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Glutamine-chitosan microparticles as oral insulin delivery matrix: In vitro characterization

机译:谷氨酰胺-壳聚糖微粒作为口服胰岛素输送基质:体外表征

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摘要

Chitosan at physiological pH lacks positive charge which reduces the mucoadhesivity and permeation enhancing capacity. Therefore glutamine conjugated chitosan (GC) was developed to enhance the protonation of chitosan at intestinal pH. Particles were prepared by sodium tripolyphosphate ionic crosslinking and were evaluated in vitro for its application toward oral insulin delivery. The particles had high positive charge of 35.6 ± 7.3 mV at physiological pH and a size of 4.434 μm. The mucoadhesive capacity was established in vitro using rat intestinal tissue. Transepithelial electrical resistance (TEER) and confocal microscopy studies proved the ability of the particles in opening the tight junctions in Caco 2 monolayers. The permeation of fluorescent dextran (M_W 4000; FD4) across intestinal tissue was evaluated using Franz diffusion apparatus. It was observed that the GC particles enhanced the permeation by 1.52 fold in comparison with native chitosan (NC) particles.
机译:在生理pH下的壳聚糖缺乏正电荷,这降低了粘膜粘附性和渗透增强能力。因此,开发了谷氨酰胺共轭壳聚糖(GC)以增强肠道pH下壳聚糖的质子化。通过三聚磷酸钠离子交联制备颗粒,并在体外评估其在口服胰岛素递送中的应用。该颗粒在生理pH下具有35.6±7.3mV的高正电荷,尺寸为4.434μm。使用大鼠肠组织在体外建立粘膜粘附能力。经上皮电阻(TEER)和共聚焦显微镜研究证明了颗粒具有打开Caco 2单层紧密连接的能力。使用Franz扩散仪评估荧光葡聚糖(M_W 4000; FD4)在肠道组织中的渗透。观察到,与天然壳聚糖(NC)颗粒相比,GC颗粒的渗透提高了1.52倍。

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