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. Author manuscript; available in PMC: 2014 Nov 25.
Published in final edited form as: Eur J Pharm Biopharm. 2013 Dec 19;86(3):514–523. doi: 10.1016/j.ejpb.2013.12.009

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.