Preparation of isoliquiritigenin-loaded nanostructured lipid carrier and the in vivo evaluation in tumor-bearing mice

Isoliquiritigenin-loaded nanostructured lipid carrier (ISL-NLC) was constructed and characterized. In vivo antitumor efficacy and immuno-modulation effects of ISL-NLC were evaluated in sarcoma 180 (S180)-bearing and murine hepatoma 22 (H22)-bearing mice model through intraperitoneal (i.p.) administration. The ISL-NLC biodistribution was also investigated in H22-bearing mice. Results demonstrated that the ISL-NLC had a spherical shape with a mean size of (160.73 ± 6.08) nm and encapsulation efficiency of (96.74 ± 1.81)%. ISL released from the nanoparticles was in a sustained manner with an initial burst release. ISL-NLC significantly inhibit tumor growth at 10, 20 and 40 mg/kg levels, and inhibition rates were 75.70%, 82.27% and 83.90% in the S180-bearing mice and 71.49%, 81.11% and 85.62% in the H22-bearing mice, respectively. The biodistribution study showed that ISL concentration of ISL-NLC in tumor is higher 2.5-fold than ISL suspension. The elimination half-life (t1/2), area under the curve (AUC) and the mean residence times (MRTs) of the ISL-NLC was much longer than that of the ISL suspension. As a whole, anticancer effect of ISL encapsulated in NLC was superior to ISL in suspension on H22-bearing and S180-bearing mice at the same dose and was a dose-dependent way, and ISL-NLC improved immunity of ISL. It can be inferred that nanostructured lipid carriers are a promising carrier for cancer therapy using ISL.

Graphical abstractConstruct isoliquiritigenin-loaded nanostructured lipid carriers that could significantly inhibit tumor growth and increase immunity of isoliquiritigenin and enhance isoliquiritigenin distribution to tumor.Download high-res image (208KB)Download full-size image