Table 2.
Pharmacokinetic Coefficients of Unconjugated and Conjugated PNA in Mouse Organs/Tissues after IP Administration: Half-Time of Biphasic Clearance Pattern
| |
Half-time of rapid clearance T1 (hours) |
Half-time of slow clearance T2 (hours) |
||||
|---|---|---|---|---|---|---|
| Organ/Tissues | PNATAR | PNATAR-Tat | PNATAR-Penetratin | PNATAR | PNATAR-Tat | PNATAR-Penetratin |
| Kidney | 1.33 (±0.6) | 10.40 (±6.4) | 6.40 (±2.9) | 25.67 (±2.4) | 26.66 (±7.0) | 45 (±5.6) |
| Intestine | 0.97 (±0.1) | 0.95 (±0.2) | 0.67 (±0.2) | 93.68 (±34.2) | 77.02 (±156.6) | 44 (±31) |
| Liver | 1.06 (±0.3) | 0.97 (±0.4) | 0.98 (±0.2) | 56.82 (±22.8) | 57.29 (±38.4) | 39 (±12) |
| Blood | 0.78 (±0.3) | 0.58 (±0.3) | 0.64 (±0.1) | 24.41 (±7.4) | 35.73 (±5.7) | 56 (±19) |
| Spleen | 0.63 (±0.1) | 0.84 (±0.3) | 1.30 (±0.4) | 119.52 (±42.2) | 42.53 (±12.5) | 23 (±5.0) |
| Heart | 1.33 (±0.3) | 1.29 (±0.3) | 2.00 (±0.7) | 45.91 (±19.8) | 24.49 (±10.4) | 43 (±11) |
| Brain | 1.16 (±0.4) | 0.94 (±0.3) | 4.80 (±9.1) | 10.46 (±4.8) | 16.43 (±4.2) | 22 (±41) |
| Lungs | 0.70 (±0.1) | 0.89 (±0.1) | 3.00 (±1.3) | 59.25 (±15.7) | 31.8 (±13.7) | 110 (±84) |
| Skeletal muscle | 1.37 (±0.5) | 1.24 (±0.5) | 1.90 (±0.3) | 30.01 (±5.9) | 44.15 (±31.2) | 45 (±29) |
The half-time of the biphasic clearance pattern is comprised of a fast-release (T1) and a slow-release component (T2). For each time point, five mice were injected. The values in italics placed in parentheses are the results of uncertainties in the fitting procedure by a two-component function, as mentioned in the Results. The goodness of fit (R2) values ranged from 0.86 to 1.