Nanoparticle delivery system for targeted anti-obesity treatment
A magnetic nanoparticles including a TRPV1 agonist, as well as methods of preparation and use, are described herein. A magnetically responsive pharmaceutical can include a core region having a magnetic nanoparticle (MNPs) and a TRPV1 protein agonist. Further, an exterior coating comprising a polymer can be formed around the core region. The magnetically responsive pharmaceutical can be administered to a recipient and directed to a target region using an external magnetic field.
1. A magnetically responsive pharmaceutical comprising:
magnetic nanoparticles (MNPs);
a first TRPV1 protein agonist interspersed in the MNPs;
a second TRPV1 protein agonist forming an intermediate layer over the MNPs; and
an exterior coating formed over the MNPs, the first TRPV1 protein agonist, and the intermediate layer, the exterior coating comprising a polymer.
2. The pharmaceutical of claim 1 , wherein the first TRPV1 agonist is selected from the group consisting of dihydrocapsiate, capsaicin, civamide, endovanilloids, resiniferatoxin, N-Vanillylnonanamide, capsiate, Capsaicin β-D-Glucopyranoside, and combinations thereof.
3. The pharmaceutical of claim 1 , wherein the polymer is selected from the group consisting of poly(lactic-co-glycolic acid) (PLGA), polylactic acid (PLA), polyglycolic acid (PGA), poly-D-lactic acid (PDLA), PLGA-dimethacrylate, fluorescent PLGA polymers, Poly(ethyl acrylate-co-methyl methacrylate-co-trimethylammonioethyl methacrylate chloride) 1:2:0.2, Poly(ethyl acrylate-co-methyl methacrylate-co-trimethylammonioethyl methacrylate chloride) 1:2:0.1, Ethyl cellulose, cellulose derivatives, and combinations thereof.
4. The pharmaceutical of claim 1 , wherein the MNPs comprise metal ions, and wherein the molar ratio of polymer to metal ions is between 1:40 and 1:300.
5. The pharmaceutical of claim 1 , wherein the MNPs comprise a material selected from the group consisting of iron, cobalt, nickel and combinations thereof.
6. The pharmaceutical of claim 1 , wherein the MNPs comprise iron oxide.
7. The pharmaceutical of claim 1 , further comprising:
the second TRPV1 agonist interspersed in the exterior coating.
8. The pharmaceutical of claim 1 , wherein the MNPs comprise Fe 3+ ions and Fe 2+ ions in a molar ratio between about 3:1 and about 1:1 of Fe 3+ ions to Fe 2+ ions.
9. The pharmaceutical of claim 1 , wherein each of the MNPs have a diameter between about 5 nm and about 30 nm.
10. An oral pharmaceutical composition in solid unit dosage form comprising:
from about 1% to about 100% of a magnetically responsive pharmaceutical, the magnetically responsive pharmaceutical comprising:
magnetic nanoparticles (MNPs);
a first TRPV1 protein agonist interspersed in the MNPs;
a second TRPV1 protein agonist forming an intermediate layer over the MNPs; and
a coating surrounding the MNPs, the first TRPV1 protein agonist, and the intermediate layer, the coating comprising a polymer; and
from about 0% to about 99% pharmaceutically-acceptable excipients.
11. The oral pharmaceutical composition of claim 10 , wherein the first TRPV1 agonist is selected from the group consisting of dihydrocapsiate, capsaicin, civamide, endovanilloids, resiniferatoxin, N-Vanillylnonanamide, capsiate, Capsaicin β-D-Glucopyranoside, and combinations thereof.
12. The oral pharmaceutical composition of claim 10 , wherein the polymer is selected from the group consisting of poly(lactic-co-glycolic acid) (PLGA), Polylactic acid (PLA), Polyglycolic acid (PGA), poly-D-lactic acid (PDLA), PLGA-dimethacrylate, fluorescent PLGA polymers, Poly(ethyl acrylate-co-methyl methacrylate-co-trimethylammonioethyl methacrylate chloride) 1:2:0.2, Poly(ethyl acrylate-co-methyl methacrylate-co-trimethylammonioethyl methacrylate chloride) 1:2:0.1, Ethyl cellulose, cellulose derivatives, and combinations thereof.
13. The oral pharmaceutical composition of claim 10 , wherein the MNPs comprise a material selected from the group consisting of iron, cobalt, nickel and combinations thereof.
14. The oral pharmaceutical composition of claim 10 , further comprising:
the second TRPV1 protein agonist interspersed in the coating.
15. The oral pharmaceutical composition of claim 10 , wherein the MNPs comprise Fe 3+ ions and Fe 2+ ions in a molar ratio between about 3:1 and about 1:1 of Fe 3+ ions to Fe 2+ ions.
16. The oral pharmaceutical composition of claim 10 , wherein each of the MNPs have a diameter between about 5 nm and about 30 nm.
17. A magnetically responsive pharmaceutical comprising:
magnetic nanoparticles (MNPs) comprising metal ions, the metal ions comprising Fe 3+ ions and Fe 2+ ions;
capsaicin interspersed in the MNPs;
a TRPV1 protein agonist forming an intermediate layer over the MNPs; and
an exterior coating formed over the MNPs, the capsaicin, and the intermediate layer, the exterior coating comprising a poly(lactic-co-glycolic acid) (PLGA) polymer.
18. The pharmaceutical of claim 17 , wherein the MNPs comprise MNP clusters, the MNP clusters having a diameter of about 200 nm or less.
19. The pharmaceutical of claim 17 , wherein the molar ratio of PLGA polymer to metal ions is between 1:40 and 1:300.