Table 9.
Pharmacokinetics (PKs) of catechin hydrate after i.n. and i.v. administration to rats at the dose of 10 mg kg−1 in the brain, lungs, and plasma (n = 6, mean ± SD). AUC, area under curve.
| Formulation Administration | Samples | Cmax (ng/mL g) | Tmax | t1/2 (h) | Ke (h−1) | AUC0–t (ng min/mL g) |
| CH–S (i.n.) | Brain | 81.68 ± 10.13 | 2.00 | 15.25 ± 2.06 | 0.04544 ± 0.0006 | 977.32 ± 33.14 |
| Lungs | 28.64 ± 3.09 | 2.00 | 21.77 ± 2.19 | 0.03184 ± 0.00011 | 373.85 ± 16.47 | |
| Plasma | 32.02 ± 2.63 | 0.50 | 8.23 ± 3.10 | 0.08420 ± 0.0009 | 170.48 ± 18.43 | |
| CH–S (i.v.) | Brain | 44.23 ± 7.04 | 2.00 | 11.16 ± 0.39 | 0.06210 ± 0.0009 | 395.26 ± 19.47 |
| Lungs | 95.43 ± 18.14 | 2.00 | 9.19 ± 0.81 | 0.07540 ± 0.00051 | 958.79 ± 34.64 | |
| Plasma | 1141.54 ± 83.45 | 0.50 | 4.69 ± 0.29 | 0.14767 ± 0.0018 | 3167.33 ± 55.67 | |
| CH–PLGA–NPs (i.n.) | Brain | 623.36 ± 24.21 | 2.00 | 24.71 ± 4.59 | 0.02806 ± 0.00006 | 7785.90 ± 83.64 |
| Lungs | 106.97 ± 11.97 | 2.00 | 11.00 ± 1.01 | 0.06303 ± 0.00011 | 1033.42 ± 44.67 | |
| Plasma | 56.78 ± 4.64 | 2.00 | 8.26 ± 0.97 | 0.08391 ± 0.00008 | 409.41 ± 25.94 | |
| CS–CH–PLGA–NPs (i.n.) | Brain | 996.24 ± 44.24 | 2.00 | 21.81 ± 3.94 | 0.03178 ± 0.00008 | 12444.50 ± 139.25 |
| Lungs | 121.64 ± 18.45 | 2.00 | 11.21 ± 2.88 | 0.06184 ± 0.0008 | 1187.01 ± 31.04 | |
| Plasma | 99.67 ± 10.18 | 2.00 | 9.33 ± 0.94 | 0.07427 ± 0.00013 | 936.04 ± 86.79 | |
| CH–PLGA–NPs (i.v.) | Brain | 98.36 ± 19.55 | 2.00 | 15.91 ± 3.06 | 0.04355 ± 0.00010 | 1170.58 ± 28.57 |
| Lungs | 109.94 ± 7.98 | 2.00 | 11.52 ± 2.97 | 0.06016 ± 0.0005 | 1091.68 ± 34.67 | |
| Plasma | 757.54 ± 33.16 | 1.00 | 16.65 ± 1.06 | 0.04162 ± 0.0007 | 9430.18 ± 189.67 | |
| CS–CH–PLGA–NPs (i.v.) | Brain | 126.48 ± 17.61 | 2.00 | 67.83 ± 5.47 | 0.01022 ± 0.00006 | 1959.57 ± 79.68 |
| Lungs | 136.48 ± 15.97 | 2.00 | 62.03 ± 2.91 | 0.01117 ± 0.0010 | 1974.57 ± 44.89 | |
| Plasma | 1064.43 ± 96.43 | 1.00 | 15.83 ± 1.06 | 0.04378 ± 0.0006 | 12948.59 ± 277.13 | |
| CH–S (i.n.) | Brain/Plasma | 2.55 | 4.00 | 1.85 | 0.54 | 5.73 |
| CH–S (i.v.) | Brain/Plasma | 0.039 | 4.00 | 2.38 | 0.42 | 0.13 |
| CH–PLGA–NPs (i.n.) | Brain/Plasma | 10.98 | 1.00 | 2.99 | 0.34 | 19.02 |
| CH–PLGA–NPs (i.v.) | Brain/Plasma | 0.13 | 2.00 | 0.96 | 1.05 | 0.12 |
| CS–CH–PLGA–NPs (i.n.) | Brain/Plasma | 10.00 | 1.00 | 2.34 | 0.43 | 13.29 |
| CS–CH–PLGA–NPs (i.v.) | Brain/Plasma | 0.13 | 2.00 | 4.29 | 0.23 | 0.15 |
| Comparative Bioavailability * (AUCi.n./AUCi.v.); (%) | ||||||
| Formulations | CH–S | CH–PLGA–NPs | CS–CH–PLGA–NPs | |||
| Blood | 5.38 | 4.34 | 7.23 | |||
| Brain | 247.26 * | 665.13 ** | 1063.11 *** | |||
* Parameters are derived using mean ± SEM values of six different estimations. For the p-value: *** (p < 0.001), ** (p < 0.01), and * (p < 0.05).