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Polyphosphoester-based paclitaxel complexes

机译:基于多磷酸酯的紫杉醇复合物

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We demonstrated a feasible approach for the preparation of a biodegradable, water soluble polyphosphoester based paclitaxel complex. Applying poly(hydroxyoxyethylene phosphate) which contains both a strong proton accepting PO group and a proton donating POH group, paclitaxel has been physically immobilized onto the polymer via H-bonding. The water soluble complex contained 16.7 wt % paclitaxel and more than 4000 times increased drug solubility was achieved. The polymer-drug complex formed nanosized aggregates that were characterized by dynamic light scattering. Intravenous injection of poly(hydroxyoxyethylene phosphate) in rats at a dose of 1000 mg/kg did not induce any clinical signs or body weight gain reduction. (c) 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015, 132, 42772.
机译:我们证明了一种可行的方法来制备可生物降解的,水溶性的基于多磷酸酯的紫杉醇复合物。使用含有强质子接受PO基团和质子给体POH基团的聚(羟基氧乙烯磷酸酯),紫杉醇已通过H键物理固定在聚合物上。该水溶性复合物含有16.7重量%的紫杉醇,并且实现了超过4000倍的药物溶解度增加。聚合物-药物复合物形成纳米聚集体,其特征在于动态光散射。在大鼠中以1000 mg / kg的剂量静脉内注射聚(羟基氧乙烯磷酸酯)不会引起任何临床体征或体重减轻。 (c)2015 Wiley Periodicals,Inc. J. Appl。 Polym。科学2015,132,42772。

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