POLYMERIC NANOPARTICLES AND A PROCESS OF PREPARATION THEREOF
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.