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Oral Administration of Salecan-Based Hydrogels for Controlled Insulin Delivery.
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2018-10-01 , DOI: 10.1021/acs.jafc.8b02879 Xiaoliang Qi 1 , Yue Yuan , Jianfa Zhang 1 , Jeff W M Bulte 2, 3, 4 , Wei Dong 1
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2018-10-01 , DOI: 10.1021/acs.jafc.8b02879 Xiaoliang Qi 1 , Yue Yuan , Jianfa Zhang 1 , Jeff W M Bulte 2, 3, 4 , Wei Dong 1
Affiliation
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We present an improved type of food gum (salecan) based hydrogels for oral delivery of insulin. Structural hydrogel formation was assessed with Fourier transform infrared spectroscopy, thermogravimetric analysis, and X-ray diffraction. We found that the hydrogel modulus, morphology, and swelling properties can be controlled by varying the salecan dose during hydrogel formation. Insulin was introduced into the hydrogel using a swelling-diffusion approach and then further used a drug prototype. In vitro insulin release profiles demonstrated that the release of entrapped insulin was suppressed in acidic conditions but markedly increased at neutral pH. Cell viability and toxicity tests revealed that the salecan hydrogel constructs were biocompatible. Oral administration of insulin-loaded salecan hydrogels in diabetic rats resulted in a sustained decrease of fasting plasma glucose levels over 6 h postadministration. For nondiabetic animals, the relative pharmacological bioavailability of insulin was significantly larger (6.24%, p < 0.05) for insulin-loaded hydrogels compared to free insulin. These results encourage further development of salecan-based hydrogels as vehicles for controlled insulin delivery following oral administration.
中文翻译：
口服基于 Salecan 的水凝胶用于控制胰岛素输送。
我们提出了一种改进类型的基于食品胶（salecan）的水凝胶，用于口服胰岛素。通过傅里叶变换红外光谱、热重分析和 X 射线衍射评估结构水凝胶的形成。我们发现，水凝胶模量、形态和溶胀特性可以通过改变水凝胶形成过程中的萨利坎剂量来控制。使用溶胀扩散方法将胰岛素引入水凝胶中，然后进一步使用药物原型。体外胰岛素释放曲线表明，包埋胰岛素的释放在酸性条件下受到抑制，但在中性 pH 条件下显着增加。细胞活力和毒性测试表明，salecan 水凝胶结构具有生物相容性。糖尿病大鼠口服负载胰岛素的苏莱坎水凝胶，导致给药后 6 小时内空腹血糖水平持续下降。对于非糖尿病动物，与游离胰岛素相比，装载胰岛素的水凝胶的胰岛素相对药理学生物利用度显着更大（6.24%，p < 0.05）。这些结果鼓励进一步开发基于 salecan 的水凝胶作为口服给药后控制胰岛素输送的载体。
更新日期：2018-09-21
中文翻译：
口服基于 Salecan 的水凝胶用于控制胰岛素输送。
我们提出了一种改进类型的基于食品胶（salecan）的水凝胶，用于口服胰岛素。通过傅里叶变换红外光谱、热重分析和 X 射线衍射评估结构水凝胶的形成。我们发现，水凝胶模量、形态和溶胀特性可以通过改变水凝胶形成过程中的萨利坎剂量来控制。使用溶胀扩散方法将胰岛素引入水凝胶中，然后进一步使用药物原型。体外胰岛素释放曲线表明，包埋胰岛素的释放在酸性条件下受到抑制，但在中性 pH 条件下显着增加。细胞活力和毒性测试表明，salecan 水凝胶结构具有生物相容性。糖尿病大鼠口服负载胰岛素的苏莱坎水凝胶，导致给药后 6 小时内空腹血糖水平持续下降。对于非糖尿病动物，与游离胰岛素相比，装载胰岛素的水凝胶的胰岛素相对药理学生物利用度显着更大（6.24%，p < 0.05）。这些结果鼓励进一步开发基于 salecan 的水凝胶作为口服给药后控制胰岛素输送的载体。
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