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Preparation,characterization and pharmacokinetics of fluorescence labeled propylene glycol alginate sodium sulfate
Authors:Pengli Li  Chunxia Li  Yiting Xue  Yang Zhang  Hongbing Liu  Xia Zhao  Guangli Yu  Huashi Guan
Institution:1. Key Laboratory of Marine Drugs of Ministry of Education, Provincial Key Laboratory of Glycoscience and Glycotechnology of Shandong, School of Medicine and Pharmacy, Ocean University of China, Qingdao, 266003, P. R. China
Abstract:A rapid and sensitive fluorescence labeling method was developed and validated for the microanalysis of a sulfated polysaccharide drug,namely propylene glycol alginate sodium sulfate (PSS), in rat plasma. Fluorescein isothiocyanate (FITC) was selected to label PSS, and 1, 6-diaminohexane was used to link PSS and FITC in order to prepare FITC-labeled PSS (F-PSS) through a reductive amination reaction. F-PSS was identified by UV-Vis, FT-IR and 1H-NMR spectrum. The cell stability and cytotoxicity of F-PSS were tested in Madin-Darby canine kidney (MDCK) cells. The results indicated that the labeling efficiency of F-PSS was 0.522% ± 0.0248% and the absolute bioavailability was 8.39%. F-PSS was stable in MDCK cells without obvious cytotoxicity. The method was sensitive and reliable; it showed a good linearity, precision, recovery and stability. The FITC labeling method can be applied to investigating the absorption and metabolism of PSS and other polysaccharides in biological samples.
Keywords:propylene glycol alginate sodium sulfate  fluorescence labeling  fluorescein isothiocyanate  pharmacokinetics
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