Preparation of camptothecin-loaded targeting nanoparticles and their antitumor effects on hepatocellular carcinoma cell line H22

Figures & data

Table 1. Characterization of CPT NPs.

Nanoparticles	Particle size (nm)	Polydispersity index	Zeta potential (mV)	Entrapment efficiency (%)	Drug loading (%)
Biotin-F127-PLA	165.7 ± 19.2	0.183 ± 0.015	−9.2 ± 0.3	29.3 ± 1.05	8.8 ± 0.56
F127-PLA	158.4 ± 16.7	0.175 ± 0.013	−14.5 ± 0.7	33.0 ± 2.06	9.9 ± 0.98

Figure 1. (A) Size distribution of CPT-loaded biotin-F127-PLA NPs and (B) transmission electron micrograph of the targeted CPT NPs.

Table 2. Evaluation of antibody binding rate and coupling ratio of antibody to NPs.

Concentration of biotinylated antibody (μg/mL)	Antibody binding rate (%)	Coupling ratio of antibody to NPs (%)
10	94.32 ± 4.67	0.18 ± 0.02
20	92.51 ± 3.84	0.35 ± 0.04^a
40	85.26 ±  2.96^a	0.65 ± 0.06^a
60	70.47 ± 2.79^a	0.81 ± 0.08^a
80	53.71 ± 2.26^a	0.82 ± 0.05^a

^ap < 0.05 compared to 10 (μg/mL) antibody.

Figure 2. In vitro release profile of CPT from NPs in phosphate buffer solutions.

Figure 3. In vitro antitumor effects of CPT NPs on H22 cell lines. The concentrations of the blank NPs (control group) were set at the same level as those in the drug-loaded NPs group. **p < 0.01 compared with the control group.

Figure 4. Tissue distribution of CPT in tumor-bearing mice after intravenous administration of non-targeted NPs (A) and targeted NPs (B). *p < 0.05 compared with the plasma.

Figure 5. In vivo antitumor effect of CPT in either targeted or non-targeted CPT NPs in H22-bearing mice. Tumor weight (A) and tumor inhibition rate (B). *p < 0.05 compared to the free CPT group.

Figure 6. Survivin mRNA expression of mice bearing H22 tumor tissue. *p < 0.05 compared with the control group.