Long-circulating nanoliposomes (LCNs) sustained delivery of baicalein (BAI) with desired oral bioavailability in vivo

Figures & data

Table1. The orthogonal designs L₉(4³) for optimize preparation conditions of BAI-loaded LCNs.

Factor Level	Mass ratio of SPC:CHOL*	Dosage of BAI/g	The volume of diethyl ether/mL	The volume of 0.1 M phosphate buffer (pH 7.4)/mL
1	4:1	0.020	5	30
2	6:1	0.040	10	25
3	8:1	0.060	15	20

*Set value of CHOL is 0.06 g.

Figure 1. Size distribution of BAI-loaded LCNs.

Table 2. Results of orthogonal experiments.

Number of experiment	Mass ratio of SPC:CHOL	Dosage of BAI/g	Volume of diethyl ether/mL	Volume of phosphate buffer (pH 7.4)/mL	EE/%
1	1	1	1	1	30.91
2	1	2	2	2	21.73
3	1	3	3	3	23.74
4	2	1	1	1	38.31
5	2	2	2	2	38.51
6	2	3	3	3	23.64
7	3	1	1	1	43.60
8	3	2	2	2	35.46
9	3	3	3	3	30.36
K1	76.38	112.82	90.01	99.78	T = ΣEF
K2	100.46	95.70	90.40	88.97	=I + II + III
K3	109.42	77.74	105.85	97.51	=286.26
R	33.04	35.08	15.48	10.81

Table 3. Results of intra- and inter-day variability for validation of the proposed method for BAI detection.

	Inter-day (n = 6)			Intra-day (n = 6)
Theoretical concentration (µg/mL)	Mean ± S.D.	R.S.D. (%)	Accuracy (%)	Mean ± S.D.	R.S.D. (%)	Accuracy (%)
0.10	0.104 ± 0.001	0.925	104.203	0.102 ± 0.003	2.546	102.223
1.00	1.025 ± 0.018	1.781	102.515	1.007 ± 0.036	3.557	100.709
3.00	2.986 ± 0.096	3.232	99.533	2.962 ± 0.090	3.050	98.733

Table 4. Results of relative recovery and absolute recovery of BAI in mice plasma (n = 6).

Added (µg/mL)	Found (µg/mL)	Relative recovery (%)	R.S.D. (%)
0.10	0.104 ± 0.001	104.263 ± 1.622	1.556
1.00	1.028 ± 0.008	102.765 ± 0.809	0.787
3.00	2.877 ± 0.036	95.885 ± 1.201	1.253

Figure 2. Plasma concentration–time curve of BAI in mice (x ± s. n = 10).

Table 5. Pharmacokinetic parameters of BAI-loaded LCNs and free BAI solution in mice plasma (n = 10).

Parameters	T1/2 (h)	AUC0--∞ (mg ċ h/L)	CL/F (L/h/kg)	V1/F (L/kg)	Tmax (h)	Cmax (mg/L)
Liposomes (60 mg/kg)	2.79	11.44	5.25	21.13	3.00	1.20
Solution (60 mg/kg)	1.58	2.531	23.702	54.028	2.00	0.688