Protective effects on myocardial infarction model: delivery of schisandrin B using matrix metalloproteinase-sensitive peptide-modified, PEGylated lipid nanoparticles

Figures & data

Figure 1 Synthesis of PEG lipid and MMP-targeting peptide conjugate (A); preparation of MMP-Sch B SLNs (B).

Abbreviations: PEG, polyethylene glycol; MMP, matrix metalloproteinase; Sch B, schisandrin B; SLNs, solid lipid nanoparticles.

Figure 2 ¹H NMR spectra of the PEG lipid and MMP-targeting peptide conjugate.

Abbreviations: ¹H NMR, ¹H nuclear magnetic resonance; MMP, matrix metallo-proteinase; PEG, polyethylene glycol.

Figure 3 The size (A), zeta potential (B), drug entrapment efficiency (C), and drug loading capacity (D) of MMP-Sch B SLNs, Sch B SLNs, and SLNs.

Abbreviations: MMP, matrix metalloproteinase; Sch B, schisandrin B; SLNs, solid lipid nanoparticles.

Figure 4 In vitro release profile of Sch B loaded SLNs and Sch B solution.

Abbreviations: MMP, matrix metalloproteinase; Sch B, schisandrin B; SLNs, solid lipid nanoparticles.

Figure 5 In vitro cytotoxicity of Sch B loaded SLNs and blank SLNs at various concentrations.

Abbreviations: MMP, matrix metalloproteinase; Sch B, schisandrin B; SLNs, solid lipid nanoparticles.

Table 1 The comparative pharmacokinetic parameters via intravenous administration of Sch B-loaded SLNs and Sch B solution in rats (n=8)

Systems	AUC0–t (mg/L⋅h)	AUC0–∞ (mg/L⋅h)	T1/2 (h)	V (L/kg)	CL (L/kg/h)
Sch B solution	12.43±1.31	13.71±1.54	0.93±0.09	18.46±2.61	3.94±0.72
Sch B SLNs	273.36±13.23*	282.41±12.53*	4.26±0.96*	9.27±0.92*	0.96±0.07*
MMP-Sch B SLNs	284.32±15.61*	291.69±18.12*	4.64±0.68*	9.58±0.75*	0.91±0.08*

Note:

* P<0.05.

Abbreviations: MMP, matrix metalloproteinase; Sch B, schisandrin B; SLNs, solid lipid nanoparticles; V, volume of distribution; CL, plasma clearance.

Figure 6 The mean plasma drug concentration-time profiles of Sch B loaded SLNs and Sch B solution.

Abbreviations: MMP, matrix metalloproteinase; Sch B, schisandrin B; SLNs, solid lipid nanoparticles.

Figure 7 In vivo tissue biodistribution behavior of Sch B loaded SLNs and Sch B solution evaluated in the myocardial infarction rat models after 2 h (A) and 48 h (B) of administration.

Note: *P<0.05.

Abbreviations: MMP, matrix metalloproteinase; Sch B, schisandrin B; SLNs, solid lipid nanoparticles.

Figure 8 In vivo effects of Sch B loaded SLNs and Sch B solution on infarct size evaluated in the myocardial infarction rat models.

Note: *P<0.05.

Abbreviations: MMP, matrix metalloproteinase; Sch B, schisandrin B; SLNs, solid lipid nanoparticles.