Preparation And Characteristics Of Liver Targeting Floxuridinyl Diacetate Solid Lipid Nanoparticles

AIMSOur aims were (1) to synthesize Floxuridinyl Diacetate (FUDRA) and galactosides(GnDE); (2) to prepare Floxuridinyl Diacetate Solid Lipid Nanoparticles (FUDRA-SLN) and the Nanoparticles modified by GnDE (FUDRA-GnSLN); (3) to establish HPLC analytical method for the determination of FUDR in biological samples; (4) to observe the distribution of FUDR, FUDRA-SLN and FUDRA-GnSLN in serum and viscera homogenates of the mice; (5) to study the differences of FUDR, FUDRA-SLN and FUDRA-GnSLN for liver-targeting in expectation of developing a new preparation of FUDR that is efficient in treating liver cancer.METHODS1. FUDRA was synthesized by the reaction of floxuridine (FUDR) with acetic anhydride at the presence of pyridine and 4-N',N'-dimethylaminopyridine. The reaction of PnSE [C₁₈H₃₇ (OCH₂CH₂)nOH, n=2,10] with tetraacetylgalactosyl bromide respectively gave...