Table 5.
Apparent (Papp) and effective (Peff) permeability coefficients of gemcitabine and its amino acid ester prodrugs in the apical-to-basolateral direction across Caco-2 monolayer and in situ perfusion study in mouse (mean ± SD, n = 3).
| Prodrug/drug | Papp, Caco-2 (×10−6 cm/s) | Peff, mouse perfusion (×10−5 cm/s) |
|---|---|---|
| Gemcitabine | 1.0 ± 0.2 | 2.0 ± 0.2 |
| 5′-L-Phenylalanyl-gemcitabine | 3.8 ± 0.9* | 33.8 ± 3.4* |
| 5′-D-Phenylalanyl-gemcitabine | 4.5 ± 0.9* | 21.6 ± 4.1* |
| 5′-L-Valyl-gemcitabine | 4.0 ± 0.1* | 35.8 ± 9.2* |
| 5′-D-Valyl-gemcitabine | 3.9 ± 0.1* | 19.1 ± 6.1* |
p < 0.05, Compared with gemcitabine.