Optimizing Manufacture of Liposomal Berberine with Evaluation of Its Antihepatoma Effects in a Murine Xenograft Model.

The aim of this work is to establish an optimal process for generating liposomal berberine and assessing its anticancer ability against human hepatic carcinoma in a murine xenograft model. Of various forms of liposomal berberine with different lipid compositions, preparation by various methods, the one that contained 5 mol% polyethenyl glycol (PEG) that was produced by a thin-film hydration/extrusion method exhibited the highest encapsulation efficiency (E.E.) of berberine (14%). Additionally, in vitro studies reveal that this batch of liposomal berberine inhibited the growth of HepG2 cells 2.5 times as effectively as berberine solution since the half maximal inhibitory concentration (IC(50)) of berberine solution was 4.23 μg berberine/mL while that of liposomal berberine was only 1.67 μg berberine/mL, and this inhibition effect was based on the induction of apoptosis through the caspase/mitochondria-dependent pathway. Additionally, the results of in vivo studies indicate that the liposome effectively reduced the rate of elimination of berberine in both plasma and tissues, and liposomal berberine effectively reduced the size and weight of tumors as compared with the untreated tumor control group. Therefore, this work demonstrates that liposome is a good carrier for berberine to inhibit the tumor growth in HepG2 tumor-bearing mice.