In-vivo bioavailability and lymphatic uptake evaluation of lipid nanoparticulates of darunavir

Figures & data

Figure 1. TEM image of freeze-dried SLN.

Table 1. Micromeritic properties of freeze-dried darunavir-SLN (n = 3).

Parameters	Value
Angle of repose	19.82
Bulk density	0.510
Tapped density	0.588
Carr's Index	13.26
Hausners ratio	1.15

Figure 2. In vitro release profile of darunavir-SLN in simulated gastric condition (n = 6, mean ± SD).

Figure 3. Ex-vivo apparent permeability of Dar SLN at (a) 37 °C, (b) 4 °C, in the presence of (c) CPZ at 37 °C and (d) NYT at 37 °C (n = 3).

Figure 4. In-vivo plasma concentrations profile of marketed tablet and darunavir-SLN in rats (n = 6, ± SD).

Table 2. In-vivo pharmacokinetic parameters of marketed tablet and darunavir-SLN in rats.

Parameters	Marketed tablet	Darunavir-SLN
Cmax	1.9 µg/ml	3.95 µg/ml
Tmax	2 h	4 h
Slope (Kele)	0.104 h^−1	0.053 h^−1
T1/2	6.64	13.16
AUC0−t	13.22	26
AUC0−∞	23.96	86.79
AUCt−∞	10.73	60.78

Figure 5. In-vivo plasma concentrations profile of darunavir-SLN in CXI-treated and CXI-non-treated rats (n = 6, ± SD).

Table 3. In-vivo pharmacokinetic parameters of darunavir-SLN in rats in the presence and absence of lymphatic uptake blockers (CXI).

Parameters	CXI treated	CXI non-treated
Cmax	2.56 µg/ml	3.95 µg/ml
Tmax	4 h	4 h
Slope (Kele)	0.040 h^−1	0.053 h^−1
T1/2	17.25	13.16
AUC0−t	17.19	26
AUC0−∞	71.46	86.79
AUCt−∞	54.26	60.78

Figure 6. Concentration of darunavir in the lymphatic fluid of rats (n = 6, ± SD).