Hepatocytes targeting of cationic liposomes modified with soybean sterylglucoside and polyethylene glycol

doi:10.3748/wjg.v11.i32.4947

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World Journal of Gastroenterology

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1007-9327

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Baishideng Publishing Group Inc, 7041 Koll Center Parkway, Suite 160, Pleasanton, CA 94566, USA

Basic Research

World J Gastroenterol. Aug 28, 2005; 11(32): 4947-4952
Published online Aug 28, 2005. doi: 10.3748/wjg.v11.i32.4947

Hepatocytes targeting of cationic liposomes modified with soybean sterylglucoside and polyethylene glycol

Xian-Rong Qi, Wen-Wei Yan, Jing Shi

Xian-Rong Qi, Wen-Wei Yan, Jing Shi, Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China

Author contributions: All authors contributed equally to the work.

Supported by the National Natural Science Foundation of China, No. 30371265

Correspondence to: Professor Xian-Rong Qi, Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China. qixr2001@yahoo.com.cn

Telephone: +86-10-82801584 Fax: +86-10-62015584

Received: November 15, 2004
Revised: February 15, 2005
Accepted: February 18, 2005
Published online: August 28, 2005

Abstract

AIM: In this study, a hepatocyte-specific targeting technology was developed by modifying cationic liposomes with soybean sterylglucoside (SG) and polyethylene glycol (PEG) (C/SG/PEG-liposomes).

METHODS: The liposomal transfection efficiencies in HepG₂ 2.2.15 cells were estimated with the use of fluorescein sodium (FS) as a model drug, by flow cytometry. The antisense activity of C/SG/PEG-liposomes entrapped antisense oligonucleotides (ODN) was determined as HBsAg and HBeAg in HepG₂ 2.2.15 cells by ELISA. The liposome uptake by liver and liver cells in mice was carried out after intravenous injection of ³H-labeled liposomes.

RESULTS: C/SG-liposomes entrapped FS were effectively transfected into HepG₂ 2.2.15 cells in vitro. C/SG/PEG-liposomes entrapped ODN, reduced the secretion of both HBsAg and HBeAg in HepG₂ 2.2.15 cells when compared to free ODN. After in vivo injection of ³H-labeled C/SG/PEG-liposomes, higher radiation accumulation was observed in the hepatocytes than non-parenchymal cells of the liver.

CONCLUSION: C/SG/PEG-liposomes mediated gene transfer to the liver is an effective gene-delivery method for hepatocytes-specific targeting, which appears to have a potential for gene therapy of HBV infections.

Keywords: Hepatocytes targeting; Cationic liposomes; Soybean sterylglucoside