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Solid lipid nanoparticles loading adefovir dipivoxil for antiviral therapy
Authors:Xing-guo Zhang  Jing Miao  Min-wei Li  Sai-ping Jiang  Fu-qiang Hu  and Yong-zhong Du
Affiliation:[1]Department of Pharmacy, the First Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou 310003, China; [2]College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China; [3]State Key Lab for Diagnosis and Treatment of lnfectious Diseases, Zhejiang University, Hangzhou 310003, China
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.
Keywords:Adefovir dipivoxil (ADV)  Solid lipid nanoparticles (SLN)  Octadecylamine-fluorescein isothiocynate (ODA-FITC)  Hepatitis B virus (HBV)
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