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. Author manuscript; available in PMC: 2020 Feb 22.
Published in final edited form as: Mol Pharm. 2019 Jun 27;16(8):3414–3429. doi: 10.1021/acs.molpharmaceut.9b00208

Table 4.

Pharmacokinetic Parameters of Plain Fasudil and Various Formulations after IT and IV Administration into PAH and Sham Ratsa

Cmax (ng/mL) t1/2 (h) AUC0-inf (ng·h/mL)
drug/formulations route Sham PAH Sham PAH Sham PAH
plain fasudil IV 14 150 ± 1050 0.2 ± 0.004 5967.1 ± 25.9
fasudil in no-CAR-liposome IV 11 700 ± 778.9 10 365 ± 1135 0.3 ± 0.05 0.4 ± 0.1 9737.9 ± 544.3 9537.3 ± 1204
CAR pretreatment then fasudil no-CAR-liposomes IV 13 200 ± 1186 12 200 ± 1268**** 0.5 ± 0.06 0.35 ± 0.1 11 890.8 ± 975.3*** 6118.8 ± 520*
fasudil in CAR-liposome IV 12 466.7 ± 1302**** 4080 ± 630* 0.7 ± 0.3 1.1 ± 0.3 5213 ± 152.8 1274 ± 218
plain fasudil IT 3035 ± 635 0.7 ± 0.08 5967.1 ± 25.9
fasudil in no-CAR-liposomes IT 1433.3 ± 87 1183.3 ± 83 3.3 ± 1.3* 4.7 ± 0.9* 9737.9 ± 544.3 10 191.8 ± 2016
CAR pretreatment then fasudil in no-CAR-liposome IT 1390 ± 150 1085 ± 45 3.9 ± 0.1 6.9 ± 1.8 11 890.8 ± 975.3* 12 677.1 ± 2910****
fasudil in CAR-liposome IT 614 ± 102 379.7 ± 11.9 12.9 ± 4.6*** 16.1 ± 4.1*** 5832 ± 1365 4210.6 ± 985
a

Data represent mean ± SD, n = 3;

*

p < 0.05,

**

p < 0.005,

***

p < 0.001,

****

p < 0.001.