Pharmaceutical composition of nanoparticles for protein drug delivery
View Patent ↗The invention discloses a pharmaceutical composition of bioactive nanoparticles composed of chitosan, poly-glutamic acid, and a bioactive agent for oral delivery. The chitosan-based nanoparticles are characterized with a positive surface charge and enhanced permeability for oral drug delivery.
1. A composition of nanoparticles, the nanoparticles consisting of positively charged chitosan, optionally a zero-charge substance or bioactive agent, and a negatively charged substrate having gadolinium (Gd) chelated to the negatively charged substrate, wherein said negatively charged substrate is neutralized with a portion of said positively charged chitosan in a core portion of said nanoparticles.
2. The composition of claim 1 , wherein said chitosan is N-trimethyl chitosan, EDTA-chitosan, low molecular weight chitosan, PEG-chitosan, mono-N-carboxymethyl chitosan, chitosan derivatives, or combinations thereof.
3. The composition of claim 2 , wherein a ligand is attached to a free —NH 3 group of the N-trimethyl chitosan.
4. The composition of claim 3 , wherein the ligand is galactosamine.
5. The composition of claim 3 , wherein the ligand includes a substrate, inhibitor, activator, or neurotransmitter.
6. The composition of claim 1 , wherein said negatively charged substrate is a PGA-complexone conjugate, γ-PGA, α-PGA, derivatives of PGA, salts of PGA, or combinations thereof.
7. The composition of claim 6 , wherein the PGA-complexone conjugate is PGA-DTPA.
8. The composition of claim 1 , wherein said nanoparticles are formulated into a tablet or pill configuration.
9. The composition of claim 8 , wherein said tablet or pill is treated with an enteric coating polymer.
10. The composition of claim 1 , wherein said nanoparticles are encapsulated in a capsule.
11. The composition of claim 10 , wherein said capsule further comprises a pharmaceutically acceptable carrier, diluent, excipient, or absorption enhancer.
12. The pharmaceutical composition of claim 10 , wherein said capsule further comprises at least a solubilizer, bubbling agent, or emulsifier.
13. The composition of claim 10 , wherein said capsule is treated with an enteric coating polymer.
14. The composition of claim 1 , wherein said nanoparticles are freeze-dried, thereby said nanoparticles being in a powder form.
15. The composition of claim 1 , wherein the nanoparticles are used in enhancing imaging contrast quality or property during an imaging procedure.
16. The composition of claim 1 , wherein the bioactive agent is an anti-cancer drug.
17. The composition of claim 16 , wherein the nanoparticles are used in cancer treatment therapy.
18. The composition of claim 1 , wherein said nanoparticles are administered to an animal subject via an oral or parenteral route.
19. The composition of claim 1 , wherein the bioactive agent is selected from the group consisting of nystatin, antifungal agent, itraconazole, fluconazole, mesalazine, prednisone, a TNF inhibitor, azathioprine (Imuran), methotrexate, or 6-mercaptopurine.
20. The composition of claim 1 , wherein said zero-charge substance is a permeation enhancer.