Purpose

Oral delivery of peptide/protein is quite difficult due to physiological barriers. Encapsulation of these drugs in the suitable biopolymeric matrix could protect the drug as well as increase the residence time of the formulation. Mucoadhesive biopolymers are being widely investigated for this purpose.

Methods

We have fabricated insulin-loaded chemically crosslinked chitosan-alginate macrobeads of approximate size 3 mm per bead. The beads were characterized for surface morphology and polymeric interaction using SEM, EDX, and FTIR, respectively.

Results

The swelling profile and insulin release were analyzed in water and PBS for 9 h. The surface had uniform undulations as observed by SEM. EDX confirmed the chemical crosslinking of chitosan and alginate. FTIR further confirmed the interaction among the polymers. The swelling study revealed a gradual increase for some time and then a decrease in weight possibly due to the disintegration of beads. A cumulative release of approximately 35% was observed by the end of 9 h in both the dissolution medium.

Conclusions

This work is done to investigate the possibility of release of protein/peptide drugs from polysaccharide biopolymer-based blended hydrogel matrix for possible non-invasive delivery of such drugs orally. Here, we have formulated mixed polyelectrolyte hydrogel beads of chitosan and alginate encapsulating insulin as the model drug. Our work shows a sustained release of insulin from the chitosan-alginate beads.

中文翻译：

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壳聚糖-藻酸盐巨珠中胰岛素释放的体外评估

目的

由于生理障碍，口服肽/蛋白质非常困难。将这些药物封装在合适的生物聚合物基质中可以保护药物以及增加制剂的停留时间。为此，粘膜粘附生物聚合物正在被广泛研究。

方法

我们已经制备了胰岛素负载的化学交联的壳聚糖-海藻酸酯大珠，每珠约3毫米。分别使用SEM，EDX和FTIR对微珠的表面形态和聚合物相互作用进行表征。

结果

在水和PBS中分析溶胀曲线和胰岛素释放9小时。通过SEM观察，表面具有均匀的起伏。EDX证实了壳聚糖和藻酸盐的化学交联。FTIR进一步证实了聚合物之间的相互作用。溶胀研究显示一段时间后逐渐增加，然后重量下降可能是由于珠子的崩解所致。在两种溶出介质中，到9 h结束时，观察到累积释放量约为35％。

结论

这项工作是为了研究从基于多糖生物聚合物的混合水凝胶基质中释放蛋白质/肽药物的可能性，从而可能通过口服方式无创地输送此类药物。在这里，我们配制了壳聚糖和藻酸盐的混合聚电解质水凝胶珠，其中囊封了胰岛素作为模型药物。我们的工作表明从壳聚糖-海藻酸盐珠中持续释放胰岛素。