Hydroxyapatite particles as carriers for 223Ra

Vasiliev, A. N.; Северин, А. В.; Lapshina, E.V.; Chernykh, E. V.; Ermolaev, S. V.; Kalmykov, Stepan N.

doi:10.1007/s10967-016-5007-y

Cited by 33 publications

(25 citation statements)

References 12 publications

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“…Additionally the loading with the α-particle emitter must be feasible with high yield. Kozempel et al ( 2015 ) and Vasiliev et al ( 2016 ) investigated the possibility to load 225 Ac onto hydroxyapatite nanoparticles by adsorption or to incorporate 225 Ac during nanoparticle synthesis. Hydroxyapatite was selected due to its known biocompatibility.…”

Section: Reviewmentioning

confidence: 99%

A random walk approach to estimate the confinement of α-particle emitters in nanoparticles for targeted radionuclide therapy

Holzwarth

Jiménez

Calzolai

2018

EJNMMI radiopharm. chem.

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BackgroundTargeted radionuclide therapy is a highly efficient but still underused treatment modality for various types of cancers that uses so far mainly readily available β-emitting radionuclides. By using α-particle emitters several shortcomings due to hypoxia, cell proliferation and in the selected treatment of small volumes such as micrometastasis could be overcome. To enable efficient targeting longer-lived α-particle emitters are required. These are the starting point of decay chains emitting several α-particles delivering extremely high radiation doses into small treatment volumes. However, as a consequence of the α-decay the daughter nuclides receive high recoil energies that cannot be managed by chemical radiolabelling techniques. By safe encapsulation of all α-emitters in the decay chain in properly sized nanocarriers their release may be avoided.ResultsThe encapsulation of small core nanoparticles loaded with the radionuclide in a shell structure that safely confines the recoiling daughter nuclides promises good tumour targeting, penetration and uptake, provided these nanostructures can be kept small enough. A model for spherical nanoparticles is proposed that allows an estimate of the fraction of recoiling α-particle emitters that may escape from the nanoparticles as a function of their size. The model treats the recoil ranges of the daughter nuclides as approximately equidistant steps with arbitrary orientation in a three-dimensional random walk model.ConclusionsThe presented model allows an estimate of the fraction of α-particles that are emitted from outside the nanoparticle when its size is reduced below the radius that guarantees complete confinement of all radioactive daughter nuclides. Smaller nanoparticle size with reduced retention of daughter radionuclides might be tolerated when the effects can be compensated by fast internalisation of the nanoparticles by the target cells.

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Section: Reviewmentioning

confidence: 99%

A random walk approach to estimate the confinement of α-particle emitters in nanoparticles for targeted radionuclide therapy

Holzwarth

Jiménez

Calzolai

2018

EJNMMI radiopharm. chem.

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“…In a series of publications, Kozempel et al [ 19 , 20 , 21 , 22 ] tested hydroxyapatite (HAP) nanoparticles as a transporter for 223 Ra radionuclide. They studied two methods for binding of 223 Ra to HAP nanoparticles.…”

Section: Introductionmentioning

confidence: 99%

Trastuzumab Modified Barium Ferrite Magnetic Nanoparticles Labeled with Radium-223: A New Potential Radiobioconjugate for Alpha Radioimmunotherapy

et al. 2020

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Barium ferrite nanoparticles (BaFeNPs) were investigated as vehicles for 223Ra radionuclide in targeted α-therapy. BaFe nanoparticles were labeled using a hydrothermal Ba2+ cations replacement by 223Ra with yield reaching 61.3 ± 1.8%. Radiolabeled nanoparticles were functionalized with 3-phosphonopropionic acid (CEPA) linker followed by covalent conjugation to trastuzumab (Herceptin®). Thermogravimetric analysis and radiometric method with the use of [131I]-labeled trastuzumab revealed that on average 19–21 molecules of trastuzumab are attached to the surface of one BaFe–CEPA nanoparticle. The hydrodynamic diameter of BaFe–CEPA–trastuzumab conjugate is 99.9 ± 3.0 nm in water and increases to 218.3 ± 3.7 nm in PBS buffer, and the zeta potential varies from +27.2 ± 0.7 mV in water to −8.8 ± 0.7 in PBS buffer. The [223Ra]BaFe–CEPA–trastuzumab radiobioconjugate almost quantitatively retained 223Ra (>98%) and about 96% of 211Bi and 94% of 211Pb over 30 days. The obtained radiobioconjugate exhibited high affinity, cell internalization and cytotoxicity towards the human ovarian adenocarcinoma SKOV-3 cells overexpressing HER2 receptor. Confocal studies indicated that [223Ra]BaFe–CEPA–trastuzumab was located in peri-nuclear space. High cytotoxicity of the [223Ra]BaFe–CEPA–trastuzumab bioconjugate was confirmed by radiotoxicity studies on SKOV-3 cell monolayers and 3D-spheroids. In addition, the magnetic properties of the radiobioconjugate should allow for its use in guide drug delivery driven by magnetic field gradient.

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“…As an alternative strategy to organic ligands, we and several other groups made substantial efforts to incorporate radium into nanocarrier-based systems, including polyoxopalladates, [17] hydroxyapatite, [18] iron oxide, [19] barium ferrite, or nanozeolites. [20] Recently, we reported on the development of a straightforward carrier system for radium based on barium sulfate nanoparticles (NPs).…”

Section: Introductionmentioning

confidence: 99%

Sub‐10 nm Radiolabeled Barium Sulfate Nanoparticles as Carriers for Theranostic Applications and Targeted Alpha Therapy

et al. 2020

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The treatment of cancer patients with α‐particle‐emitting therapeutics continues to gain in importance and relevance. The range of radiopharmaceutically relevant α‐emitters is limited to a few radionuclides, as stable chelators or carrier systems for safe transport of the radioactive cargo are often lacking. Encapsulation of α‐emitters into solid inorganic systems can help to diversify the portfolio of candidate radionuclides, provided, that these nanomaterials effectively retain both the parent and the recoil daughters. We therefore focus on designing stable and defined nanocarrier‐based systems for various clinically relevant radionuclides, including the promising α‐emitting radionuclide 224Ra. Hence, sub‐10 nm barium sulfate nanocontainers were prepared and different radiometals like 89Zr, 111In, 131Ba, 177Lu or 224Ra were incorporated. Our system shows stabilities of >90 % regarding the radiometal release from the BaSO4 matrix. Furthermore, we confirm the presence of surface‐exposed amine functionalities as well as the formation of a biomolecular corona.

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Hydroxyapatite particles as carriers for 223Ra

Cited by 33 publications

References 12 publications

A random walk approach to estimate the confinement of α-particle emitters in nanoparticles for targeted radionuclide therapy

A random walk approach to estimate the confinement of α-particle emitters in nanoparticles for targeted radionuclide therapy

Trastuzumab Modified Barium Ferrite Magnetic Nanoparticles Labeled with Radium-223: A New Potential Radiobioconjugate for Alpha Radioimmunotherapy

Sub‐10 nm Radiolabeled Barium Sulfate Nanoparticles as Carriers for Theranostic Applications and Targeted Alpha Therapy

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