Baicalin-loaded PEGylated lipid nanoparticles: characterization, pharmacokinetics, and protective effects on acute myocardial ischemia in rats

Figures & data

Figure 1. A sketch of the preparation of BN-PEG-NLC. BN: baicalin; PEG: polyethylene glycol; NLC: nanostructured lipid carriers.

Table 1. Characterization of NLC.

	Particle size distribution
Formulations	Mean particle size (nm)	Polydispersity index	Zeta potential	EE (%)	DL (%)
NLC	82.6 ± 2.3	0.18 ± 0.06	−36.7 ± 2.1	–	–
BN-NLC	80.8 ± 3.2	0.26 ± 0.07	−34.3 ± 1.6	90.6 ± 2.7	6.5 ± 0.12
BN-PEG-NLC	83.9 ± 1.6	0.21 ± 0.06	−32.1 ± 1.8	83.5 ± 1.2	6.0 ± 0.08

Figure 2. In vitro release profiles of BN from BN-PEG-NLC, BN-NLC, or BN solution. BN: baicalin; PEG: polyethylene glycol; NLC: nanostructured lipid carriers.

Figure 3. The plasma concentration-time profiles of BN following single dose i.v. administration of BN solution, BN-NLC, and BN-PEG-NLC. BN: baicalin; PEG: polyethylene glycol; NLC: nanostructured lipid carriers.

Table 2. Pharmacokinetic parameters of BN after i.v. injecting of BN solution, BN-NLC, and BN-PEG-NLC in rats at a dose of 10 mg/kg (n = 6).

Parameters	Unit	BN solution	BN-NLC	BN-PEG-NLC
AUC0–t	mg/L h	4.35 ± 0.52	13.32 ± 1.20*	32.45 ± 4.36**
AUC0–∞	mg/L h	4.62 ± 0.63	14.02 ± 1.33*	33.26 ± 4.27**
t1/2α	H	0.12 ± 0.02	0.09 ± 0.03	0.11 ± 0.01
t1/2β	h	2.32 ± 0.31	4.29 ± 0.54*	9.82 ± 0.87**
V	L/kg	8.31 ± 1.12	4.35 ± 0.67*	4.26 ± 0.58*
CL	L/kg/h	2.61 ± 0.31	0.83 ± 0.11*	0.76 ± 0.12*

*p < 0.05.

** p < 0.01.

Figure 4. BN tissue concentration of heart, liver, spleen, lung, kidney, and brain at 15 min following i.v. administration of BN solution, BN-NLC, and BN-PEG-NLC in acute MI rat models. BN: baicalin; PEG: polyethylene glycol; NLC: nanostructured lipid carriers.

Figure 5. The images of BN solution, BN-NLC, and BN-PEG-NLC on infract size. BN: baicalin; PEG: polyethylene glycol; NLC: nanostructured lipid carriers.

Figure 6. The effect of BN solution, BN-NLC, and BN-PEG-NLC on infract size. BN: baicalin; PEG: polyethylene glycol; NLC: nanostructured lipid carriers.