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Table 1 Compilation of encapsulation experiments reported in literature

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

Nanoparticle type and size

label

labelling yield/label leaching

Retention/release of daughter nuclides

remarks

reference

Zwitterionic pegylated phosphatydylcholine cholesterol liposomes 200 / 400 / 650 nm

225Ac

225Ac retention > 88% for zwitterionic liposomes after 30d

213Bi retention ≈ 12% for 650 nm size liposomes after 2 days and ≈4% after 30 days

Retention values for 225Ac and 213Bi lower for cationic liposomes

Sofou et al., 2004

liposomes

225Ac

Yield (73±9)% / retention up to (81±7)% achievable

 

Funtionalised liposomes maintain targeting efficacy after 225Ac loading

Chang et al., 2008

Polymersomes 100 / 200 /400 /800 nm filtered fractions

225Ac

(67±0.8)% in 30 min leaching - 200 nm: 2% after 8d 7% after 28d

highest retention after 24h

800 nm: 221Fr (69±1.5)%

213Bi (53±4)%

100 nm: 221Fr (37±4)%

213Bi (22±1)%

Polymerosomes can be internalized by target cells

Wang et al., 2014

[225Ac]InPO4 nanoparticles Inside polymersomes 100 / 200 /400 /800 nm filtered fractions

225Ac

Retention of 225Ac in polymersomes containing [225Ac]InPO4 nanoparticles (92±3)%

retention after 24h

100 nm: 221Fr ≈ 57%

213Bi ≈ 40%

Amorphous [225Ac]InPO4 nanoparticles (≈ 20 nm) were created inside the polymersomes; works well for polymersomes < 400 nm

De Kruijff et al., 2017

Hydroxylapatite XRD: 15 nm

223Ra

99% yield achievable /Release after 24 h in saline 0.7% (surface absorption) 0.8% (in synthesis labelling)

 

Labelling during synthesis and after synthesis (surfacesorption) show both very low leaching – re-absorption on surface?

Kozempel et al., 2015

Hydroxylapatite TEM: nanoplates ≤ 100nm x ≤ 500nm x 0.8…2.4 nm

223Ra

Labelling yield (97±1)% in 20 h /6% - 15% released within 24h depending on loading strategy

 

After surface sorption: 8%

loading during synthesis: 15%

+ annealing 900oC, 3h: 6% release during 24h

Vasiliev et al., 2016

Nanozeolite XRD 43 nm SEM 50-170 nm DLS 40-120 nm

224Ra

225Ra

Labelling yield >99.9% leaching < 0.5% (4d)

Release 1d after incubation

224Ra: 212Pb (2.6±1.5)%

208Tl (7.9±0.9)%

212Pb (6.2±0.5)%

Release 1d after incubation

225Ra: 225Ac (2.3±1.9)%

221Fr(2.7±0.2)%

213Bi(7.4±0.8)%

daughter release data reported in human blood serum (data available also for other media)

Piotrowska et al., 2013

Functionalised Nanozeolite-silane-PEG-SP(5-11)TEM: 60 nm

223Ra

labelling yield > 99.9%

leaching < 0.5%

released daughter nuclides

211Pb and 211Bi increasing from ≈2% (1d) to ≈5% (6d), each

High receptor affinity preserved; intravenous application not possible

Piotrowska et al., 2017

Fe3O4 SPIONS

TEM: 4…26 nm

DLS: 284 nm

223Ra

Yield in 0.9% NaCl ≤ 50% , in PBS 85-99% within 1h

Leaching in bovine serum and plasma 1.5% (11.4d) to 2% (22.8d)

 

Labelling by surface complexation suggested

Mokhodoeva et al., 2016

{La 0.5 Gd 0.5}PO4 core (2.9±0.7) nm

+4 shells GdPO4

+ external Au shell

27 nm (with Au shell)

(22.4±7.7)nm

225Ac

76% after 4 days of core synthesis

225Ac retention > 99.9% after 3 weeks

221Fr retention ≈90% after 3 weeks

Ac will co-crystallize into a lanthanide phosphate crystal

Gd allows separation of 225Ac-labelled NPs from co-produced Au-NPs

McLaughlin et al., 2013

  1. The type and size of nanocarriers is presented, the loaded radionuclide and the achievable loading yield and the retention of the mother nuclide. As far as reported the retention of the daughter nuclides are presented