Solid lipid nanoparticles loading adefovir dipivoxil for antiviral therapy.
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.
Zhang
Xing-guo
XG
Department of Pharmacy, the First Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou 310003, China. xgzhang666@yahoo.com.cn
Miao
Jing
J
Li
Min-wei
MW
Jiang
Sai-ping
SP
Hu
Fu-qiang
FQ
Du
Yong-zhong
YZ
D000225:Adenine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D000588:Amines; D000998:Antiviral Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002460:Cell Line; D016503:Drug Delivery Systems; D016650:Fluorescein-5-isothiocyanate; D005456:Fluorescent Dyes; D005989:Glycerides; D006515:Hepatitis B virus / Q000187:drug effects; D006801:Humans; D053758:Nanoparticles; D036103:Nanotechnology; D063065:Organophosphonates / Q000008:administration & dosage* / Q000493:pharmacokinetics
D000588:Amines; D000998:Antiviral Agents; D005456:Fluorescent Dyes; D005989:Glycerides; D063065:Organophosphonates; C048159:glyceryl monostearate; C009317:stearylamine; D016650:Fluorescein-5-isothiocyanate; D000225:Adenine; C106812:adefovir dipivoxil