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首页> 外文期刊>Biological & pharmaceutical bulletin >Preparation of Chondroitin Sulfate-Glycyl-Prednisolone Conjugate Nanogel and Its Efficacy in Rats with Ulcerative Colitis
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Preparation of Chondroitin Sulfate-Glycyl-Prednisolone Conjugate Nanogel and Its Efficacy in Rats with Ulcerative Colitis

机译：硫酸软骨素 - 甘氨酸 - 甘糖酮醇缀合物纳米凝胶的制备及其在溃疡性结肠炎大鼠大鼠的疗效

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摘要

A conjugate between chondroitin sulfate (CS) and glycyl-prednisolone (GP), named CS-GP, was produced by carbodiimide coupling at a high GP/CS ratio. CS-GP was not water-soluble and gave a nanogel (NG) in aqueous solution. Two types of nanogels, NG(I) and NG(II), with prednisolone (PD) contents of 5.5 and 21.1% (w/w), respectively, were obtained. They had particle sizes of approximately 280 and 570nm, respectively, and showed negative zeta-potentials of approximately -40 mV. The PD release rate was slower in the nanogels than in a solution of CS-GP with a PD content of 1.4% (w/w). The PD release rate was slower in NG(II) than in NG(I), and was elevated at pH 7.4 than at pH 6.8. NG(II) was applied in vivo to rats with trinitrobenzene sulfonic acid (TNBS)-induced colitis, and its therapeutic efficacy and pharmacokinetic features were investigated. The therapeutic efficacy of NG(II) was slightly better than that of PD alone. Drug delivery to the lower intestines was enhanced with NG(II). The CS-GP nanogel has potential as a potent DDS for the treatment of ulcerative colitis.
机译：通过高GP / CS比的碳二亚胺偶联产生硫酸软骨素硫酸盐（Cs）和糖氨基醇酮（GP）之间的缀合物。 CS-GP不溶于水溶性，并在水溶液中纳米凝胶（Ng）。得到两种类型的纳米凝胶，Ng（I）和Ng（II），分别具有5.5和21.1％（w / w）的泼尼松醇（Pd）含量。它们分别具有约280和570nm的粒度，并且显示出约-40mV的负Zeta电位。在纳米凝胶中的Pd释放速率比在CS-GP的溶液中较慢，PD含量为1.4％（w / w）。在Ng（II）中Pd释放速率比Ng（I）较慢，并且在pH 7.4升高而不是pH 6.8。将Ng（II）在体内施用至具有三硝基苯磺酸（TNB）诱导的结肠炎的大鼠，并研究了其治疗效果和药代动力学特征。 Ng（II）的治疗效果略好于单独的Pd。 Ng（II）增强了下肠的药物递送。 CS-GP纳米凝胶具有用于治疗溃疡性结肠炎的有效DDS。

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