Table 2.
Pharmacokinetic analysis of 3H-2-PAM after IV injection of 3H-2-PAM@scFv-Lipo in mice.
| Organs | Vd-V0 (μL/g) | PS (μL/min/g) | %ID/g | |||
|---|---|---|---|---|---|---|
| 3H-2PAM@46.1-Lipo | 3H-2PAM@Ctrl-Lipo | 3H-2PAM@46.1-Lipo | 3H-2PAM@Ctrl-Lipo | 3H-2PAM@46.1-Lipo | 3H-2PAM@Ctrl-Lipo | |
| brain | 5.39 ± 0.35* | 0.82 ± 1.43 | 0.016 ± 0.0036* | 0.0024 ± 0.0041 | 0.24 ± 0.016* | 0.023 ± 0.040 |
| heart | 32.36 ± 2.58 | 41.86 ± 9.91 | 0.097 ± 0.023 | 0.10 ± 0.045 | 1.43 ± 0.11 | 1.17 ± 0.28 |
| lung | 21.32 ± 1.93 | 31.46 ± 10.60 | 0.063 ± 0.010 | 0.076 ± 0.036 | 0.94 ± 0.086 | 0.88 ± 0.30 |
| liver | 67.60 ± 10.03* | 162.80 ± 11.56 | 0.20 ± 0.039 | 0.39± 0.13 | 2.99 ± 0.44* | 4.55 ± 0.32 |
| spleen | 38.93 ± 4.85* | 108.52 ± 14.24 | 0.12 ± 0.026* | 0.25± 0.040 | 1.72 ± 0.21* | 3.03 ± 0.40 |
| kidney | 27.72 ± 3.40* | 53.63 ± 8.04 | 0.081 ± 0.0093 | 0.12 ± 0.026 | 1.23 ± 0.15 | 1.50 ± 0.22 |
3H-2-PAM@scFv-Lipo was intravenously administered to C57BL6 mice at a dose corresponding to 5 mg/kg of liposomally-conjugated scFvs, and 3.4–4.3 × 107 DPM/kg of 3H-2-PAM (n=3). An aliquot of orbital vein blood sample was collected at 0.5, 2, 15, 30, 60, 120 and 240 min after injection. Plasma amounts of 3H-2-PAM were determined by scintillation counting and used to determine the AUC. After 4 hours of circulation, mice were whole body perfused, organs were isolated, and scintillation counting was used to measure 2-PAM uptake in the whole organ homogenates. Organ uptake parameters were calculated as described in the Materials and Methods. Reported are means ± S.D., n=3 independent mice.
p<0.05 by two-tailed unpaired Student’s t test.