Galactosylated Nanostructured Lipid Carriers for Delivery of 5-Fu to Hepatocellular Carcinoma Publisher Pubmed



Varshosaz J¹ ; Hassanzadeh F² ; Sadeghi H² ; Khadem M¹ Show Affiliations
Source: Journal of Liposome Research Published:2012

Abstract

The aim of the present study was to design a targeted delivery system of 5-fluorouracil (5-FU) for hepatocellular carcinoma (HCC). Lactobionic acid (LB) was conjugated to stearyl amine (SA) by a chemical reaction. The nanostructured lipid carriers (NLCs), containing LB conjugate, lecithin, glyceryl monostearate, oil [oleic acid (OA) or Labrafac 5 or 10%], and 5-FU, were dissolved in alcohol/acetone, the oil phase was added to the aqueous phase containing Tween 80 or Solutol® HS15 (0.25 or 0.5%), and NLCs were prepared by an emulsification-solvent diffusion method. Physical properties and drug release were studied in NLCs. The thiazolyl blue tetrazolium bromide assay was used to study the cytotoxicity of NLCs on HepG2 cells, and the cellular uptake of NLCs was determined by flow cytometry. Fourier transform infrared spectroscopy and H-NMR spectra confirmed the successful conjugation of LB and SA. The optimized NLCs consisted of 0.5% Solutol HS15 and 10% OA oil. The particle size of these nanoparticles was 139.2 nm, with a zeta potential of 18 mV, loading efficiency of 34.2%, release efficiency after 2 hours of the release test was 72.6%, and crystallinity was 0.63%. The galactosylated NLCs of 5-FU were cytotoxic on the HepG2 cell line in a half concentration of 5-FU and seems promising in reducing 5-FU dose in HCC. © 2012 Informa Healthcare USA, Inc.