Journal of Zhejiang University SCIENCE B
ISSN 1673-1581(Print), 1862-1783(Online), Monthly

2008   Vol. 9   No. 6   p. 506~510

Solid lipid nanoparticles loading adefovir dipivoxil for antiviral therapy

Xing-guo ZHANG^†1, Jing MIAO¹, Min-wei LI^1,3, Sai-ping JIANG¹, Fu-qiang HU², Yong-zhong DU²

(¹Department of Pharmacy, the First Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou 310003, China)
(²College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China)
(³State Key Lab for Diagnosis and Treatment of Infectious Diseases, Zhejiang University, Hangzhou 310003, China)
^†E-mail: xgzhang666@yahoo.com.cn
Received Feb. 16, 2008; revision accepted Apr. 24, 2008

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.

Key words: Adefovir dipivoxil (ADV), Solid lipid nanoparticles (SLN), Octadecylamine-fluorescein isothiocynate (ODA-FITC), Hepatitis B virus (HBV)
doi:10.1631/jzus.B0820047             CLC number: R512.6+2; R943; R978.7

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