Table 3.
Pharmacokinetic parameters after oral administration of CyA-loaded SPC/SDC, SPC/Chol liposomes and Sandimmune Neoral (n = 6)
Formulation | Tmax (h) | Cmax (μg/mL) | t1/2 (h) | AUC0–t (μg · h/mL) | AUC0−∞ (μg · h/mL) | MRT (h) | Relative bioavailability* |
---|---|---|---|---|---|---|---|
SPC/SDC liposomes | 4.67 ± 1.49 | 2.65 ± 0.70 | 20.54 ± 7.63 | 42.16 ± 6.30 | 73.90 ± 6.63 | 10.73 ± 0.90 | 120.3% |
SPC/Chol liposomes | 2.67 ± 0.69 | 2.28 ± 0.31 | 19.84 ± 6.50 | 34.56 ± 4.08 | 60.49 ± 10.79 | 10.42 ± 0.37 | 98.6% |
Sandimmun Neoral® | 2.67 ± 0.69 | 2.57 ± 0.20 | 19.09 ± 10.15 | 35.02 ± 4.68 | 65.41 ± 29.55 | 10.23 ± 0.64 |
Note:
Relative bioavailability (%) of the liposomes calculated on AUC0−t with Sandimmune Neoral as the reference.
Abbreviations: Chol, cholesterol; CyA, cyclosporine A; soybean phosphatidylcholine; SDC, sodium deoxycholate; MRT, maximum retention time.