Table 2. Pharmacokinetic (PK) Parameters of 111In-Labeled HAuNS Conjugates in Micea.
| PEG-HAuNS | ||||||
|---|---|---|---|---|---|---|
| PK parameter | mouse 1 | mouse 2 | mouse 3 | mouse 4 | mouse 5 | mean ± SD |
| AUC0-∞ (%ID·h/g) | 105.43 | 79.90 | 84.32 | 96.74 | 65.32 | 86.34 ± 15.49 |
| T1/2 (h) | 9.29 | 8.58 | 9.52 | 7.08 | 11.99 | 9.29 ± 1.78 |
| CL (g/h) | 0.9485 | 1.2516 | 1.186 | 1.0337 | 1.531 | 1.1902 ± 0.23 |
| Vss (g) | 10.90 | 12.48 | 13.91 | 8.51 | 22.06 | 13.57 ± 5.15 |
| MRT (h) | 11.49 | 9.97 | 11.73 | 8.24 | 14.41 | 11.17 ± 2.29 |
| Aptmer-HAuNS | ||||||
|---|---|---|---|---|---|---|
| PK parameter | mouse 1 | mouse 2 | mouse 3 | mouse 4 | mouse 5 | mean ± SD |
| AUC0-∞ (%ID·h/g) | 45.35 | 67.54 | 90.16 | 64.04 | 57.17 | 64.85 ± 16.49 |
| T1/2 (h) | 5.62 | 4.95 | 5.80 | 6.84 | 5.17 | 5.68 ± 0.73b |
| CL (g/h) | 2.2052 | 1.4805 | 1.1092 | 1.5616 | 1.7493 | 1.6212 ± 0.40 |
| Vss (g) | 13.62 | 8.15 | 7.43 | 11.39 | 10.13 | 10.14 ± 2.50 |
| MRT (h) | 6.17 | 5.50 | 6.70 | 7.29 | 5.79 | 6.29 ± 0.72b |
| C225-HAuNS | |||||
|---|---|---|---|---|---|
| PK parameter | mouse 1 | mouse 2 | mouse 3 | mouse 4 | mean ± SD |
| AUC0-∞ (%ID·h/g) | 108.63 | 120.45 | 139.31 | 108.29 | 119.17 ± 14.57c,d |
| T1/2 (h) | 9.10 | 9.60 | 11.48 | 8.73 | 9.73 ± 1.22d |
| CL (g/h) | 0.9205 | 0.8303 | 0.7178 | 0.9234 | 0.848 ± 0.0970d |
| Vss (g) | 8.79 | 8.37 | 8.97 | 8.30 | 8.61 ± 0.32 |
| MRT (h) | 9.54 | 10.08 | 12.49 | 8.99 | 10.28 ± 1.54d |
a
AUC: area under the curve; T1/2: terminal elimination half-life; CL: systemic clearance; Vss: volume of distribution at steady state; MRT: mean residence time.
b
Significantly different between PEG-HAuNS and apt-HAuNS groups.
c
Significantly different between PEG-HAuNS and C225-HAuNS groups.
d
Significantly different between apt-HAuNS and C225-HAuNS groups.