Table 1 Experimental design and sample collection.

From: Pharmacokinetics, biodistribution and toxicology of novel cell-penetrating peptides

 

Animal

Substance

N/group

Doses

Time points

Pharmacokinetic profiles

Rats

3H-L-S-CPP

3

6.3 × 107 dpm  kg−1 (Do)

(32.0 ug  kg−1)

0.016, 0.033, 0.083, 0.166, 0.5, 1, 2, 5, and 24 h after administration

3H-D-S-CPP

3

16.2 × 107 dpm  kg−1 (Do)

(3.5 ug  kg−1)

3H-IgG

3

12.8 × 106 dpm  kg−1 (Do)

(19.1 ug  kg−1)

 ± L-S-CPP 1.4 mg  kg−1

(250 µM)

0.016, 0.033, 0.083, 0.166, 0.5, 1, 2, 5, 24 and 48 h after administration

3H-IgG + L-S-CPP

3

Biodistribution

Mice

3H-L-S-CPP

2–4 per group

10.4–15.9 ug  kg−1

1 and 5 h after administration

3H-D-S-CPP

3H-IgGantiNUP

6

82.5 ug  kg−1

 ± L/D-S-CPP or Scramble ≈ 3.6 mg  kg−1

1 h after administration

3H-IgGantiNUP + L-S-CPP

11–15 per group

3H-IgGantiNUP + D-S-CPP

3H-IgGantiNUP + Scramble

Toxicology

Mice

L-S-CPP

4–5 per group

3.6 mg  kg−1

120 h

D-S-CPP

PBS

BBB Transport

Mice

3H-L-S-CPP

15

0.2–0.8 µCi  ml−1

Corresponding to 0.2–0.8 µg (≈7.0-27 µg  kg−1)

60 s

  1. BBB blood brain barrier, D0 initial dose (in syringe), S-CPP Shuttle-cell penetrating peptides, h hour, IgG immunoglobulin G, IgGantiNUP anti-Nuclear Pore Complex Proteins Antibody, PBS Phosphate-buffered saline.