Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes

Figures & data

Figure 1 Chemical structure of baicalin.

Table 1 Stability of BA-LP in simulated gastrointestinal fluid

Parameter	Particle size (nm)			Entrapment efficiency (%)
	Initial	3 hours	6 hours	Initial	3 hours	6 hours
SGF	381±10.8	456±12.5	493±11.0	83.6±0.85	62.7±0.78	44.6±0.59
SIF	381±10.8	366±11.7	371±13.5	83.6±0.85	73.5±0.75	60.0±0.68

Abbreviations: BA-LP, baicalin-loaded liposome; SGF, simulated gastric fluid; SIF, simulated intestinal fluid.

Table 2 Dissolution kinetic parameters of BA from BA solution and BA-LP

	BA solution		BA-LP
	Equation	Correlation coefficient (R)	Equation	Correlation coefficient (R)
Zero-order equation	Q =7.583t+44.326	0.895	Q =3.151t+30.053	0.900
First-order equation	Ln (1–Q) =−0.382t−0.327	0.990	Ln(1−Q) =−0.077t−0.312	0.969
Higuchi	Q =28.732t1/2 + 21.701	0.951	Q =17.636t1/2 +10.705	0.973
Weibull’s equation	lnln(1/(1−Q)) =0.753 lnt −0.371	0.993	lnln(1/(1−Q)) =0.609 lnt −1.230	0.995

Abbreviations: BA, baicalin; BA-LP, BA-loaded liposome.

Figure 2 The in vitro release profile of BA solution and BA-LP.

Abbreviations: BA, baicalin; BA-LP, BA-loaded liposome.

Table 3 Pharmacokinetic parameters of BA in plasma after oral administration of BA-LP and BA-CMC to rats

	BA-CMC	BA-LP
AUC(0−t) (mg/L*h)	12.397	37.64
MRT(0−t) (h)	9.775	8.358
t1/2z (h)	24.833	10.628
Tmax (h)	0.25	0.5
Vz (L/kg)	142.088	32.446
CLz (L/h/kg)	3.965	2.116
Cmax (mg/L)	1.25	3.52

Abbreviations: AUC_(0−t), area under the plasma drug concentration–time curve; BA, baicalin; BA-CMC, baicalin carboxymethyl cellulose solution; BA-LP, BA-loaded liposome; C_max, peak concentration; CL_z, clearance rate; MRT, mean residence time; t_1/2z, statistical moments half life; T_max, time to reach the maximum plasma drug concentration; V_z, volume of distribution.

Figure 3 The plasma concentration–time profile of BA after oral administration of BA solution and BA-LP to rats, at a dose of 100 mg/kg.

Note: The values are expressed as mean ± SD (n=5).

Abbreviations: BA, baicalin; BA-CMC, baicalin–carboxymethyl cellulose solution; BA-LP, BA-loaded liposome; SD, standard deviation.

Figure 4 The tissue distribution of BA after 30 minutes of oral administration of BA-CMC suspension and BA-LP, at a dose of 100 mg/kg, to rats.

Notes: The values expressed as mean ± SD (n=5).

Abbreviations: BA, baicalin; BA-CMC, baicalin–carboxymethyl cellulose solution; BA-LP, BA-loaded liposome; SD, standard deviation.