Bufalin-loaded mPEG-PLGA-PLL-cRGD nanoparticles: preparation, cellular uptake, tissue distribution, and anticancer activity

Figures & data

Figure 1 TEM (A), size distribution (B), and zeta potential (C) images of bufalin-mPEG-PLGA-PLL-cRGD NPs.

Abbreviations: NPs, nanoparticle drug delivery systems; TEM, transmission electron microscopy.

Table 1 Encapsulation efficiency and drug-loading rate of bufalin-mPEG-PLGA-PLL-cRGD NPs

No	Encapsulation efficiency (%)	Drug-loading rate (%)
1	82.67	4.09
2	81.52	3.78
3	80.91	3.89

Abbreviation: NPs, nanoparticle drug delivery systems.

Figure 2 UV spectrum of PBS, mPEG-PLGA-PLL-cRGD and bufalin.

Abbreviation: PBS, phosphate-buffered saline.

Figure 3 Drug-release profile of NPs.

Abbreviation: NPs, nanoparticle drug delivery systems.

Table 2 The main pharmacokinetic parameters of compartment model estimation

Parameter	Bufalin	BNPs
AUC(0-t) (mg/L*h)	0.26 ± 0.02	0.11 ± 0.01
AUC(0-∞) (mg/L*h)	0.57 ± 0.02	0.43 ± 0.06
MRT(0-t) (h)	1.31 ± 0.11	2.32 ± 0.28
MRT(0-∞) (h)	3.45 ± 0.37	7.63 ± 0.85
t1/2z (h)	3.35 ± 0.31	7.17 ± 2.05
Tmax (h)	0.083 ± 0.011	0.083 ± 0.009
Vz (L/kg)	63.37 ± 1.56	187.83 ± 2.48
Cmax (mg/L)	0.61 ± 0.040	0.34 ± 0.011

Note: Values are mean ± standard deviation (n = 3).

Abbreviations: AUC, area under the curve; MRT, mean residence time; t_1/2z, elimination half-life; T_max, time of maximum concentration; V_z, apparent volume of distribution; C_max, maximal concentration; BNPs, bufalin-loaded mPEG-PLGA-PLL-cRGD nanoparticles.

Figure 4 Cellular viability of SW620 colon cancer cells after 24hours culture with free bufalin and bufalin-NPs.

Notes: *P < 0.05 when compared with bufalin; **P < 0.01 when compared with bufalin by t-test.

Abbreviation: NPs, nanoparticle drug delivery systems.

Figure 5 Confocal images of SW620 colon cancer cells and HUVECs after treatment with Rb-mPEG-PLGA-PLL NPs (A) and Rb-mPEG-PLGA-PLL-cRGD NPs (B), and confocal images of HUVECs after treatment with Rb-mPEG-PLGA-PLL NPs (C) and Rb-mPEG-PLGA-PLL-cRGD NPs (D).

Abbreviations: HUVECs, human umbilical vein endothelial cells; NPs, nanoparticle drug delivery systems; Rb, rhodamine B.

Figure 6 In vivo noninvasive targeted imaging of the tumor-bearing mice injected with Rb-mPEG-PLGA-PLL (A) and Rb-mPEG-PLGA-PLL-cRGD (B) NPs.

Notes: The colors indicate the changes in fluorescence signal intensity from high (red) to low (blue).

Abbreviations: NPs, nanoparticle drug delivery systems; Rb, rhodamine B.

Figure 7 Tumor size in different groups (mm³; n = 10).