Pharmaceutical composition of nanoparticles
View Patent ↗The invention discloses a composition of nanoparticles composed of positively charged chitosan, one negatively charged substrate, and optionally a zero-charge compound or at least one tumor necrosis factor inhibitor 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, said nanoparticles consisting of a shell portion that is dominated by positively charged chitosan, and a core portion that consists of said positively charged chitosan, one negatively charged substrate, and optionally a zero-charge compound or at least one tumor necrosis factor (TNF) inhibitor.
2. The composition according to claim 1 , wherein said chitosan is N-trimethyl chitosan, EDTA-chitosan, low molecular weight chitosan, pegylated chitosan (PEG-chitosan), mono-N-carboxymethyl chitosan, N-palmitoyl chitosan (NPCS), chitosan derivatives, or combinations thereof.
3. The composition according to claim 1 , wherein said negatively charged substrate is PGA-complexone conjugate, γ-PGA, α-PGA, derivatives of PGA, or salts of PGA.
4. The composition according to claim 1 , wherein said nanoparticles are freeze-dried, thereby said nanoparticles being in a powder form.
5. The composition according to claim 1 , wherein said nanoparticles are mixed with a cryoprotectant and then freeze-dried, thereby said nanoparticles being in a powder form.
6. The composition according to claim 5 , wherein said cryoprotectant is selected from the group consisting of trehalose, hexan-1,2,3,4,5,6-hexyl, mannitol, dimethyl sulfoxide, ethylene glycol, glycol, 2-methyl-2,4-pentanediol, propylene, sucrose, and combinations thereof.
7. The composition according to claim 1 , wherein said nanoparticles are encapsulated in a capsule.
8. The composition according to claim 7 , wherein said capsule is made of methyl cellulose selected from the group consisting of hydroxypropyl methyl cellulose (HPMC), carboxymethyl cellulose, hydroxyethyl methyl cellulose (HEMC), and methyl cellulose derivatives.
9. The composition according to claim 7 , wherein said capsule is treated with an enteric coating.
10. The composition according to claim 7 , wherein said capsule further comprises a pharmaceutically acceptable carrier, diluent, excipient, desiccant, solubilizer, bubbling agent, or emulsifier.
11. The composition according to claim 7 , wherein said capsule further comprises at least one absorption enhancer.
12. The composition according to claim 11 , wherein said absorption enhancer is selected from the group consisting of bile salts, surfactants, medium-chain fatty acids, phosphate esters, chitosan, and chitosan derivatives.
13. The composition according to claim 7 , wherein said capsule is made of gelatin.
14. The composition according to claim 1 , wherein said nanoparticles are treated with an enteric coating or surfactants.
15. The composition according to claim 1 , wherein said nanoparticles are administered via a parenteral route.
16. The composition according to claim 1 , wherein said composition is administered via an oral route.
17. The composition according to claim 1 , wherein the nanoparticles have a mean particle size between about 50 and 500 nanometers.
18. The composition according to claim 1 , wherein the nanoparticles are formed via a simple and mild ionic-gelation process.
19. The composition according to claim 1 , wherein the TNF inhibitor is selected from the group consisting of infliximab (Remicade), adalimumab (Humira), etanercept (Enbrel), and pentoxifylline.
20. The composition according to claim 1 , wherein use of the composition is for treatment of inflammation, plaque psoriasis, rheumatoid arthritis, psoriatic arthritis, adult Crohn's disease, pediatric Crohn's disease, ulcerative colitis, and ankylosing spondylitis.