Amphiphile-polymer particles

1. A particle comprising:

a water-insoluble polymeric core; and

a nucleic acid and a first amphiphile comprising an amino dendrimer comprising a lipophilic moiety selected from the group consisting of G0-C14 dendrimer, polypropyleneimine tetramine dendrimer generation 1, and ethylenediamine branched polyethyleneimine within the core.

2. The particle of claim 1 , further comprising a shell comprising a second amphiphile surrounding the water-insoluble polymeric core.

3. The particle of claim 1 , wherein the water-insoluble polymeric core comprises one or more polymers selected from a polylactic acid, a polyglycolic acid, and a copolymer of lactic acid and glycolic acid.

4. The particle of claim 2 , wherein the second amphiphile comprises one or more compounds selected from neutral, cationic and anionic lipids, PEG-phospholipid, and a PEG-ceramide.

5. The particle of claim 4 , wherein the neutral, cationic or anionic lipid is lecithin; the PEG-phospholipid is 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-3000] or 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-5000]; and the PEG-ceramide is N-palmitoyl-sphingosine-1-{succinyl[methoxy(polyethylene glycol)5000]}.

6. A particle prepared by a process comprising:

obtaining a first solution comprising a water-insoluble polymer, a nucleic acid and a first amphiphile comprising an amino dendrimer comprising a lipophilic moiety selected from the group consisting of G0-C14 dendrimer, polypropyleneimine tetramine dendrimer generation 1, and ethylenediamine branched polyethyleneimine in a water-miscible solvent; and

mixing the first solution with an aqueous second solution to form an aqueous composition comprising the particle.

7. The particle of claim 6 , wherein the process further comprises mixing the aqueous composition with a solution comprising a second amphiphile to form a shell surrounding the core.

8. A pharmaceutical composition comprising the particle of claim 1 , and a pharmaceutically acceptable carrier.

9. A method of preparing a particle according to claim 1 , the method comprising:

obtaining a first solution comprising a water-insoluble polymer, a nucleic acid and a first amphiphile comprising an amino dendrimer comprising a lipophilic moiety selected from the group consisting of G0-C14 dendrimer, polypropyleneimine tetramine dendrimer generation 1, and ethylenediamine branched polyethyleneimine in a water-miscible solvent; and

mixing the first solution with an aqueous second solution to form an aqueous composition comprising the particle.

10. The method of claim 9 , further comprising mixing the aqueous composition with a solution comprising a second amphiphile to form a shell surrounding the core.

11. A method of administering a nucleic acid to a subject, the method comprising administering to the subject in need thereof a pharmaceutical composition according to claim 8 .

12. The particle of claim 1 , further comprising a small-molecule drug within the core.

13. The particle of claim 6 , wherein the first solution further comprises a small-molecule drug.

14. The method of claim 9 , wherein the first solution further comprises a small-molecule drug.

15. The particle of claim 1 or 6 , wherein the nucleic acid comprises siRNA.

16. The particle of claim 1 or 6 , wherein the nucleic acid comprises mRNA.

17. The particle of claim 1 or 6 , wherein the nucleic acid comprises microRNA.

18. The method of claim 9 , wherein the nucleic acid comprises siRNA.

19. The method of claim 9 , wherein the nucleic acid comprises mRNA.

20. The method of claim 9 , wherein the nucleic acid comprises microRNA.