In Vitro and in Vivo Antitumor Efficacy of Berberine-solid Lipid Nanoparticles Against H22 Tumor

Abstract

Hepatocarcinoma, a malignant cancer, threaten human life badly. It is a current issue to seek the effective natural remedy from plant to treat cancer due to the resistance of the advanced hepatocarcinoma to chemotherapy. Berberine (Ber), an isoquinoline derivative alkaloid, has a wide range of pharmacological properties and is considered to have anti-hepatocarcinoma effects. However its low oral bioavailability restricts its wide application. In this report, Ber loaded solid lipid nanoparticles (Ber-SLN) was prepared by hot melting and then high pressure homogenization technique. Both in vitro and in vivo anti-hepatocarcinoma effects of Ber-SLN relative to efficacy of bulk Ber were evaluated. The particle size and zeta potential of Ber-SLN were 154.2 ± 0.8 nm and −18.63±0.99mV, respectively. MTT assay showed that Ber-SLN effectively inhibited the proliferation of H22 cells, and the corresponding IC 50 values were 11.6 µg/ml (18.3 µg/ml of bulk Ber). In vivo studies also showed higher antitumor efficacy, and inhibition rates was 65.1% (41.4 % of bulk Ber) at 100mg/kg intragastric administration in H22 solid tumor bearing mice. These results suggest that the delivery of Ber-SLN is a promising approach for treating tumors.

The therapeutic effects of berberine for gastrointestinal cancers

“…Berberine reduced the proliferation of H22 cancer cells in vivo and in vitro 89 Abbreviations: AMPK, AMP-activated protein kinase; CAR, constitutive androstane receptor; MAPK, mitogen-activated protein kinase; PI3K, phosphatidylinositol-3 kinase; mTOR, mammalian target of rapamycin; VEGF, vascular endothelial growth factor.…”