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Biodistribution and hepatocytes targeting of cationic liposomes surface-modified with sterylglucoside and golyethylene glycol

Shi, J.; Yan, W-Wei.; Qi, X-Rong.; Yang, L.; Zhang, L.

Yao Xue Xue Bao 39(7): 551-555

2004

ISSN/ISBN: 0513-4870
PMID: 15493849
Document Number: 570597
Aim To investigate the biodistribution and the hepatoctyes targeting of cationic liposome containing 3beta-(N-(N',N'-dimethylaminoethane) carbamoyl) cholesterol (DC-Chol) and surface-modified liposomes with sterylglucoside (SG) and polyethylene glycol-distearoylphosphatidylethanolamine (PEGDSPE). Methods Cationic liposomes (CL) composed of DC-Chol and dipalmitoylphosphatidylcholine (DPPC), SG/PEG modified cationic liposome (SG/PEG-CL), both contained trace 3H-cholesterol (3H-Chol) as radiolabel, were prepared. The liposomes encapsulating 125I-labled antisense oligodeoxynucleotide (125I-asODN) (SG/PEG-CL-asODN) were also prepared. The biodistribution of CL, SG/PEG-CL, SG/PEG-C2-asODN as well as 125I-asODN solution, were studied. The radioactivities in hepatoctyes and non-hepatoctyes after administration of CL and SG/PEG-CL were determined by infuseing method. Results CL and SG/PEG CL significantly aggregated in liver. The distribution of SG/PEG CL was significantly higher in hepatocytes (P0.01) and lower in non-hepatocytes (P0.01) than that of CL. The concentrations of SG/PEG-CL-asODN in liver and spleen were significantly higher than that of asODN solution (P 0.01). Conclusion Cationic liposome modified with SG/PEG changed the distribution of asODN. Cationic liposome can target hepatocytes more effective after being modified with SG.

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