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Uptake of albumin nanoparticle surface modified with glycyrrhizin by primary cultured rat hepatocytes

2005; Baishideng Publishing Group; Volume: 11; Issue: 20 Linguagem: Inglês

10.3748/wjg.v11.i20.3075

2219-2840

Shengjun Mao,

Phytochemistry and biological activity of medicinal plants

AIM:To investigate the uptake difference between bovine serum albumin nanoparticle (BSA-NP) and bovine serum albumin nanoparticles with their surface modified by glycyrrhizin (BSA-NP-GL) and to develop a novel hepatocyte targeting BSA-NP-GL based on active targeting technology mediated by specific binding site of GL on rat cellular membrane. METHODS:Calcein loaded bovine serum albumin nanoparticles (Cal-BSA-NP) were prepared by desolvation process.Glycyrrhizin was conjugated to the surface reactive amino groups (SRAG) of Cal-BSA-NP by sodium periodate oxidization, which resulted in calcein-loaded bovine serum albumin nanoparticles with their surface modified by glycyrrhizin (Cal-BSA-NP-GL).The morphology of the two types of prepared nanoparticles (NP) was observed by transmission electron microscopy.The diameter of NP was measured with a laser particle size analyzer.The interaction between Cal-BSA-NP-GL and primary cultured hepatocytes was studied through cellular uptake experiments.The uptake amount of Cal-BSA-NP-GL and Cal-BSA-NP by rat hepatocytes was determined by fluorospectrophotometry. Uptake characteristics were investigated through experiments of competitive inhibition of specific binding site of GL. RESULTS:Both Cal-BSA-NP-GL and Cal-BSA-NP had regular spherical surfaces.The average diameter of Cal-BSA-NP-GL and Cal-BSA-NP was 77 and 79 nm respectively.The uptake amount of the two NP by hepatocytes reached its maximum at 2 h after incubation.The uptake amount of Cal-BSA-NP-GL by rat hepatocytes was 4.43-fold higher than that of Cal-BSA-NP.There was a significant difference in the uptake of Cal-BSA-NP-GL and Cal-BSA-NP by hepatocytes (P<0.01).The uptake of Cal-BSA-NP-GL was inhibited when GL was added previously to isolated rat hepatocytes, and the uptake of Cal-BSA-NP was not affected by GL. CONCLUSION:A binding site of GL is present on the surface of rat hepatocytes, BSA-NP-GL may be internalized via this site by hepatocytes and can be used as a drug carrier for active targeting of delivery drugs to hepatocytes.