Figure 5.

(A) Comparative efficacy study in an HCC Hep 3B cancer cell-derived xenograft nude mouse model using SN38-formulated NPs. NP solutions containing SN38 prodrugs (15 mg/kg, the SN38 equivalent dose) were injected three successive times. Saline and CPT-11 (22.5 mg/kg) were also intravenously injected as controls. Arrows represent the i.v. injections. The tumor sizes were monitored using a caliper. The data are expressed as the means ± s.d. (n = 7); *p < 0.05, ***p < 0.001. (B) Body weight changes of the mice after drug administration. (C) Representative images of the excised tumors for the groups treated with saline, CPT-11, and oLA₈-SN38-NPs. However, the largest tumors in the other groups at the end point are shown in (C). (D) H&E and TUNEL analyses of the excised tumors from the treated groups at day 2 post-single injection of the drugs (15 mg/kg, at SN38 equivalent dose). The tumor sections were stained with H&E (left), DAPI for nuclei (blue, middle), and fluorescein-dUTP for apoptosis (green, right). Potent induction of apoptosis was observed in NP-treated mice, which is consistent with the tumor inhibition results. Scale bars, 100 μm.