Table 1.
Api | NLCs | PEG-NLCs | Apt-NLCs | ||
---|---|---|---|---|---|
In vivo plasma pharmacokinetic data | Cmax (ng/ml) | 15.5 ± 0.16 | 17.2 ± 1.13 | 18.1 ± 0.55 | 19.2 ± 0.51 |
AUC last (ng/h/ml) | 125.8 ± 52 | 496.4 ± 62.9 | 826.4 ± 53# | 986.2 ± 47# | |
AUMC | 1608 ± 1419 | 15,290 ± 3089 | 30,457 ± 2350 | 37,988 ± 1994 | |
MRT (h) | 12.81 ± 1.58 | 30.83 ± 1.09 | 36.94 ± 0.41$ | 38.91 ± 0.21$ | |
AUC 0-∞ (ng h/ml) | 130.61 ± 53.4 | 539.64 ± 79.34 | 1072.47 ± 171.21* | 1446.21 ± 182.65* | |
t1/2 (h) | 5.25 ± 0.25 | 13.51 ± 0.2 | 39.02 ± 0.2 | 43.02 ± 0.25 | |
Clearance (L/h/Kg) | 15.9 ± 0.55 | 4.03 ± 0.63 | 2.42 ± 0.66 | 2.03 ± 0.52 | |
In vivo liver pharmacokinetic data | Cmax (ng/ml) | 160 ± 7.87 | 165.7 ± 7.37 | 178.9 ± 8.14 | 223.4 ± 6.64 |
Tmax (h) | 1 ± 0.15 | 3 ± 0.2 | 6 ± 0.22 | 6 ± 0.26 | |
AUC last (ng.h/ml) | 1828 ± 194 | 4336 ± 474 | 9410 ± 553 | 14,658 ± 592 | |
AUMC | 25,535 ± 3589 | 119,549 ± 17,352 | 330,328 ± 2126* | 582,753 ± 21,258* | |
MRT (h) | 13.2 ± 3.8 | 27.55 ± 6.1 | 35.48 ± 5.9 | 42 ± 4.6 | |
AUC 0-∞ (ng.h/ml) | 1898 ± 197 | 6440 ± 542 | 8961 ± 705 | 12,955 ± 892 | |
T1/2 (h) | 5.65 ± 0.52 | 16 ± 1.2 | 34 ± 2 | 50 ± 1.45 | |
Clearance (L/h/Kg) | 1.01 ± 0.01 | 0.461 ± 0.033 | 0.213 ± 0.006^ | 0.136 ± 0.005^ |
Data from the three independent experiments denote mean ± standard deviation (n = 3)
#, $Indicated significant (p < 0.05) improvement in AUC and MRT values in plasma for Apt-NLCs/PEG-NLCs treated animals in comparison to NLCs. (*) Indicated significant (p < 0.05) improvement in AUC in liver values in Apt-NLCs/PEG-NLCs treated animals in comparison to NLCs. ^ indicated significant (p < 0.05) reduction in hepatic clearance in Apt-NLCs/PEG-NLCs treated animals in comparison to NLCs