Table 5.
The in vivo study results of the third-generation boron agents.
| Agent | Type | Injection | Max Boron in Tumor (ppm) | Tumor/Blood Ratio | Efficacy | Safety | Drug Loading Property | Imaging Property | Citation |
|---|---|---|---|---|---|---|---|---|---|
| BPN (boronated porphyrin nanocomplex) |
Nanoparticle (micelle) | Intravenous injection | 125.17 ± 13.54 (five-time injection) |
33.85 ± 5.73 (five injections) |
Tumor growth was suppressed and survival was prolonged | No obvious weight changes or abnormity of major organs | N | Y (PET-CT) |
[32] |
| BCOPs (carborane-loaded covalent organic polymers) |
Nanoparticle (micelle) | Intravenous injection | 84.93 ± 2.68 (three injections) |
7.46 ± 0.66 (three injections) |
Tumor growth was suppressed and survival was prolonged | No significant pathological damage or changes in major organs | N | Y (PET-CT) |
[33] |
| B-COFs (carborane-based covalent organic frameworks) |
Nanoparticle (COF) | Intratumoral injection | 19.8 (24 h) |
N.A. | Tumor growth was delayed over 40 days and survival was prolonged | No obvious loss of body weight and the results of serum biochemical test, routine blood analysis, and Hematoxylin-Eosin staining of major organs showed negligible systemic toxicity | Y | Y (PET-CT) |
[34] |
| PTL@BNNPs (phase-transitioned lysozyme decorated boron nitride nanoparticles) | Nanoparticle (nanosheet) | Intravenous injection | Above 120 (24 h) |
2.71 ± 0.96 (24 h) |
Tumor growth was suppressed and survival was prolonged | No obvious histological abnormality | N | Y (PET-CT) |
[35] |
| BNNSs (boron nitride nanosheets) |
Nanoparticle (boron nanosheet) | Intravenous injection | Above 20 (24 h) |
2.4 (24 h) |
Tumor growth was suppressed and survival was prolonged | No abnormalities were observed in major organs | Y | Y (PET-CT) |
[36] |
| Boronsome (carborane-derived liposome) | Nanoparticle (liposome) | Intravenous injection | 93 (12 h) |
4.2 (12 h) |
The tumor volume shrank to 1/5 after about 3 weeks (PARPi-boronsome) and survival was prolonged |
No systemic toxicity or side effects |
Y | Y (PET-CT) |
[37] |
| FBY (boron-derived tyrosine) | Small molecular | Intravenous injection | 19.59 ± 0.47 (1 h) |
3.13 ± 0.50 (1 h) |
Tumor growth was suppressed and survival was prolonged | No obvious weight changes or abnormity of major organs | N | Y (PET-CT) |
[38] |
|
157Gd-TCPP MOFs (MOF fabricated by Gd3+ and porphyrin derivative) |
Nanoparticle (MOF) |
Intratumoral injection | 95.1 ± 43.7 (8 d) |
Above 800 (8 d) |
Tumor growth was suppressed and survival was prolonged | No obvious weight changes or abnormity of major organs | N | Y (PET-CT) |
[40] |
| Zr-TCPP MOFs nano-co-crystals loaded with boric acids | Nanoparticle (MNC and MOFs nano-co-crystal) | Intravenous injection | 67.50 ± 4.20 (2 h) |
3.80 ± 0.35 (2 h) |
Tumor growth was suppressed and survival was prolonged | No obvious weight changes | N | Y (PET-CT) |
[41] |
| BCD-Exos (exosome-coated 10B carbon dots) | Nanoparticle (carbon dots) | Intravenous injection | 107.07 ± 1.58 (4 h) |
5.28 ± 0.29 (4 h) |
Tumor growth was suppressed and survival was prolonged | No obvious abnormity of major organs | N | Y (Fluorescence imaging) |
[42] |
| PEG-b-P(Glu-SS-BSH) (PEGylated BSH-polymer conjugate) |
Nanoparticle (micelle) | Intravenous injection | 128 (24 h) |
~10 (24 h) |
Tumor growth was suppressed | No visible damage of surrounding skin/tissue or body weight loss | N | N | [43] |
| PD-CD133/BSH (folate receptor-mediated boron-10 containing carbon nanoparticles) |
Antibody (boron conjugated antibody) |
Intratumoral injection | 25.7 ± 5.8 (12 h, with 100 mg/kg BSH) |
~2.7 (12 h, with 100 mg/kg BSH) |
The survival of mouse was prolonged | N.A. | N | N | [44] |
Abbreviations: N: no; Y: yes; N.A.: not available; PET-CT: positron emission tomography–computed tomography; d: day; and h: hour.