Table 1 Summary of studies conducted with radium radioisotopes bound in nanocarriers
From: The Curies’ element: state of the art and perspectives on the use of radium in nuclear medicine
Nanocarrier | Incorporated radionuclide | Surface functionalization | Targeting vector | Radiochemical incorporation[a] | Stability[b] | In vitro and in vivo results | References |
|---|---|---|---|---|---|---|---|
Barium sulphate (BaSO4) functionalized nanoparticles | 133Ba [c] | Alendronate | – | 20% (single-step precipitation) | > 95% at 7 d in water | Not explored | Reissig et al. (2019) |
224Ra | |||||||
131Ba [d] | Alendronate | – | 40% (two-step precipitation) | 93% at 7 d in water | Not explored | Reissig et al. (2020b) | |
133Ba | 41% (two-step precipitation) | ||||||
224Ra | 31% (two-step precipitation) | 96% (82% if measuring 212Pb) at 7 d in water | |||||
Barium hexaferrite (BaFe12O19) functionalized nanoparticles | 223Ra | 3-phosphonopropionic acid (CEPA) | Trastuzumab | 70% (autoclave method) | Almost quantitative in 0.01 M phosphate buffered saline (PBS), 0.9% NaCl, and human blood serum (20% release of 211Pb) | High affinity to human epidermal growth factor receptor 2 (HER2) on ovarian cancer cells High cytotoxicity | Gaweda (2019) |
Titanium dioxide (TiO2) nanoparticles | 223Ra | – | – | 98.7% (surface sorption) 99.1% (single-step precipitation) | > 99% at 59 h and 55 d in saline; > 97.5% at 59 h and > 97% at 55 d in bovine blood serum | Not explored | Suchánková et al. (2020a) |
Hydroxyapatite (Ca10(PO4)6(OH)2) nanoparticles | 223Ra | – | – | 94.2% (surface sorption) 97.0% (single-step precipitation) | ~ 40% at 59 h and ~ 80% at 55 d in saline; ~ 78% at 59 h and > 80% at 55 d in bovine blood serum | Not explored | Suchánková et al. (2020a) |
Lanthanum phosphate (LaPO4) nanoparticles | 223Ra | – | – | 91% (precipitation) | 87.3% at 35 d in a dialysis membrane against water | Not explored | Rojas et al. (2015) |
Two shells of LaPO4 | 80% (precipitation and surface deposition) | > 99.9% at 27 d in a dialysis membrane against water | |||||
α-zirconium phosphate nanoparticles | 223Ra | – | – | 98.5% (surface sorption) | < 1.5% in saline; 14% in bovine plasma at 48 h | Not explored | Sakmár et al. (2023) |
NaA nanozeolites | 224Ra | – | – | > 99.9% (ion exchange) | > 99.5% at 24 h in saline, PBS, EDTA, L-cysteine, and human blood serum | Not explored | Piotrowska et al. (2013) |
Functionalized NaA nanozeolites | 223Ra | Silane-poly(ethyleneglycol) (PEG) | Substance P (SP) (5–11) | > 99.9% (ion exchange) | > 99.5% at 6 d in human serum at 37 °C (~ 5% release of 211Pb and 211Bi) | High affinity (IC50 = 14.3 μg·mL−1) to neurokinin 1 (NK-1) receptor on human glioma T98G cells [e] High cytotoxicity | Piotrowska et al. (2017) |
Functionalized NaA nanozeolites | 223Ra | Silane-PEG | D2B (~ 50 antibodies/ nanoparticle) | 99.8%, specific activity 0.65 MBq/mg (ion exchange) | > 95% at 12 d in human serum at 37 °C | Specific binding to PSMA + human lymph node prostate carcinoma LNCaP C4-2 cells [f] High cytotoxicity Significant accumulation in the spleen, liver, bone, lungs, but not in the tumor, at 7 d in LNCaP C4-2 tumor-bearing BALB/c nude male mice | |
Sterically stabilized PEG-liposomes [g] | 223Ra | – | Dual: human F(ab’)2-folate | 78% (ionophore-mediated loading) | 93% at 100 h in human serum at 37 °C | High affinity (Ka ~ 109–1012) to folate receptor (FR) on human ovarian carcinoma OvCar-3 (ATTC HTB-161) cells | Henriksen et al. (2004) |
Pegylated liposomal doxorubicin (PLD) | 223Ra | – | – | 51–67% (ionophore-mediated loading) | No release at 7 d in fetal calf serum at 37 °C | Significant accumulation in the spleen, skull, and femur at 14 d in healthy white BALB/c mice | Jonasdottir et al. (2006) |