Bifendate liposomes modified by bile and its role in enhancing hepatocytes uptake in vitro

The aim of this study was to investigate the possibility of using bile-modified liposomes as a targeting carrier to increase the accumulation of bifendate (DDB) in hepatic cells.Both liposomes (LP) and liposomes modified by bile (BP₂B-LP) containing DDB(BP₂B-LP-DDB) were prepared by the method of film ultrasonic dispersion.The entrapment efficiency of LP-DDB and BP₂B-LP-DDB was determined following the separation by Sephadex gel and their physicochemical properties were also studied.Hepatic cellular uptake of LP-DDB and BP₂B-LP-DDB was evaluated in vitro，including incubation temperature，the dose and the addition of bile.It revealed that the entrapment efficiencies of LP-DDB and BP₂B-LP-DDB were about (90.66±1.22)% and (86.89±1.61)%；the mean size (309.52±16.74) nm and (273.77±14.14) nm；the Zeta potential (24.98±2.03 ) mV and (22.21±7.03) mV，respectively.And it was shown that there was remarkable increase in cellular uptake of BP₂B-LP-DDB when compared to that of LP-DDB.Hence，BP₂B-LP could be a targeting carrier to facilitate the delivery of the encapsulated DDB into the hepatocytes，possibly via the mechanism of receptor mediation.