Therapeutic Targeting of Lipid Nanoparticles
US-2024131181-A1 · Apr 25, 2024 · US
US9327038B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9327038-B2 |
| Application number | US-201213660198-A |
| Country | US |
| Kind code | B2 |
| Filing date | Oct 25, 2012 |
| Priority date | Oct 25, 2011 |
| Publication date | May 3, 2016 |
| Grant date | May 3, 2016 |
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The present invention provides radiotherapeutic agents and compositions and methods for making and using the same. In some embodiments, the radiotherapeutic agent is a nanoparticle comprising a radionuclide and a carrier moiety. In some embodiments, the radionuclide is produced by activating a stable activatable particle via neutron activation.
Opening claim text (preview).
That which is claimed: 1. A stable activatable particle comprising an activatable radionuclide precursor and a carrier moiety, wherein said activatable radionuclide precursor comprises a radionuclide selected from the group consisting of 23 Na, 31 P, 56 Fe, 74 Se, 85 Rb, 88 Sr, 89 Y, 127 I, 139 La, 141 Pr, 149 Sm, 150 Sm, 152 Sm, 164 Dy, 165 Ho, 168 Er, 175 Lu, 185 Re, 187 Re, 197 Au, 203 Tl, and any combination thereof, conjugated to a hydrophobic and/or lipophilic moiety selected from the group consisting of acetylacetone, ethyl acetoacetate, 3-methyl-2,4-pentanedione, 3-ethyl-2,4-pentanedione, 2,4-hexanedione, and diethyl malonate, and wherein said carrier moiety is a silica particle having a diameter of about 1 nm to about 500 nm. 2. The stable activatable particle of claim 1 , wherein said activatable radionuclide precursor comprises a radionuclide selected from the group consisting of 31 P, 88 Sr, 89 Y, 127 I, 149 Sm, 150 Sm, 152 Sm, 164 Dy, 165 Ho, 175 Lu, and any combination thereof. 3. The stable activatable particle of claim 1 , wherein said activatable radionuclide precursor comprises 165 Ho. 4. The stable activatable particle of claim 1 , wherein said activatable radionuclide precursor is holmium-165 acetylacetonate ( 165 Ho(AcAc) 3 ). 5. The stable activatable particle of claim 1 , wherein said carrier moiety is a mesoporous silica particle. 6. The stable activatable particle of claim 1 , wherein said carrier moiety comprises a targeting agent. 7. The stable activatable particle of claim 6 , wherein said targeting agent is a tumor-targeting agent. 8. A radiotherapeutic agent produced by activating the stable activatable particle of claim 1 . 9. The radiotherapeutic agent of claim 8 , wherein activating the stable activatable particle comprises neutron activation. 10. A pharmaceutical composition comprising the stable activatable particle of claim 1 . 11. A pharmaceutical composition comprising the radiotherapeutic agent of claim 8 .
microparticles or nanoparticles, e.g. polymeric nanoparticles · CPC title
Micelles, e.g. phospholipidic or polymeric micelles · CPC title
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