecular weight in the range of about 4,000 to about 90,000 g/mol and/or wherein the PEG-PPG-PEG has an average molecular weight in the range of about 4,000 g/mol to about 15,000 g/mol. 
     
     
         78 . The biodegradable polymeric nanoparticles of  claim 67 , wherein the diameter of the biodegradable polymeric nanoparticles is in the range of about 10 to about 200 nm. 
     
     
         79 . The biodegradable polymeric nanoparticles of  claim 67 , wherein the biodegradable polymeric nanoparticles are substantially free of emulsifier. 
     
     
         80 . The biodegradable polymeric nanoparticles of  claim 75 , wherein the anti-cancer peptide is D- or L-FSRSLHSLL. 
     
     
         81 . The biodegradable polymeric nanoparticles of  claim 75 , wherein the anti-cancer peptide is selected from the group consisting of
 a) CQCRRKN;   b) AQARRKN;   c) RRRRRRRRRCQCRRKN; and   d) RRRRRRRRRAQARRKN.   
     
     
         82 . The biodegradable polymeric nanoparticles of  claim 72 , wherein the therapeutic agent comprises a chemotherapeutic agent selected from the group consisting of paclitaxel, doxorubicin, docetaxel, and gemcitabine. 
     
     
         83 . A method for treating cancer in a subject in need thereof comprising administering the biodegradable polymeric nanoparticles of claim  6  to the subject, wherein the therapeutic agent is selected from the group consisting of an anti-cancer peptide, DNA, oligonucleotide, siRNA and a chemotherapeutic. 
     
     
         84 . The method of  claim 83 , wherein the anti-cancer peptide is D- or L-FSRSLHSLL. 
     
     
         85 . The method of  claim 83 , wherein the anti-cancer peptide is selected from the group consisting of
 a) CQCRRKN;   b) AQARRKN;   c) RRRRRRRRRCQCRRKN; and   d) RRRRRRRRRAQARRKN.   
     
     
         86 . The method of  claim 83 , wherein the chemotherapeutic agent is selected from the group consisting of paclitaxel, doxorubicin, docetaxel, and gemcitabine.