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Influence of Molecular Weight and Degree of Deacetylation of Low Molecular Weight Chitosan on the Bioactivity of Oral Insulin Preparations

机译:分子量和低分子量壳聚糖脱乙酰度对口服胰岛素制剂生物活性的影响

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摘要

The objective of the present study was to prepare and characterize low molecular weight chitosan (LMWC) with different molecular weight and degrees of deacetylation (DDA) and to optimize their use in oral insulin nano delivery systems. Water in oil nanosized systems containing LMWC-insulin polyelectrolyte complexes were constructed and their ability to reduce blood glucose was assessed in vivo on diabetic rats. Upon acid depolymerization and testing by viscosity method, three molecular weights of LMWC namely, 1.3, 13 and 18 kDa were obtained. As for the DDA, three LMWCs of 55%, 80% and 100% DDA were prepared and characterized by spectroscopic methods for each molecular weight. The obtained LMWCs showed different morphological and in silico patterns. Following complexation of LMWCs with insulin, different aggregation sizes were obtained. Moreover, the in vivo tested formulations showed different activities of blood glucose reduction. The highest glucose reduction was achieved with 1.3 kDa LMWC of 55% DDA. The current study emphasizes the importance of optimizing the molecular weight along with the DDA of the incorporated LMWC in oral insulin delivery preparations in order to ensure the highest performance of such delivery systems.
机译:本研究的目的是制备和表征具有不同分子量和脱乙酰度(DDA)的低分子量壳聚糖(LMWC),并优化其在口服胰岛素纳米递送系统中的使用。构建了包含LMWC-胰岛素聚电解质复合物的油纳米级系统中的水,并在糖尿病大鼠体内评估了它们降低血糖的能力。通过酸解聚并通过粘度法进行测试,获得三个分子量的LMWC,即1.3、13和18kDa。对于DDA,制备了55%,80%和100%DDA的三种LMWC,并通过光谱法对每种分子量进行了表征。所获得的LMWC显示出不同的形态和计算机模式。 LMWC与胰岛素复合后,获得了不同的聚集大小。此外,体内测试的制剂显示出降低血糖的不同活性。用55%DDA的1.3 kDa LMWC可获得最高的葡萄糖减少量。当前的研究强调了在口服胰岛素输送制剂中优化掺入的LMWC的分子量以及DDA的重要性,以确保此类输送系统的最高性能。

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