Solid lipid nanoparticles loading adefovir dipivoxil for antiviral therapy.

Area of Science:

• Nanotechnology
• Pharmacology
• Hepatology

Background:

• Hepatitis B virus (HBV) infection remains a significant global health concern.
• Adefovir dipivoxil (ADV) is an antiviral medication used to treat HBV infection.
• Developing advanced drug delivery systems can improve the efficacy of existing antiviral therapies.

Purpose of the Study:

• To develop and characterize solid lipid nanoparticles (SLN) for the delivery of adefovir dipivoxil (ADV).
• To investigate the cellular uptake and in vitro efficacy of ADV-loaded SLN against HBV.
• To evaluate the potential of SLN as an improved drug delivery system for ADV.

Main Methods:

• Synthesis of octadecylamine-fluorescein isothiocyanate (ODA-FITC) as a fluorescence marker.
• Preparation of monostearin-based SLN encapsulating ODA-FITC or ADV using the solvent diffusion method.
• Characterization of SLN for drug entrapment efficiency (EE) and drug loading (DL).
• In vitro assessment of ADV-loaded SLN efficacy by measuring hepatitis B surface antigen (HBsAg), hepatitis B e antigen (HBeAg), and HBV DNA levels.

Main Results:

• Solid lipid nanoparticles (SLN) were successfully prepared with adefovir dipivoxil (ADV), achieving approximately 15 wt% entrapment efficiency and 3 wt% drug loading.
• Cellular uptake of SLN by HepG2.2.15 cells was investigated using ODA-FITC labeled SLN.
• ADV-loaded SLN demonstrated significantly enhanced inhibitory effects on HBsAg, HBeAg, and HBV DNA levels compared to free ADV in vitro.

Conclusions:

• Solid lipid nanoparticles (SLN) represent a promising drug delivery system for adefovir dipivoxil (ADV).
• ADV-loaded SLN significantly improved the in vitro antiviral activity against key hepatitis B virus (HBV) markers.
• This nanotechnology-based approach offers potential for enhanced therapeutic outcomes in HBV treatment.