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首页> 美国卫生研究院文献>International Journal of Nanomedicine >Nanoemulsions coated with alginate/chitosan as oral insulin delivery systems: preparation characterization and hypoglycemic effect in rats
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Nanoemulsions coated with alginate/chitosan as oral insulin delivery systems: preparation characterization and hypoglycemic effect in rats

机译：藻酸盐/壳聚糖包衣的纳米乳剂作为口服胰岛素输送系统：在大鼠中的制备表征和降血糖作用

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This study aimed to prepare nanoemulsions coated with alginate/chitosan for oral insulin delivery. Uncoated nanoemulsions were prepared by homogenization of a water in oil in water (w/o/w) multiple emulsion that was composed of Labrafac® CC, phospholipid, Span™ 80 and Cremorphor® EL. Coating of the nanoemulsions was achieved based on polyelectrolyte cross-linking, with sequential addition of calcium chloride and chitosan to the bulk nanoemulsion dispersion that contained alginate. The particle size of the coated nanoemulsions was about 488 nm and the insulin entrapment ratio was 47.3%. Circular dichroism spectroscopy proved conformational stability of insulin against the preparative stress. In vitro leakage study indicated well-preserved integrity of the nanoemulsions in simulated gastric juices. Hypoglycemic effects were observed in both normal and diabetic rats. The relative pharmacological bioavailability of the coated nanoemulsion with 25 and 50 IU/kg insulin were 8.42% and 5.72% in normal rats and 8.19% and 7.84% in diabetic rats, respectively. Moreover, there were significantly prolonged hypoglycemic effects after oral administration of the coated nanoemulsions compared with subcutaneous (sc) insulin. In conclusion, the nanoemulsion coated with alginate/chitosan was a potential delivery system for oral delivery of polypeptides and proteins.
机译：这项研究旨在制备纳米藻酸盐/壳聚糖包衣的纳米乳剂，用于口服胰岛素递送。通过将由Labrafac ® CC，磷脂，Span™80和Cremorphor ®组成的水包油（w / o / w）多元乳化液均质化来制备未涂覆的纳米乳液。 sup> EL。纳米乳液的涂层是基于聚电解质交联而实现的，向包含藻酸盐的本体纳米乳液分散体中依次添加氯化钙和壳聚糖。涂覆的纳米乳剂的粒径为约488nm，胰岛素的包封率为47.3％。圆二色光谱证明胰岛素对制备应力的构象稳定性。体外渗漏研究表明，模拟胃液中纳米乳的保存完好。在正常和糖尿病大鼠中均观察到降血糖作用。用25和50 IU / kg胰岛素包被的纳米乳剂的相对药理生物利用度在正常大鼠中分别为8.42％和5.72％，在糖尿病大鼠中分别为8.19％和7.84％。此外，与皮下（sc）胰岛素相比，口服给予包衣的纳米乳剂后，降血糖作用明显延长。总之，用藻酸盐/壳聚糖包衣的纳米乳剂是用于口服递送多肽和蛋白质的潜在递送系统。

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