The aim of this study was the synthesis and in vitro characterization of aminated cellulose as alternative excipient to chitosan. The aldehyde form of cellulose was generated via the oxidative cleavage of vicinal diols by the addition of increasing concentrations of sodium periodate. The insertion of primary amines was achieved by reductive amination with ammonia. The degree of substitution was calculated via primary amino group quantification using a 2,4,6-trinitrobenzenesulfonic acid assay. Mucoadhesiveness was examined by adopting the rotating-cylinder method and tensile studies using porcine intestinal mucosa. Hydration was evaluated at pH 2–11. The successful formation of aldehydes as well as a subsequent introduction of up to 311.61 micromoles per gram of primary amines were proven to correlate with the amount of added periodate. There was a 3- to 14-fold prolongation in the mucosal residence time of the new polymer in comparison to chitosan, as measured by the rotating-cylinder method. Although cationic cellulose did not reach the maximum detachment force of chitosan, the total work of adhesion of the newly synthesized cellulose derivate was higher than that of chitosan. The higher the degree of amination, the higher the degree of hydration in neutral and alkaline aqueous media was. Compared to chitosan, the novel cationic cellulose derivative displays improved mucoadhesive properties as well as sufficient hydration at physiological pH. Therefore, aminated cellulose is a promising alternative to the cationic polymers, such as chitosan, used thus far.

中文翻译：

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壳聚糖：唯一的吗？胺化纤维素是含聚合物伯氨基的创新选择

这项研究的目的是胺化纤维素作为壳聚糖的替代赋形剂的合成和体外表征。纤维素的醛形式是通过添加浓度递增的高碘酸钠通过邻二醇的氧化裂解而产生的。伯胺的插入是通过用氨进行还原胺化来实现的。取代度通过使用2,4,6-三硝基苯磺酸测定的伯氨基基团定量来计算。通过采用旋转圆筒法和使用猪肠粘膜的拉伸研究来检查粘膜粘附性。在pH 2-11下评估水合作用。醛的成功形成以及随后引入的每克伯胺高达311.61微摩尔被证明与高碘酸盐的添加量相关。通过旋转圆筒法测定，与壳聚糖相比，新聚合物的黏膜停留时间延长了3到14倍。尽管阳离子纤维素没有达到壳聚糖的最大剥离力，但新合成的纤维素衍生物的总粘合功却高于壳聚糖。胺化度越高，在中性和碱性水性介质中的水合度越高。与壳聚糖相比，新型阳离子纤维素衍生物在生理pH值下具有改善的粘膜粘附性能以及足够的水合作用。因此，胺化纤维素是迄今为止所用的阳离子聚合物（例如壳聚糖）的一种有前途的替代品。通过旋转圆筒法测量。尽管阳离子纤维素没有达到壳聚糖的最大剥离力，但新合成的纤维素衍生物的总粘合功却高于壳聚糖。胺化程度越高，在中性和碱性水性介质中的水合程度越高。与壳聚糖相比，新型阳离子纤维素衍生物在生理pH值下显示出改善的粘膜粘附特性​​以及足够的水合作用。因此，胺化纤维素是迄今为止所用的阳离子聚合物（例如壳聚糖）的一种有前途的替代品。通过旋转圆筒法测量。尽管阳离子纤维素没有达到壳聚糖的最大剥离力，但新合成的纤维素衍生物的总粘合功却高于壳聚糖。胺化度越高，在中性和碱性水性介质中的水合度越高。与壳聚糖相比，新型阳离子纤维素衍生物在生理pH值下具有改善的粘膜粘附性能以及足够的水合作用。因此，胺化纤维素是迄今为止所用的阳离子聚合物（例如壳聚糖）的一种有前途的替代品。胺化度越高，在中性和碱性水性介质中的水合度越高。与壳聚糖相比，新型阳离子纤维素衍生物在生理pH值下具有改善的粘膜粘附性能以及足够的水合作用。因此，胺化纤维素是迄今为止所用的阳离子聚合物（例如壳聚糖）的一种有前途的替代品。胺化度越高，在中性和碱性水性介质中的水合度越高。与壳聚糖相比，新型阳离子纤维素衍生物在生理pH值下具有改善的粘膜粘附性能以及足够的水合作用。因此，胺化纤维素是迄今为止所用的阳离子聚合物（例如壳聚糖）的一种有前途的替代品。