ABSTRACT
OBJECTIVE: To develop a polyethylene glycol (PEG) modified cationic liposomes for the co-delivery of siRNA and honokiol to improve tumor therapy. METHODS: The PEG-modified cationic liposomes were prepared by thin film hydration method. Honokiol was loaded in the liposomes with hydrophobic interaction and siRNA was loaded with electrostatic interaction. The optimal formulation was screened according to size, Zeta potential, entrapment efficiency and serum stability. The liposomes were characterized with cellular uptake and intracellular localization of siRNA. The pharmacodynamic effect of honokiol-loaded liposomes (LH) and hono-kiol-siRNA-loaded liposomes (LH-siRNA) were verified by inhibition of cancer cell growth. RESULTS: All the honokiol-loaded liposomes had an average particel size of about 100 nm with high drug entrapment efficiency. The optimal liposome formulation (N/P ratio of 5) exhibited the best cellular uptake. The results of pH-dependent hemolysis and intracellular localization suggested that the LH-siRNA had good ability of endosomal escape. In vitro cell growth experiments showed that both LH and LH-siRNA had good inhibition action on tumor cell growth based on the effects of honokiol and siRNA. CONCLUSION: The PEG-modified cationic liposomes can be a potential carrier for co-delivery of siRNA and honokiol to tumors.