JZUS - Journal of Zhejiang University SCIENCE

Journal of Zhejiang University SCIENCE B 2008 Vol.9 No.6 P.506-510

http://doi.org/10.1631/jzus.B0820047

Solid lipid nanoparticles loading adefovir dipivoxil for antiviral therapy

Author(s): Xing-guo ZHANG, Jing MIAO, Min-wei LI, Sai-ping JIANG, Fu-qiang HU, Yong-zhong DU
Affiliation(s): Department of Pharmacy, the First Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou 310003, China; more
Corresponding email(s): xgzhang666@yahoo.com.cn
Key Words: Adefovir dipivoxil (ADV), Solid lipid nanoparticles (SLN), Octadecylamine-fluorescein isothiocynate (ODA-FITC), Hepatitis B virus (HBV)

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Abstract: Herein, solid lipid nanoparticles (SLN) were proposed as a new drug delivery system for adefovir dipivoxil (ADV). The octadecylamine-fluorescein isothiocynate (ODA-FITC) was synthesized and used as a fluorescence maker to be incorporated into SLN to investigate the time-dependent cellular uptake of SLN by HepG2.2.15. The SLN of monostearin with ODA-FITC or ADV were prepared by solvent diffusion method in an aqueous system. About 15 wt% drug entrapment efficiency (EE) and 3 wt% drug loading (DL) could be reached in SLN loading ADV. Comparing with free ADV, the inhibitory effects of ADV loaded in SLN on hepatitis B surface antigen (HBsAg), hepatitis B e antigen (HBeAg) and hepatitis B virus (HBV) DNA levels in vitro were significantly enhanced.

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