Preparation and Anti-liver Cancer Effect of Galactose-modified Polyamide-amine Dendrimers Loaded with Baicalin Nanocomposites

OBJECTIVE To prepare a novel liver-targeting nanocomposite(BA/PAMAM-Gal) using galactose(Gal)-modified polyamide-amine(PAMAM) dendrimers loaded with baicalin(BA), and to evaluate its physicochemical properties and in vitro proliferation inhibitory activity against hepatocellular carcinoma(HCC) cells.

METHODS The structure of PAMAM-Gal carrier was characterized using the Fourier transform infrared spectroscopy(FT-IR) and proton nuclear magnetic resonance spectroscopy(¹H NMR). The particle size distribution and Zeta potential of BA/PAMAM-Gal nanocomposite were determined using a laser particle size analyzer. HPLC was applied to evaluate the drug loading, encapsulation efficiency and in vitro release rate. The cytotoxicity of the nanocomposite against HCC cells was evaluated via CCK-8 assay.

RESULTS The BA/PAMAM-Gal nanocomposite was successfully prepared with a particle size of (386.4±10.0)nm and a Zeta potential of (–5.3±1.8)mV. The drug loading and encapsulation efficiency were (16.9±4.8)% and (19.6%±3.4)%, respectively. The nanocomposite exhibited sustained release behavior in vitro. Furthermore, BA/PAMAM-Gal significantly inhibited the viability of MHCC97H liver cancer cells and induced cell cycle arrest at the G0/G1 phase.

CONCLUSION The novel liver-targeting BA/PAMAM-Gal nanocomposite is successfully prepared with satisfactory properties. It exhibits excellent inhibitory effects on liver cancer cells and can block the cell cycle progression of MHCC97H cells.